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Apoptosis

As one of the cellular death mechanisms, apoptosis, also known as programmed cell death, can be defined as the process of a proper death of any cell under certain or necessary conditions. Apoptosis is controlled by the interactions between several molecules and responsible for the elimination of unwanted cells from the body.

Many biochemical events and a series of morphological changes occur at the early stage and increasingly continue till the end of apoptosis process. Morphological event cascade including cytoplasmic filament aggregation, nuclear condensation, cellular fragmentation, and plasma membrane blebbing finally results in the formation of apoptotic bodies. Several biochemical changes such as protein modifications/degradations, DNA and chromatin deteriorations, and synthesis of cell surface markers form morphological process during apoptosis.

Apoptosis can be stimulated by two different pathways: (1) intrinsic pathway (or mitochondria pathway) that mainly occurs via release of cytochrome c from the mitochondria and (2) extrinsic pathway when Fas death receptor is activated by a signal coming from the outside of the cell.

Different gene families such as caspases, inhibitor of apoptosis proteins, B cell lymphoma (Bcl)-2 family, tumor necrosis factor (TNF) receptor gene superfamily, or p53 gene are involved and/or collaborate in the process of apoptosis.

Caspase family comprises conserved cysteine aspartic-specific proteases, and members of caspase family are considerably crucial in the regulation of apoptosis. There are 14 different caspases in mammals, and they are basically classified as the initiators including caspase-2, -8, -9, and -10; and the effectors including caspase-3, -6, -7, and -14; and also the cytokine activators including caspase-1, -4, -5, -11, -12, and -13. In vertebrates, caspase-dependent apoptosis occurs through two main interconnected pathways which are intrinsic and extrinsic pathways. The intrinsic or mitochondrial apoptosis pathway can be activated through various cellular stresses that lead to cytochrome c release from the mitochondria and the formation of the apoptosome, comprised of APAF1, cytochrome c, ATP, and caspase-9, resulting in the activation of caspase-9. Active caspase-9 then initiates apoptosis by cleaving and thereby activating executioner caspases. The extrinsic apoptosis pathway is activated through the binding of a ligand to a death receptor, which in turn leads, with the help of the adapter proteins (FADD/TRADD), to recruitment, dimerization, and activation of caspase-8 (or 10). Active caspase-8 (or 10) then either initiates apoptosis directly by cleaving and thereby activating executioner caspase (-3, -6, -7), or activates the intrinsic apoptotic pathway through cleavage of BID to induce efficient cell death. In a heat shock-induced death, caspase-2 induces apoptosis via cleavage of Bid.

Bcl-2 family members are divided into three subfamilies including (i) pro-survival subfamily members (Bcl-2, Bcl-xl, Bcl-W, MCL1, and BFL1/A1), (ii) BH3-only subfamily members (Bad, Bim, Noxa, and Puma9), and (iii) pro-apoptotic mediator subfamily members (Bax and Bak). Following activation of the intrinsic pathway by cellular stress, pro‑apoptotic BCL‑2 homology 3 (BH3)‑only proteins inhibit the anti‑apoptotic proteins Bcl‑2, Bcl-xl, Bcl‑W and MCL1. The subsequent activation and oligomerization of the Bak and Bax result in mitochondrial outer membrane permeabilization (MOMP). This results in the release of cytochrome c and SMAC from the mitochondria. Cytochrome c forms a complex with caspase-9 and APAF1, which leads to the activation of caspase-9. Caspase-9 then activates caspase-3 and caspase-7, resulting in cell death. Inhibition of this process by anti‑apoptotic Bcl‑2 proteins occurs via sequestration of pro‑apoptotic proteins through binding to their BH3 motifs.

One of the most important ways of triggering apoptosis is mediated through death receptors (DRs), which are classified in TNF superfamily. There exist six DRs: DR1 (also called TNFR1); DR2 (also called Fas); DR3, to which VEGI binds; DR4 and DR5, to which TRAIL binds; and DR6, no ligand has yet been identified that binds to DR6. The induction of apoptosis by TNF ligands is initiated by binding to their specific DRs, such as TNFα/TNFR1, FasL /Fas (CD95, DR2), TRAIL (Apo2L)/DR4 (TRAIL-R1) or DR5 (TRAIL-R2). When TNF-α binds to TNFR1, it recruits a protein called TNFR-associated death domain (TRADD) through its death domain (DD). TRADD then recruits a protein called Fas-associated protein with death domain (FADD), which then sequentially activates caspase-8 and caspase-3, and thus apoptosis. Alternatively, TNF-α can activate mitochondria to sequentially release ROS, cytochrome c, and Bax, leading to activation of caspase-9 and caspase-3 and thus apoptosis. Some of the miRNAs can inhibit apoptosis by targeting the death-receptor pathway including miR-21, miR-24, and miR-200c.

p53 has the ability to activate intrinsic and extrinsic pathways of apoptosis by inducing transcription of several proteins like Puma, Bid, Bax, TRAIL-R2, and CD95.

Some inhibitors of apoptosis proteins (IAPs) can inhibit apoptosis indirectly (such as cIAP1/BIRC2, cIAP2/BIRC3) or inhibit caspase directly, such as XIAP/BIRC4 (inhibits caspase-3, -7, -9), and Bruce/BIRC6 (inhibits caspase-3, -6, -7, -8, -9). 

Any alterations or abnormalities occurring in apoptotic processes contribute to development of human diseases and malignancies especially cancer.

References:
1.Yağmur Kiraz, Aysun Adan, Melis Kartal Yandim, et al. Major apoptotic mechanisms and genes involved in apoptosis[J]. Tumor Biology, 2016, 37(7):8471.
2.Aggarwal B B, Gupta S C, Kim J H. Historical perspectives on tumor necrosis factor and its superfamily: 25 years later, a golden journey.[J]. Blood, 2012, 119(3):651.
3.Ashkenazi A, Fairbrother W J, Leverson J D, et al. From basic apoptosis discoveries to advanced selective BCL-2 family inhibitors[J]. Nature Reviews Drug Discovery, 2017.
4.McIlwain D R, Berger T, Mak T W. Caspase functions in cell death and disease[J]. Cold Spring Harbor perspectives in biology, 2013, 5(4): a008656.
5.Ola M S, Nawaz M, Ahsan H. Role of Bcl-2 family proteins and caspases in the regulation of apoptosis[J]. Molecular and cellular biochemistry, 2011, 351(1-2): 41-58.

What is Apoptosis? The Apoptotic Pathways and the Caspase Cascade

Targets for  Apoptosis

Products for  Apoptosis

  1. Cat.No. Nombre del producto Información
  2. GC10350 TIC10 isomer

    ONC201 isomer

    El isÓmero TIC10 es el isÓmero de TIC10.  TIC10 isomer  Chemical Structure
  3. GC41183 α-Carotene

    all-trans-α-Carotene

    α-El caroteno, precursor de la vitamina A, se utiliza como agente antimetastÁsico o como adyuvante de fÁrmacos contra el cÁncer. α-El caroteno se aÍsla de vegetales de color amarillo-naranja y verde oscuro. α-Carotene  Chemical Structure
  4. GC48292 α-MSH (human, mouse, rat, porcine, bovine, ovine) (trifluoroacetate salt)

    α-Melanocyte-stimulating Hormone, Ac-SYSMEHFRWGKPV-NH2

    α-MSH (α-Melanocyte-Stimulating Hormone) TFA, un neuropéptido endÓgeno, es un agonista endÓgeno del receptor 4 de melanocortina (MC4R) con actividades antiinflamatorias y antipiréticas. α-MSH (human, mouse, rat, porcine, bovine, ovine) (trifluoroacetate salt)  Chemical Structure
  5. GC45213 α-NETA α-NETA es un inhibidor potente y no competitivo de colina acetiltransferasa (ChA; IC50\u003d76 μM) y colinesterasa (ChE; IC50\u003d40 µM). α-NETA inhibe débilmente la acetilcolinesterasa (AChE; IC50\u003d1 mM). α-NETA  Chemical Structure
  6. GC41499 α-Phellandrene

    p-Mentha-1,5-diene, (±)-α-Phellandrene

    α-Phellandrene is a cyclic monoterpene that has been found in various plants, including Cannabis, and has diverse biological activities. α-Phellandrene  Chemical Structure
  7. GC63941 α-Solanine α se ha observado que la solanina, un componente bioactivo y uno de los principales glicoalcaloides esteroideos de las patatas, inhibe el crecimiento e induce la apoptosis en las células cancerosas. α-Solanine  Chemical Structure
  8. GC67618 α-Tocopherol phosphate disodium

    alpha-Tocopherol phosphate disodium; TocP disodium; Vitamin E phosphate disodium

    α-El fosfato de tocoferol (fosfato de alfa-tocoferol) disódico, un antioxidante prometedor, puede proteger contra la muerte celular inducida por UVA1 de onda larga y eliminar las ROS inducidas por UVA1 en un modelo de células de la piel. α-El fosfato de tocoferol disódico posee potencial terapéutico en la inhibición de la apoptosis y aumenta la capacidad migratoria de las células progenitoras endoteliales en condiciones de hiperglucemia/hipoxia y promueve la angiogénesis. α-Tocopherol phosphate disodium  Chemical Structure
  9. GC48920 β-Carboline-1-carboxylic Acid

    1-Formic Acid-β-carboline

    An alkaloid with diverse biological activities β-Carboline-1-carboxylic Acid  Chemical Structure
  10. GC41623 β-Elemonic Acid

    Elemadienonic Acid, 3-Oxotirucallenoic Acid, 3-oxo Tirucallic Acid

    β-El Ácido elemÓnico es un triterpeno aislado de Boswellia papyrifera. β-Elemonic Acid  Chemical Structure
  11. GC64619 β-Ionone β-La ionona es eficaz en la inducciÓn de apoptosis en células de adenocarcinoma gÁstrico SGC7901. Actividad anticancerÍgena. β-Ionone  Chemical Structure
  12. GC66048 δ-Secretase inhibitor 11 δ-El inhibidor de secretasa 11 (compuesto 11) es un inhibidor de secretasa oralmente activo, potente, penetrado por BBB, no tÓxico, selectivo y especÍfico, con un IC50 de 0,7 μM. δ-El inhibidor de secretasa 11 interactÚa tanto con el sitio activo como con el sitio alostérico de δ-secretasa. δ-El inhibidor de secretasa 11 atenÚa la escisiÓn de tau y APP (proteÍna precursora de amiloide). δ-El inhibidor de secretasa 11 mejora la disfunciÓn sinÁptica y los deterioros cognitivos en modelos de ratones transgénicos tau P301S y 5XFAD. δ-El inhibidor de secretasa 11 puede usarse para la investigaciÓn de la enfermedad de Alzheimer's. δ-Secretase inhibitor 11  Chemical Structure
  13. GC46008 (±)-Thalidomide-d4

    N-Phthaloylglutamimide-d4

    (±)-Thalidomide-d4 es una talidomida marcada con deuterio. (±)-Thalidomide-d4  Chemical Structure
  14. GC45618 (±)-trans-GK563

    GK563

    A GVIA iPLA2 inhibitor (±)-trans-GK563  Chemical Structure
  15. GC45270 (±)10(11)-EDP Ethanolamide

    10,11-EDP-EA, 10,11-EDP epoxide, 10,11-epoxy Docosapentaenoic Ethanolamide

    (±)10(11)-EDP ethanolamide is an ω-3 endocannabinoid epoxide and cannabinoid (CB) receptor agonist (EC50s = 0.43 and 22.5 nM for CB1 and CB2 receptors, respectively). (±)10(11)-EDP Ethanolamide  Chemical Structure
  16. GC49268 (+)-δ-Cadinene A sesquiterpene with antimicrobial and anticancer activities (+)-δ-Cadinene  Chemical Structure
  17. GC18516 (+)-Aeroplysinin-1

    NSC 170364

    (+)-Aeroplysinin-1 ((+)-Aeroplysinin-1), un metabolito secundario aislado de esponjas marinas, muestra potentes efectos antibióticos en bacterias grampositivas y ejerce actividad antiviral contra el VIH-1 (IC50 \u003d 14,6 μM). (+)-Aeroplysinin-1  Chemical Structure
  18. GC17008 (+)-Apogossypol (+)-Apogossypol es un antagonista pan-BCL-2. (+)-Apogossypol se une a Mcl-1, Bcl-2 y Bcl-xL con EC50 de 2,6, 2,8 y 3,69 μM, respectivamente. (+)-Apogossypol  Chemical Structure
  19. GC45256 (+)-ar-Turmerone

    (S)(+)arTurmerone

    (+)-ar-Turmerone ((+)-(+)-ar-Turmerone) es un importante compuesto bioactivo de la hierba Curcuma longa con actividades antitumorales y antiinflamatorias. (+)-ar-Turmerone  Chemical Structure
  20. GN10654 (+)-Corynoline

    (+)-Corynoline, 13-methyl-Chelidonine, CRL, (d)-Corynoline

    (+)-Corynoline  Chemical Structure
  21. GC31691 (+)-DHMEQ

    (1R,2R,6R)-Dehydroxymethylepoxyquinomicin; (1R,2R,6R)-DHMEQ

    (+)-DHMEQ es un activador del factor de transcripciÓn antioxidante Nrf2. (+)-DHMEQ  Chemical Structure
  22. GC45265 (+)-Goniothalesdiol (+)-Goniothalesdiol, isolated from the bark of the Malaysian tree G. (+)-Goniothalesdiol  Chemical Structure
  23. GC45274 (+)-Pinoresinol

    NSC 35444

    (+)-Pinoresinol es un lignol de origen vegetal que sirve para la defensa en una oruga. (+)-Pinoresinol sensibiliza drásticamente las células cancerosas contra la apoptosis inducida por el ligando inductor de apoptosis relacionado con TNF (TRAIL). (+)-Pinoresinol  Chemical Structure
  24. GC18749 (+)-Rugulosin

    NSC 160880, NSC 249990, Rugulosin A

    (+) - La rugulosina es una materia colorante cristalina de Penicillium rugulosum Thom. (+)-Rugulosin  Chemical Structure
  25. GC41345 (-)-α-Bisabolol

    DL-α-Bisabolol

    (-)-α-Bisabolol ((-)-α-Bisabolol), un alcohol sesquiterpénico monocÍclico, ejerce actividades antioxidantes, antiinflamatorias y antiapoptÓticas. (-)-α-Bisabolol  Chemical Structure
  26. GC49502 (-)-β-Sesquiphellandrene A sesquiterpene with antiviral and anticancer activities (-)-β-Sesquiphellandrene  Chemical Structure
  27. GC45244 (-)-(α)-Kainic Acid (hydrate)

    Un potente estimulante del sistema nervioso central para la inducción de convulsiones.

    (-)-(α)-Kainic Acid (hydrate)  Chemical Structure
  28. GC45246 (-)-Chaetominine

    (-)-Chaetominine

    La (-)-chaetominina es un metabolito alcaloidal. La (-)-chaetominina tiene citotoxicidad contra la leucemia humana K562 y las líneas celulares de cáncer de colon SW1116. (-)-Chaetominine reduce la resistencia a fármacos mediada por MRP1 a través de la inhibición de la vía de señalización PI3K/Akt/Nrf2 en células de leucemia humana K562/Adr. (-)-Chaetominine  Chemical Structure
  29. GC40698 (-)-Perillyl Alcohol

    (L)-Perillyl Alcohol, (S)-Perillic Alcohol, (S)-(–)-Perillyl Alcohol

    (-)-El alcohol perilÍlico es un monoterpeno que se encuentra en la lavanda, inhibe la farnesilaciÓn de Ras, regula al alza el receptor de manosa-6-fosfato e induce la apoptosis. Actividad anticancerÍgena. (-)-Perillyl Alcohol  Chemical Structure
  30. GC40076 (-)-Voacangarine

    NSC 306219, (-)-Voacristine

    (-)-Voacangarine is an indole alkaloid originally isolated from V. (-)-Voacangarine  Chemical Structure
  31. GC62193 (1S,2S)-Bortezomib (1S,2S)-bortezomib es un enantiÓmero de bortezomib. Bortezomib es un inhibidor del proteasoma selectivo, reversible y permeable a las células, e inhibe potentemente el proteasoma 20S (Ki de 0,6 nM) al dirigirse a un residuo de treonina. Bortezomib interrumpe el ciclo celular, induce la apoptosis e inhibe el NF-κB. Bortezomib es un agente anticancerÍgeno y el primer inhibidor terapéutico del proteasoma que se usa en humanos. (1S,2S)-Bortezomib  Chemical Structure
  32. GC34965 (20S)-Protopanaxatriol

    20(S)-APPT, 20(S)-PPT

    Un metabolito activo de ginsenósido.

    (20S)-Protopanaxatriol  Chemical Structure
  33. GC60397 (5Z,2E)-CU-3 (5Z,2E)-CU-3 es un inhibidor potente y selectivo contra la isoenzima α de DGK con un valor de IC50 de 0,6 μM, inhibe competitivamente la afinidad de DGKα por ATP con un valor de Km de 0,48 mM. (5Z,2E)-CU-3 se dirige a la regiÓn catalÍtica, pero no a la regiÓn reguladora de DGKα. (5Z,2E)-CU-3 tiene efectos antitumorales y proinmunogénicos, potencia la apoptosis de las células cancerosas y la activaciÓn de las células T. (5Z,2E)-CU-3  Chemical Structure
  34. GC60398 (6R)-FR054 (6R)-FR054 es un isÓmero menos activo de FR054. (6R)-FR054  Chemical Structure
  35. GC50482 (D)-PPA 1 PD-1/PD-L1 interaction inhibitor (D)-PPA 1  Chemical Structure
  36. GC69009 (D)-PPA 1 TFA

    (D)-PPA 1 TFA es un antagonista de péptido D anti-hidrólisis. Es un inhibidor efectivo de PD-1/PD-L1. La afinidad de (D)-PPA 1 TFA por la unión a PD-1 es de 0,51 μM y es efectivo tanto in vitro como in vivo.

    (D)-PPA 1 TFA  Chemical Structure
  37. GA20156 (D-Ser(tBu)⁶,Azagly¹⁰)-LHRH (free base) (D-Ser(tBu)⁶,Azagly¹⁰)-LHRH (free base)  Chemical Structure
  38. GC41700 (E)-2-(2-Chlorostyryl)-3,5,6-trimethylpyrazine

    CSTMP

    (E)-2-(2-Chlorostyryl)-3,5,6-trimethylpyrazine (CSTMP) is a stilbene derivative with antioxidant and anticancer activities. (E)-2-(2-Chlorostyryl)-3,5,6-trimethylpyrazine  Chemical Structure
  39. GC41268 (E)-2-Hexadecenal

    trans-2-Hexadecenal

    Sphingosine-1-phosphate (S1P), a bioactive lipid involved in many signaling processes, is irreversibly degraded by the membrane-bound S1P lyase. (E)-2-Hexadecenal  Chemical Structure
  40. GC41701 (E)-2-Hexadecenal Alkyne (E)-2-Hexadecenal alkyne is an alkyne version of the sphingolipid degradation product (E)-2-hexadecenal that can be used as a click chemistry probe. (E)-2-Hexadecenal Alkyne  Chemical Structure
  41. GC34980 (E)-Ferulic acid El Ácido (E)-ferÚlico es un isÓmero del Ácido ferÚlico, que es un compuesto aromÁtico, abundante en las paredes celulares de las plantas. El Ácido (E)-ferÚlico provoca la fosforilaciÓn de la β-catenina, lo que da como resultado la degradaciÓn proteasomal de la β-catenina y aumenta la expresiÓn del factor proapoptÓtico Bax y disminuye la expresiÓn del factor prosupervivencia survivina. El Ácido (E)-ferÚlico muestra una potente capacidad para eliminar las especies reactivas de oxÍgeno (ROS) e inhibe la peroxidaciÓn lipÍdica. El Ácido (E)-ferÚlico ejerce efectos antiproliferaciÓn y antimigraciÓn en la lÍnea celular de cÁncer de pulmÓn humano H1299. (E)-Ferulic acid  Chemical Structure
  42. GC34981 (E)-Flavokawain A

    Flavokavain A, 4-methoxy Flavokawain B

    (E)-Flavokawain A, una chalcona extraÍda de Kava, tiene efecto anticancerÍgeno. (E)-Flavokawain A induce la apoptosis en células de cÁncer de vejiga mediante la participaciÓn de la vÍa apoptÓtica dependiente de la proteÍna bax y dependiente de las mitocondrias y suprime el crecimiento tumoral en ratones. (E)-Flavokawain A  Chemical Structure
  43. GC61437 (E)-Methyl 4-coumarate

    trans-4-Coumaric Acid methyl ester, trans-p-Coumaric Acid methyl ester, trans-para-Coumaric Acid methyl ester

    (E)-4-Cumarato de metilo (4-hidroxicinamato de metilo), que se encuentra en varias plantas, como la cebolla verde (Allium cepa) o el noni (Morinda citrifolia L. (E)-Methyl 4-coumarate  Chemical Structure
  44. GC34125 (E)-[6]-Dehydroparadol (E)-[6]-Dehydroparadol, un metabolito oxidativo de [6]-Shogaol, es un potente activador de Nrf2. (E)-[6]-Dehydroparadol puede inhibir el crecimiento e inducir la apoptosis de células cancerosas humanas. (E)-[6]-Dehydroparadol  Chemical Structure
  45. GC49189 (E/Z)-4-hydroxy Tamoxifen-d5

    Afimoxifene-d5, 4-OHT-d5

    An internal standard for the quantification of (E/Z)-4-hydroxy tamoxifen (E/Z)-4-hydroxy Tamoxifen-d5  Chemical Structure
  46. GN10783 (R) Ginsenoside Rh2 (R) Ginsenoside Rh2  Chemical Structure
  47. GC15104 (R)-(+)-Etomoxir sodium salt

    (R)(+)Etomoxir

    La sal sÓdica de etomoxir((R)-(+)-Etomoxir) es un inhibidor irreversible de la carnitina palmitoiltransferasa 1a (CPT-1a), inhibe la oxidaciÓn de Ácidos grasos (FAO) a través de CPT-1a e inhibe la oxidaciÓn del palmitato en humanos, ratas y conejillo de indias. (R)-(+)-Etomoxir sodium salt  Chemical Structure
  48. GC34096 (R)-(-)-Gossypol acetic acid (AT-101 (acetic acid)) El Ácido acético (R)-(-)-gosipol (AT-101 (Ácido acético)) (AT-101 (Ácido acético)) es el isÓmero levorrotatorio de un producto natural Gosipol. Se determina que AT-101 se une a las proteÍnas Bcl-2, Mcl-1 y Bcl-xL con Kis de 260±30 nM, 170±10 nM y 480±40 nM, respectivamente. (R)-(-)-Gossypol acetic acid (AT-101 (acetic acid))  Chemical Structure
  49. GC65610 (R)-5-Hydroxy-1,7-diphenyl-3-heptanone La (R)-5-hidroxi-1,7-difenil-3-heptanona es un diarilheptanoide que se puede encontrar en Alpinia officinarum. (R)-5-Hydroxy-1,7-diphenyl-3-heptanone  Chemical Structure
  50. GC41716 (R)-CR8 (R)-CR8 (CR8), un análogo de segunda generación de roscovitina, es un potente inhibidor de CDK1/2/5/7/9. (R)-CR8  Chemical Structure
  51. GC39281 (R)-CR8 trihydrochloride

    CR8, (R)-Isomer trihydrochloride

    El triclorhidrato de (R)-CR8 (CR8), un anÁlogo de segunda generaciÓn de la roscovitina, es un potente inhibidor de CDK1/2/5/7/9. (R)-CR8 trihydrochloride  Chemical Structure
  52. GC41719 (R)-nitro-Blebbistatin

    R(-)7Desmethyl8nitro Blebbistatin

    (R)-nitro-Blebbistatin is a more stable form of (+)-blebbistatin, which is the inactive form of (-)-blebbistatin. (R)-nitro-Blebbistatin  Chemical Structure
  53. GC60407 (R)-Verapamil D7 hydrochloride

    (R)-(+)-Verapamil D7 hydrochloride

    El clorhidrato de (R)-Verapamilo D7 ((R)-(+)-clorhidrato de Verapamilo D7) es un clorhidrato de (R)-Verapamilo marcado con deuterio. (R)-clorhidrato de verapamilo ((R)-(+)-clorhidrato de verapamilo) es un inhibidor de la glicoproteÍna P. El clorhidrato de (R)-verapamilo bloquea el transporte mediado por MRP1, lo que da como resultado la quimiosensibilizaciÓn de las células que sobreexpresan MRP1 a los medicamentos contra el cÁncer. (R)-Verapamil D7 hydrochloride  Chemical Structure
  54. GC60408 (R)-Verapamil hydrochloride (R)-clorhidrato de verapamilo ((R)-(+)-clorhidrato de verapamilo) es un inhibidor de la glicoproteÍna P. El clorhidrato de (R)-verapamilo bloquea el transporte mediado por MRP1, lo que da como resultado la quimiosensibilizaciÓn de las células que sobreexpresan MRP1 a los medicamentos contra el cÁncer. (R)-Verapamil hydrochloride  Chemical Structure
  55. GC19541 (rac)-Antineoplaston A10 (rac)-Antineoplaston A10 es el racemato de Antineoplaston A10. Antineoplaston A10 es un inhibidor de Ras potencialmente para el tratamiento de glioma, linfoma, astrocitoma y cÁncer de mama. (rac)-Antineoplaston A10  Chemical Structure
  56. GC69795 (Rac)-BIO8898

    (Rac)-BIO8898 es un inhibidor de la interacción coestimuladora CD40-CD154. (Rac)-BIO8898 inhibe la unión de CD154 a CD40-Ig, con una IC50 de 25 μM.

    (Rac)-BIO8898  Chemical Structure
  57. GC62528 (Rac)-Hesperetin (Rac)-Hesperetin es el racemato de Hesperetin. (Rac)-Hesperetin  Chemical Structure
  58. GC61750 (Rac)-Indoximod (Rac)-indoximod (1-metil-DL-triptÓfano) es un inhibidor de la indolamina 2,3-dioxigenasa (IDO). (Rac)-Indoximod  Chemical Structure
  59. GC10098 (S)-10-Hydroxycamptothecin

    ChEMBL 273862, NSC 107124

    La (S)-10-hidroxicamptotecina (10-HCPT;10-hidroxicamptotecina) es un inhibidor de la topoisomerasa I del ADN aislado de la planta china Camptotheca accuminata. La (S)-10-hidroxicamptotecina muestra un notable efecto inductor de la apoptosis. La (S)-10-hidroxicamptotecina tiene potencial para el tratamiento de hepatoma, carcinoma gÁstrico, cÁncer de colon y leucemia. (S)-10-Hydroxycamptothecin  Chemical Structure
  60. GC41557 (S)-3'-amino Blebbistatin

    (-)-3'-amino Blebbistatin, m-amino Blebbistatin, meta-amino Blebbistatin

    (S)-3'-amino Blebbistatin is a more stable and less phototoxic form of (-)-blebbistatin, which is a selective cell-permeable inhibitor of non-muscle myosin II ATPases. (S)-3'-amino Blebbistatin  Chemical Structure
  61. GC41484 (S)-3'-hydroxy Blebbistatin

    (-)-3'-hydroxy Blebbistatin, meta-hydroxy-Blebbistatin, m-hydroxy-Blebbistatin

    (S)-3'-hydroxy Blebbistatin is a more stable and less phototoxic form of (-)-blebbistatin, which is a selective cell-permeable inhibitor of non-muscle myosin II ATPases. (S)-3'-hydroxy Blebbistatin  Chemical Structure
  62. GC52192 (S)-4'-nitro-Blebbistatin

    (-)-4'-nitro-Blebbistatin, p-nitro-Blebbistatin, para-nitro-Blebbistatin

    (S)-4'-nitro-Blebbistatin es un inhibidor de miosina II no citotÓxico, fotoestable, fluorescente y especÍfico, utilizado en el estudio del papel especÍfico de la miosina II en estudios fisiolÓgicos, de desarrollo y biolÓgicos celulares. (S)-4'-nitro-Blebbistatin  Chemical Structure
  63. GC35001 (S)-Gossypol acetic acid

    (S)-(+)-Gossypol acetic acid

    (S)-Gosipol es el isómero de un producto natural Gosipol. El (S)-gosipol se une al surco de unión a BH3 de las proteínas Bcl-xL y Bcl-2 con gran afinidad. (S)-Gossypol acetic acid  Chemical Structure
  64. GC41739 (S)-nitro-Blebbistatin

    S(-)7Desmethyl8nitro Blebbistatin

    (S)-nitro-Blebbistatin is a more stable form of (-)-blebbistatin, which is a selective cell-permeable inhibitor of non-muscle myosin II ATPases. (S)-nitro-Blebbistatin  Chemical Structure
  65. GC60425 (S)-Verapamil D7 hydrochloride

    (S)-(-)-Verapamil D7 hydrochloride

    El clorhidrato de (S)-Verapamilo D7 ((S)-(-)-clorhidrato de Verapamilo D7) es un clorhidrato de (S)-Verapamilo marcado con deuterio. (S)-clorhidrato de verapamilo (S(-)-clorhidrato de verapamilo) inhibe el transporte de leucotrieno C4 (LTC4) y calceÍna por MRP1. El clorhidrato de (S)-verapamilo conduce a la muerte de células tumorales potencialmente resistentes. (S)-Verapamil D7 hydrochloride  Chemical Structure
  66. GC60008 (S)-Verapamil hydrochloride (S)-clorhidrato de verapamilo (S(-)-clorhidrato de verapamilo) inhibe el transporte de leucotrieno C4 (LTC4) y calceÍna por MRP1. El clorhidrato de (S)-verapamilo conduce a la muerte de células tumorales potencialmente resistentes. (S)-Verapamil hydrochloride  Chemical Structure
  67. GC18787 (±)-Dunnione

    NSC 95403

    (±)-Dunnione is a naturally occurring naphthoquinone with diverse biological activities. (±)-Dunnione  Chemical Structure
  68. GC11965 (±)-Huperzine A

    Hup A, (-)-Selagine

    A neuroprotective AChE inhibitor (±)-Huperzine A  Chemical Structure
  69. GC16375 (±)-Jasmonic Acid methyl ester

    (±)-Methyl Jasmonate

    (±)-El éster metÍlico del Ácido jasmÓnico es un metabolito endÓgeno. (±)-Jasmonic Acid methyl ester  Chemical Structure
  70. GC14154 (±)-Nutlin-3

    Nutlin 3b

    MDM2 antagonist, potent and selective

    (±)-Nutlin-3  Chemical Structure
  71. GC46379 1,2-Dioleoyl-sn-glycero-3-PS (sodium salt)

    1,2-DOPS, 18:1/18:1-PS; PS(18:1/18:1), 1,2-Dioctadecenoyl-sn-glycero-3-Phosphoserine, 1,2-Dioctadecenoyl-sn-glycero-3-Phosphatidylserine

    La 1,2-dioleoil-sn-glicero-3-PS (sal de sodio) es un sustituto de la fosfoserina/fosfatidilserina. 1,2-Dioleoyl-sn-glycero-3-PS (sodium salt)  Chemical Structure
  72. GC19528 1,4-Benzoquinone

    p-Benzoquinone, NSC 36324, p-Quinone

    A toxic metabolite of benzene 1,4-Benzoquinone  Chemical Structure
  73. GC42018 1-O-Octadecyl-2-O-methyl-sn-glycerol

    2Methyl1octadecylsnglycerol, PIA 7

    1-O-Octadecyl-2-O-methyl-sn-glycerol is a metabolite of a phosphotidylinositol ether lipid analog (PIA). 1-O-Octadecyl-2-O-methyl-sn-glycerol  Chemical Structure
  74. GC41865 10'-Desmethoxystreptonigrin 10'-Desmethoxystreptonigrin is an antibiotic originally isolated from Streptomyces and a derivative of the antibiotic streptonigrin. 10'-Desmethoxystreptonigrin  Chemical Structure
  75. GC49736 10-acetyl Docetaxel

    PNU 101383, 10-acetyl Taxotere

    10-acetyl Docetaxel (10-Acetyl docetaxel) es un anÁlogo de Docetaxel, con actividad anticancerÍgena. Docetaxel es un inhibidor del desensamblaje de microtÚbulos, con actividad antimitÓtica. 10-acetyl Docetaxel  Chemical Structure
  76. GC64726 10-Formyl-5,8-dideazafolic acid El Ácido 10-formil-5,8-dideazafÓlico es un inhibidor de la timidilato sintasa. 10-Formyl-5,8-dideazafolic acid  Chemical Structure
  77. GC49872 10-Formyltetrahydrofolate (sodium salt) (technical grade)

    10-CHO-FH4, 10-CHO-THF, N10-Formyltetrahydrofolate, 10-formyl H4PteGlu, 10-fTHF

    El 10-formiltetrahidrofolato (sal de sodio) (grado técnico) es una forma de Ácido tetrahidrofÓlico que actÚa como donante de grupos formilo en el anabolismo. 10-Formyltetrahydrofolate (sodium salt) (technical grade)  Chemical Structure
  78. GC35057 14-Deoxyandrographolide

    14-DAG

    El 14-desoxiandrografÓlido es un diterpeno de labdano con actividad bloqueadora de los canales de calcio. 14-Deoxyandrographolide  Chemical Structure
  79. GC11988 15-acetoxy Scirpenol

    4-Deacetylanguidin,NSC 267030

    El 15-acetoxiscirpenol, una de las micotoxinas de la fracción acetoxiscirpenol (ASM), induce fuertemente la apoptosis e inhibe el crecimiento de las células T Jurkat de manera dependiente de la dosis mediante la activación de otras caspasas independientes de la caspasa-3. 15-acetoxy Scirpenol  Chemical Structure
  80. GC41938 15-Lipoxygenase Inhibitor 1

    15LO Inhibitor 1

    El inhibidor 1 de la 15-lipoxigenasa es un inhibidor selectivo de la 15-lipoxigenasa, con una IC50 de 18 μM. El inhibidor de 15-lipoxigenasa 1 tiene IC50 de 19,5 μM y 19,1 μM para la 15-lipoxigenasa de soja (SLO) y la 15-lipoxigenasa-1 humana (15-LOX-1), respectivamente. El inhibidor de 15-lipoxigenasa 1 tiene potencial para la investigaciÓn del cÁncer de prÓstata. 15-Lipoxygenase Inhibitor 1  Chemical Structure
  81. GC46451 16F16 A PDI inhibitor 16F16  Chemical Structure
  82. GC11720 17-AAG (KOS953)

    BMS 722782, CP 127374, KOS 953, NSC 330507, Tanespimycin

    17-AAG(Geldanamycin), a natural benzoquinone ansamycin antibiotic, is the first established inhibitor of Hsp90. 17-AAG (KOS953)  Chemical Structure
  83. GC13044 17-DMAG (Alvespimycin) HCl 17-DMAG (Alvespimicina) HCl (clorhidrato de 17-DMAG; KOS-1022; BMS 826476) es un potente inhibidor de Hsp90, que se une a Hsp90 con EC50 de 62± 29 nM. 17-DMAG (Alvespimycin) HCl  Chemical Structure
  84. GC41983 19,20-Epoxycytochalasin D La 19,20-epoxicitocalasina D, una citocalasina, es un metabolito fÚngico de Nemania sp. 19,20-Epoxycytochalasin D  Chemical Structure
  85. GC48423 19-O-Acetylchaetoglobosin A

    Chaetoglobosin A Acetate

    La 19-O-acetilquetoglobosina A, un alcaloide del citocalasano, es un metabolito fÚngico aislado originalmente de C. globosum que tiene actividades inhibidoras de la polimerizaciÓn de actina y citotÓxicas. La 19-O-acetilquetoglobosina A es citotÓxica para las células de cÁncer de cuello uterino HeLa. 19-O-Acetylchaetoglobosin A  Chemical Structure
  86. GC39296 1G244 1G244 es un potente inhibidor de DPP8/9 con IC50 de 12 nM y 84 nM, respectivamente. 1G244 no inhibe DPPIV y DPPII. 1G244 induce la apoptosis en células de mieloma mÚltiple y tiene efectos antimieloma. 1G244  Chemical Structure
  87. GC46508 2',2'-Difluoro-2'-deoxyuridine

    dFdU

    An active metabolite of gemcitabine 2',2'-Difluoro-2'-deoxyuridine  Chemical Structure
  88. GC41612 2'-O-Methylguanosine La 2'-O-metilguanosina es un nucleÓsido modificado producido en los ARNt por la acciÓn de la guanosina-2'-O-metiltransferasa del ARNt. 2'-O-Methylguanosine  Chemical Structure
  89. GC12258 2,3-DCPE hydrochloride 2,3-DCPE hydrochloride  Chemical Structure
  90. GC40947 2,3-Dimethoxy-5-methyl-p-benzoquinone

    Coenzyme Q0, CoQ0

    La 2,3-dimetoxi-5-metil-p-benzoquinona (CoQ0) es un compuesto de ubiquinona activo oral potente que puede derivarse de Antrodia cinnamomea. 2,3-Dimethoxy-5-methyl-p-benzoquinone  Chemical Structure
  91. GC68452 2,4,6-Triiodophenol 2,4,6-Triiodophenol  Chemical Structure
  92. GC46057 2,5-Dihydroxycinnamic Acid phenethyl ester An inhibitor of 5-LO 2,5-Dihydroxycinnamic Acid phenethyl ester  Chemical Structure
  93. GC45324 2,5-dimethyl Celecoxib

    DMC

      2,5-dimethyl Celecoxib  Chemical Structure
  94. GN10065 2-Atractylenolide

    2-Atractylenolide

    2-Atractylenolide  Chemical Structure
  95. GC40675 2-deoxy-Artemisinin 2-deoxy-Artemisinin is an inactive metabolite of the antimalarial agent artemisinin. 2-deoxy-Artemisinin  Chemical Structure
  96. GC17430 2-Deoxy-D-glucose

    2-DG

    2-Deoxy-D-glucose (2DG), un análogo de la glucosa, actúa como un inhibidor competitivo de la glucólisis. 2-Deoxy-D-glucose  Chemical Structure
  97. GC49223 2-deoxy-D-Glucose-13C6

    2-DG-13C6

    An internal standard for the quantification of 2-deoxy-D-glucose 2-deoxy-D-Glucose-13C6  Chemical Structure
  98. GC46545 2-Fluoroadenine

    F-Ade, NSC 27364

    La 2-fluoroadenina es una base de purina tÓxica. La 2-fluoroadenina tiene toxicidad en células tumorales proliferantes y no proliferantes. La 2-fluoroadenina se puede utilizar para investigar el cÁncer. 2-Fluoroadenine  Chemical Structure
  99. GC12545 2-HBA

    Bis(2-hydroxybenzylidene)acetone

    2-HBA es un potente inductor de NAD(P)H: oxidorreductasa 1 del aceptor de quinona (NQO1) que también puede activar la caspasa-3 y la caspasa-10. 2-HBA  Chemical Structure
  100. GC38318 2-Methoxycinnamaldehyde El 2-MetoxicinamaldehÍdo (o-MetoxicinamaldehÍdo) es un compuesto natural de Cinnamomum cassia, con actividad antitumoral. El 2-metoxicinamaldehÍdo inhibe la proliferaciÓn e induce la apoptosis por pérdida del potencial de membrana mitocondrial (δψm), activaciÓn de caspasa-3 y caspasa-9. El 2-metoxicinamaldehÍdo inhibe eficazmente la migraciÓn de HASMC inducida por el factor de crecimiento derivado de plaquetas (PDGF). 2-Methoxycinnamaldehyde  Chemical Structure
  101. GC15084 2-Methoxyestradiol (2-MeOE2)

    2Hydroxyestradiol 2methyl ether, 2ME2, NSC 659853, Panzem

    2-Methoxyestradiol (2-MeOE2/2-Me) is an HIF-1α inhibitor. 2-Methoxyestradiol (2-MeOE2)  Chemical Structure

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