Home >> Signaling Pathways >> Apoptosis

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. Product Name Information
  2. GC10350 TIC10 isomer

    ONC201 isomer

    Potent Akt/ERK inhibitor

     TIC10 isomer  Chemical Structure
  3. GC41183 α-Carotene

    all-trans-α-Carotene

    α-Carotene is a precursor of vitamin A that has been found in various fruits and vegetables.

    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, an endogenous neuropeptide, is an endogenous melanocortin receptor 4 (MC4R) agonist with anti-inflammatory and antipyretic activities. α-MSH (human, mouse, rat, porcine, bovine, ovine) (trifluoroacetate salt)  Chemical Structure
  5. GC45213 α-NETA Choline acetyltransferase (ChAT) mediates the synthesis of the neurotransmitter acetylcholine from acetyl-CoA and choline. 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-solanine, a bioactive component and one of the major steroidal glycoalkaloids in potatoes, has been observed to inhibit growth and induce apoptosis in cancer cells. α-Solanine  Chemical Structure
  8. GC67618 α-Tocopherol phosphate disodium

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

    α-Tocopherol phosphate (alpha-Tocopherol phosphate) disodium, a promising antioxidant, can protect against long-wave UVA1 induced cell death and scavenge UVA1 induced ROS in a skin cell model. α-Tocopherol phosphate disodium possesses therapeutic potential in the inhibition of apoptosis and increases the migratory capacity of endothelial progenitor cells under high-glucose/hypoxic conditions and promotes angiogenesis. 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-Elemonic acid is a triterpene isolated from Boswellia (Burseraceae) that exhibits anticancer activity. β-Elemonic Acid  Chemical Structure
  11. GC64619 β-Ionone β-Ionone is effective in the induction of apoptosis in gastric adenocarcinoma SGC7901 cells. Anti-cancer activity. β-Ionone  Chemical Structure
  12. GC66048 δ-Secretase inhibitor 11 δ-Secretase inhibitor 11 (compound 11) is an orally active, potent, BBB-penetrated, non-toxic, selective and specific δ-secretase inhibitor, with an IC50 of 0.7 μM. δ-Secretase inhibitor 11 interacts with both the active site and allosteric site of δ-secretase. δ-Secretase inhibitor 11 attenuates tau and APP (amyloid precursor protein) cleavage. δ-Secretase inhibitor 11 ameliorates synaptic dysfunction and cognitive impairments in tau P301S and 5XFAD transgenic mouse models. δ-Secretase inhibitor 11 can be used for Alzheimer's disease research. δ-Secretase inhibitor 11  Chemical Structure
  13. GC46008 (±)-Thalidomide-d4

    N-Phthaloylglutamimide-d4

    An internal standard for the quantification of (±)-thalidomide (±)-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 is a metabolite originally isolated from the marine sponge V. (+)-Aeroplysinin-1  Chemical Structure
  18. GC17008 (+)-Apogossypol inhibitor of Bcl-2 family proteins (+)-Apogossypol  Chemical Structure
  19. GC45256 (+)-ar-Turmerone

    (S)(+)arTurmerone

    (+)-ar-Turmerone is an aromatic compound from the rhizomes of C. (+)-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 is an activator of antioxidant transcription factor 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  Chemical Structure
  24. GC18749 (+)-Rugulosin

    NSC 160880, NSC 249990, Rugulosin A

    (+)-Rugulosin is a pigment and mycotoxin produced by certain fungi. (+)-Rugulosin  Chemical Structure
  25. GC41345 (-)-α-Bisabolol

    DL-α-Bisabolol

    (-)-α-Bisabolol ((-)-α-Bisabolol), a monocyclic sesquiterpene alcohol, exerts antioxidant, anti-inflammatory, and anti-apoptotic activities. (-)-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) A potent central nervous system stimulant for induction of seizures (-)-(α)-Kainic Acid (hydrate)  Chemical Structure
  28. GC45246 (-)-Chaetominine

    (-)-Chaetominine

    (-)-Chaetominine is a cytotoxic alkaloid originally isolated from Chaetomium sp. (-)-Chaetominine  Chemical Structure
  29. GC40698 (-)-Perillyl Alcohol

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

    (-)-Perillyl Alcohol is a monoterpene found in lavender, inhibits farnesylation of Ras, upregulates the mannose-6-phosphate receptor and induces apoptosis. Anti-cancer activity. (-)-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 is an enantiomer of Bortezomib. Bortezomib is a cell-permeable, reversible, and selective proteasome inhibitor, and potently inhibits 20S proteasome (Ki of 0.6 nM) by targeting a threonine residue. Bortezomib disrupts the cell cycle, induces apoptosis, and inhibits NF-κB. Bortezomib is an anti-cancer agent and the first therapeutic proteasome inhibitor to be used in humans. (1S,2S)-Bortezomib  Chemical Structure
  32. GC34965 (20S)-Protopanaxatriol

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

    An active ginsenoside metabolite (20S)-Protopanaxatriol  Chemical Structure
  33. GC60397 (5Z,2E)-CU-3 (5Z,2E)-CU-3 is a potent and selective inhibitor against the α-isozyme of DGK with an IC50 value of 0.6 μM, competitively inhibits the affinity of DGKα for ATP with a Km value of 0.48 mM. (5Z,2E)-CU-3 targets the catalytic region, but not the regulatory region of DGKα. (5Z,2E)-CU-3 has antitumoral and proimmunogenic effects, enhances the apoptosis of cancer cells and the activation of T cells. (5Z,2E)-CU-3  Chemical Structure
  34. GC60398 (6R)-FR054 (6R)-FR054 is a less active isomer of 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 is an anti-hydrolysis D-peptide antagonist. It is an effective PD-1/PD-L1 inhibitor with an affinity of 0.51 μM for binding to PD-1, and it works both in vitro and 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 (E)-Ferulic acid is a isomer of Ferulic acid which is an aromatic compound, abundant in plant cell walls. (E)-Ferulic acid causes the phosphorylation of β-catenin, resulting in proteasomal degradation of β-catenin and increases the expression of pro-apoptotic factor Bax and decreases the expression of pro-survival factor survivin. (E)-Ferulic acid shows a potent ability to remove reactive oxygen species (ROS) and inhibits lipid peroxidation. (E)-Ferulic acid exerts both anti-proliferation and anti-migration effects in the human lung cancer cell line H1299. (E)-Ferulic acid  Chemical Structure
  42. GC34981 (E)-Flavokawain A

    Flavokavain A, 4-methoxy Flavokawain B

    (E)-Flavokawain A, a chalcone extracted from Kava, has anticarcinogenic effect. (E)-Flavokawain A induces apoptosis in bladder cancer cells by involvement of bax protein-dependent and mitochondria-dependent apoptotic pathway and suppresses tumor growth in mice. (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)-Methyl 4-coumarate (Methyl 4-hydroxycinnamate), found in several plants, such as green onion (Allium cepa) or noni (Morinda citrifolia L. (E)-Methyl 4-coumarate  Chemical Structure
  44. GC34125 (E)-[6]-Dehydroparadol (E)-[6]-Dehydroparadol, an oxidative metabolite of [6]-Shogaol, is a potent Nrf2 activator. (E)-[6]-Dehydroparadol can inhibit the growth and induce the apoptosis of human cancer cells. (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

    Etomoxir((R)-(+)-Etomoxir) sodium salt is an irreversible inhibitor of carnitine palmitoyltransferase 1a (CPT-1a), inhibits fatty acid oxidation (FAO) through CPT-1a and inhibits palmitate β-oxidation in human, rat and guinea pig. (R)-(+)-Etomoxir sodium salt  Chemical Structure
  48. GC34096 (R)-(-)-Gossypol acetic acid (AT-101 (acetic acid)) (R)-(-)-Gossypol acetic acid (AT-101 (acetic acid)) (AT-101 (acetic acid)) is the levorotatory isomer of a natural product Gossypol. AT-101 is determined to bind to Bcl-2, Mcl-1 and Bcl-xL proteins with Kis of 260±30 nM, 170±10 nM, and 480±40 nM, respectively. (R)-(-)-Gossypol acetic acid (AT-101 (acetic acid))  Chemical Structure
  49. GC65610 (R)-5-Hydroxy-1,7-diphenyl-3-heptanone (R)-5-Hydroxy-1,7-diphenyl-3-heptanone is a diarylheptanoid that can be found in Alpinia officinarum. (R)-5-Hydroxy-1,7-diphenyl-3-heptanone  Chemical Structure
  50. GC41716 (R)-CR8 Cyclin-dependent kinases (CDKs) are key regulators of cell cycle progression and are therefore promising targets for cancer therapy. (R)-CR8  Chemical Structure
  51. GC39281 (R)-CR8 trihydrochloride

    CR8, (R)-Isomer trihydrochloride

    (R)-CR8 (CR8) trihydrochloride, a second-generation analog of Roscovitine, is a potent CDK1/2/5/7/9 inhibitor. (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

    (R)-Verapamil D7 hydrochloride ((R)-(+)-Verapamil D7 hydrochloride) is a deuterium labeled (R)-Verapamil hydrochloride. (R)-Verapamil hydrochloride ((R)-(+)-Verapamil hydrochloride) is a P-Glycoprotein inhibitor. (R)-Verapamil hydrochloride blocks MRP1 mediated transport, resulting in chemosensitization of MRP1-overexpressing cells to anticancer drugs. (R)-Verapamil D7 hydrochloride  Chemical Structure
  54. GC60408 (R)-Verapamil hydrochloride (R)-Verapamil hydrochloride ((R)-(+)-Verapamil hydrochloride) is a P-Glycoprotein inhibitor. (R)-Verapamil hydrochloride blocks MRP1 mediated transport, resulting in chemosensitization of MRP1-overexpressing cells to anticancer drugs. (R)-Verapamil hydrochloride  Chemical Structure
  55. GC19541 (rac)-Antineoplaston A10

    (rac)-Antineoplaston A10 is the racemate of Antineoplaston A10

    (rac)-Antineoplaston A10  Chemical Structure
  56. GC69795 (Rac)-BIO8898

    (Rac)-BIO8898 is a CD40-CD154 co-stimulatory interaction inhibitor. (Rac)-BIO8898 inhibits the binding of CD154 to CD40-Ig, with an IC50 of 25 μM.

    (Rac)-BIO8898  Chemical Structure
  57. GC62528 (Rac)-Hesperetin (Rac)-Hesperetin is the racemate of Hesperetin. (Rac)-Hesperetin  Chemical Structure
  58. GC61750 (Rac)-Indoximod (Rac)-Indoximod (1-Methyl-DL-tryptophan) is an indoleamine 2,3-dioxygenase (IDO) inhibitor. (Rac)-Indoximod  Chemical Structure
  59. GC10098 (S)-10-Hydroxycamptothecin

    ChEMBL 273862, NSC 107124

    inhibitor of topoisomerase I (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 is a non-cytotoxic, photostable, fluorescent and specific Myosin II inhibitor, usd in the study of the specific role of myosin II in physiological, developmental, and cell biological studies. (S)-4'-nitro-Blebbistatin  Chemical Structure
  63. GC35001 (S)-Gossypol acetic acid

    (S)-(+)-Gossypol acetic acid

    (S)-Gossypol is the isomer of a natural product Gossypol. (S)-Gossypol binds to the BH3-binding groove of Bcl-xL and Bcl-2 proteins with high affinity. (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

    (S)-Verapamil D7 hydrochloride ((S)-(-)-Verapamil D7 hydrochloride) is a deuterium labeled (S)-Verapamil hydrochloride. (S)-Verapamil hydrochloride (S(-)-Verapamil hydrochloride) inhibits leukotriene C4 (LTC4) and calcein transport by MRP1. (S)-Verapamil hydrochloride leads to the death of potentially resistant tumor cells. (S)-Verapamil D7 hydrochloride  Chemical Structure
  66. GC60008 (S)-Verapamil hydrochloride (S)-Verapamil hydrochloride (S(-)-Verapamil hydrochloride) inhibits leukotriene C4 (LTC4) and calcein transport by MRP1. (S)-Verapamil hydrochloride leads to the death of potentially resistant tumor cells. (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

    (±)-Jasmonic Acid methyl ester is an endogenous metabolite. (±)-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

    1,2-Dioleoyl-sn-glycero-3-PS (sodium salt) is a ubstitute for Phosphoserine/phosphatidylserine. 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) is an analog of Docetaxel, with anticancer activity. Docetaxel is a microtubule disassembly inhibitor, with antimitotic activity. 10-acetyl Docetaxel  Chemical Structure
  76. GC64726 10-Formyl-5,8-dideazafolic acid 10-Formyl-5,8-dideazafolic acid is a thymidylate synthase inhibitor. 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

    10-Formyltetrahydrofolate (sodium salt) (technical grade) is a form of tetrahydrofolic acid that acts as a donor of formyl groups in anabolism. 10-Formyltetrahydrofolate (sodium salt) (technical grade)  Chemical Structure
  78. GC35057 14-Deoxyandrographolide

    14-DAG

    A diterpene lactone with diverse biological properties 14-Deoxyandrographolide  Chemical Structure
  79. GC11988 15-acetoxy Scirpenol

    4-Deacetylanguidin,NSC 267030

    mycotoxin that induce apoptotic cell death 15-acetoxy Scirpenol  Chemical Structure
  80. GC41938 15-Lipoxygenase Inhibitor 1

    15LO Inhibitor 1

    15-Lipoxygenase Inhibitor 1 is a selective inhibitor of 15-lipoxygenase, with an IC50 of 18 μM. 15-Lipoxygenase Inhibitor 1 has IC50s of 19.5 μM and 19.1 μM for soybean 15-lipoxygenase (SLO) and human 15-lipoxygenase-1 (15-LOX-1), respectively. 15-Lipoxygenase Inhibitor 1 has potential for the research of prostate cancer. 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 (Alvespimycin) HCl (17-DMAG hydrochloride; KOS-1022; BMS 826476) is a potent inhibitor of Hsp90, binding to Hsp90 with EC50 of 62±29 nM. 17-DMAG (Alvespimycin) HCl  Chemical Structure
  84. GC41983 19,20-Epoxycytochalasin D

    19,20-Epoxycytochalasin D is a fungal metabolite that has been found in the endophytic fungus Nemania sp.

    19,20-Epoxycytochalasin D  Chemical Structure
  85. GC48423 19-O-Acetylchaetoglobosin A

    Chaetoglobosin A Acetate

    A fungal metabolite with actin polymerization inhibitory and cytotoxic activities 19-O-Acetylchaetoglobosin A  Chemical Structure
  86. GC39296 1G244 1G244 is a potent DPP8/9 inhibitor with IC50s of 12 nM and 84 nM, respectively. 1G244 does not inhibit DPPIV and DPPII. 1G244 induces apoptosis in multiple myeloma cells and has anti-myeloma effects. 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 2'-O-Methylguanosine is a modified nucleoside that is produced in tRNAs by the action of tRNA guanosine-2'-O-methyltransferase, using S-adenosyl-L-methionine as a substrate. 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

    2,3-Dimethoxy-5-methyl-p-benzoquinone (CoQ0) is a potent, oral active ubiquinone compound can be derived from 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), is a glucose analogue, act as competitive glycolytic inhibitor. 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

    A heterocyclic building block 2-Fluoroadenine  Chemical Structure
  99. GC12545 2-HBA

    Bis(2-hydroxybenzylidene)acetone

    indirect inducer of enzymes that catalyze detoxification reactions through the Keap1-Nrf2-ARE pathway. 2-HBA  Chemical Structure
  100. GC38318 2-Methoxycinnamaldehyde 2-Methoxycinnamaldehyde (o-Methoxycinnamaldehyde) is a natural compound of Cinnamomum cassia, with antitumor activity. 2-Methoxycinnamaldehyde inhibits proliferation and induces apoptosis by mitochondrial membrane potential (ΔΨm) loss, activation of both caspase-3 and caspase-9. 2-Methoxycinnamaldehyde effectively inhibits platelet-derived growth factor (PDGF)-induced HASMC migration. 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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