Apoptosis
Read More about this categoryShow Less
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.
Research Areas
- Caspase(144)
- Pyroptosis(42)
- 14.3.3 Proteins(1)
- Apoptosis Inducers(42)
- Bax(6)
- Bcl-2 Family(188)
- Bcl-xL(8)
- c-RET(8)
- IAP(33)
- KEAP1-Nrf2(90)
- MDM2(12)
- p53(153)
- PC-PLC(4)
- PKD(7)
- RasGAP (Ras- P21)(1)
- Survivin(13)
- Thymidylate Synthase(12)
- TNF-α(262)
- Other Apoptosis(877)
- APC(6)
- PD-1/PD-L1 interaction(132)
- ASK1(4)
- PAR4(2)
- RIP kinase(57)
- FKBP(25)
- Cuproptosis(4)
Products Related to Apoptosis(3381)
- GC70114Venetoclax-d8CAS: 1257051-06-1Purity: >99.50%
Venetoclax-d8 es un isotopo deuterado de Venetoclax. Venetoclax (ABT-199; GDC-0199) es un inhibidor selectivo y altamente efectivo de Bcl-2, que se administra por vía oral con una Ki menor a 0.01 nM. Venetoclax puede inducir la autófagia.
- GC70137VudalimabCAS: 2329669-72-7Purity: >99.00%
Vudalimab es un inhibidor dual efectivo de PD-1 y CTLA-4, que es un anticuerpo monoclonal biespecífico completamente humanizado. Vudalimab se dirige a los receptores de puntos de control inmunológicos PD-1 y CTLA-4, lo que promueve la activación selectiva de las células T contra el tumor.
- GC70257Gallium maltolateCAS: 108560-70-9Purity: >98.00%
Gallium maltolate (GAM) es un inductor de la apoptosis con actividad anti-cáncer y anti-inflamatoria.
- GC70289AC-VEID-CHO TFAPurity: >98.00%
AC-VEID-CHO TFA es un inhibidor de la caspasa derivado de un péptido y tiene una potencia de inhibide la caspasa-6, caspasa-3 y caspasa-7 con valores de IC50 de 16,2 nM, 13,6 nM y 162,1 nM, respectivamente.
- GC70298Peginterferon beta-1aCAS: 1211327-92-2
Peginterferon β-1a es la primera molécula pegilada de interferón beta-1a.
- GC70332(+)-Erinacin ACAS: 156101-08-5Purity: >99.00%
(+)-Erinacin A es un compuesto contra el cáncer que se puede aislar del hongo Hericium erinaceum.
- GC70388Justicidin BCAS: 17951-19-8Purity: >99.00%
Justicidin B es un potente Lignano contra el cáncer y agente proapoptótico.
- GC70411Nrf2-Activator-12GCAS: 1554271-18-9Purity: >99.00%
Nrf2-Activator-12G (compd 12g) es un activador de Nrf2.
- GC70584Actinomycin X2CAS: 18865-48-0Purity: >98.00%
Actinomycin X2 (actinomicina V), producido por muchos Streptomyces sp.
- GC70658C5 LenalidomideCAS: 191732-70-4
C5 Lenalidomide (lenalidomi5 '-amina) es un análogo de la talidomiy es un potente inhibide la producción de TNF-alfa (IC50=100 μM en LPS estimulpbmc humana).
- GC706599-cis-Retinoic acid-d5Purity: >98.00%
9-cis-Retinoic acid-d5 es el deuterio etiquetado como ácido 9-cis-retinoico.
- GC70733ABT-510 acetateCAS: 442526-87-6Purity: >99.00%
ABT-510 acetate es un péptido antiangitsp (análogo de la tromboespondina 1) que induce apoptosis e inhiel crecimiento de tumores ovárien un modelo ortotópico y singénico de cáncer de ovariepiteli.
- GC70756Cytarabine-d2CAS: 40632-26-6Purity: >98.00%
Cytarabine-d2 es el deuterio etiquetado citarabina.
- GC70853Broussochalcone ACAS: 99217-68-2Purity: >97.00%
Broussochalcone A es un antioxidante y un inhibidor de la xantina oxid(IC50=2.21 μM), con actividad de eliminación de radicales libres.
- GC70868Nrf2 activator-3CAS: 2766570-23-2Purity: >98.00%
Nrf2 activator-3 es un potente activador Nrf2.
- GC70875RIPK1-IN-9CAS: 2682889-57-0
RIPK1-IN-9 (ejemplo 45), un compuesto de dihidronaftiridona, es un potente y selectivo inhibide RIPK1.
| Catalog No. | Product Name | CAS No. | Purity | Structure |
|---|---|---|---|---|
| GC70114 | Venetoclax-d8 | 1257051-06-1 | >99.50% | |
Venetoclax-d8 es un isotopo deuterado de Venetoclax. Venetoclax (ABT-199; GDC-0199) es un inhibidor selectivo y altamente efectivo de Bcl-2, que se administra por vía oral con una Ki menor a 0.01 nM. Venetoclax puede inducir la autófagia. | ||||
| GC70137 | Vudalimab | 2329669-72-7 | >99.00% | |
Vudalimab es un inhibidor dual efectivo de PD-1 y CTLA-4, que es un anticuerpo monoclonal biespecífico completamente humanizado. Vudalimab se dirige a los receptores de puntos de control inmunológicos PD-1 y CTLA-4, lo que promueve la activación selectiva de las células T contra el tumor. | ||||
| GC70145 | WL12 | - | >98.00% | |
WL12 is a specific targeting programmatic death ligand 1 (PD-L1) binding peptide. WL12 can be radiolabeled with different radioactive isotopes to produce a radiotracer for evaluating the expression of tumor PD-L1. | ||||
| GC70242 | Thymocartin TFA | - | - | |
Thymocartin TFA es la forma de sal TFA de la timocartina. | ||||
| GC70257 | Gallium maltolate | 108560-70-9 | >98.00% | |
Gallium maltolate (GAM) es un inductor de la apoptosis con actividad anti-cáncer y anti-inflamatoria. | ||||
| GC70289 | AC-VEID-CHO TFA | - | >98.00% | |
AC-VEID-CHO TFA es un inhibidor de la caspasa derivado de un péptido y tiene una potencia de inhibide la caspasa-6, caspasa-3 y caspasa-7 con valores de IC50 de 16,2 nM, 13,6 nM y 162,1 nM, respectivamente. | ||||
| GC70298 | Peginterferon beta-1a | 1211327-92-2 | - | |
Peginterferon β-1a es la primera molécula pegilada de interferón beta-1a. | ||||
| GC70332 | (+)-Erinacin A | 156101-08-5 | >99.00% | |
(+)-Erinacin A es un compuesto contra el cáncer que se puede aislar del hongo Hericium erinaceum. | ||||
| GC70388 | Justicidin B | 17951-19-8 | >99.00% | |
Justicidin B es un potente Lignano contra el cáncer y agente proapoptótico. | ||||
| GC70411 | Nrf2-Activator-12G | 1554271-18-9 | >99.00% | |
Nrf2-Activator-12G (compd 12g) es un activador de Nrf2. | ||||
| GC70418 | Cipepofol | 1637741-58-2 | >98.00% | |
Cipepofol (Ciprofol), un nuevo derivado del 2,6-disustituido fenol, es un modulador alostérico positivo y agonista directo del receptor GABAA. | ||||
| GC70520 | MIND4-17 | 345989-24-4 | >99.00% | |
MIND4-17 es un potente activador NRF2 que modifica covalentemente un residuo C151 de Keap1. | ||||
| GC70570 | RH01386 | 301177-36-6 | >99.00% | |
RH01386 es una molécula pequeña que puede prevenir la disfunción y muerte celular indupor estrés del retículo endoplásmico (ERS), e inhila la expresión génica proapoptótica. | ||||
| GC70584 | Actinomycin X2 | 18865-48-0 | >98.00% | |
Actinomycin X2 (actinomicina V), producido por muchos Streptomyces sp. | ||||
| GC70658 | C5 Lenalidomide | 191732-70-4 | - | |
C5 Lenalidomide (lenalidomi5 '-amina) es un análogo de la talidomiy es un potente inhibide la producción de TNF-alfa (IC50=100 μM en LPS estimulpbmc humana). | ||||
| GC70659 | 9-cis-Retinoic acid-d5 | - | >98.00% | |
9-cis-Retinoic acid-d5 es el deuterio etiquetado como ácido 9-cis-retinoico. | ||||
| GC70733 | ABT-510 acetate | 442526-87-6 | >99.00% | |
ABT-510 acetate es un péptido antiangitsp (análogo de la tromboespondina 1) que induce apoptosis e inhiel crecimiento de tumores ovárien un modelo ortotópico y singénico de cáncer de ovariepiteli. | ||||
| GC70742 | Betamethasone-d5-1 | 2244574-92-1 | - | |
βmethasone-d5-1 es deuterio etiquetado betametasona. | ||||
| GC70753 | PDK4-IN-1 | 2310262-10-1 | >98.00% | |
PDK4-IN-1 es un derivado de la antraquinona y un potente inhibide la piruvato deshidrogenasa quinasa 4 (PDK4) con un valor de IC50 de 84 nM. | ||||
| GC70756 | Cytarabine-d2 | 40632-26-6 | >98.00% | |
Cytarabine-d2 es el deuterio etiquetado citarabina. | ||||
| GC70759 | AQX-435 | 1619983-52-6 | >99.00% | |
AQX-435 es un potente activador de la fosfatasa SHIP1. | ||||
| GC70853 | Broussochalcone A | 99217-68-2 | >97.00% | |
Broussochalcone A es un antioxidante y un inhibidor de la xantina oxid(IC50=2.21 μM), con actividad de eliminación de radicales libres. | ||||
| GC70868 | Nrf2 activator-3 | 2766570-23-2 | >98.00% | |
Nrf2 activator-3 es un potente activador Nrf2. | ||||
| GC70875 | RIPK1-IN-9 | 2682889-57-0 | - | |
RIPK1-IN-9 (ejemplo 45), un compuesto de dihidronaftiridona, es un potente y selectivo inhibide RIPK1. | ||||
