Apoptosis
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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(126)
- Pyroptosis(38)
- 14.3.3 Proteins(1)
- Apoptosis Inducers(42)
- Bax(6)
- Bcl-2 Family(170)
- Bcl-xL(8)
- c-RET(8)
- IAP(32)
- KEAP1-Nrf2(83)
- MDM2(12)
- p53(147)
- PC-PLC(4)
- PKD(6)
- RasGAP (Ras- P21)(1)
- Survivin(12)
- Thymidylate Synthase(10)
- TNF-α(220)
- Other Apoptosis(877)
- APC(6)
- PD-1/PD-L1 interaction(118)
- ASK1(4)
- PAR4(2)
- RIP kinase(55)
- FKBP(24)
- Cuproptosis(4)
Products Related to Apoptosis(3157)
- GC79231RMC-4998 TFAPurity: >99.00%
RMC-4998 TFA is an orally active inhibitor targeting the active or GTP-bound state of the KRAS G12C mutant.
- GC79277SolaprubartCAS: 3057433-10-7Purity: >99.50%
Solaprubart (STAR-0310) is a fully human IgG1 subtype monoclonal antibody targeting OX40 (CD134/TNFRSF4), with a K d of 7.2 nM.
- GC79278VedastotugCAS: 2878367-20-3Purity: >99.50%
Vedastotug is a human monoclonal antibody targeting TNFRSF4/OX40/CD134, with its corresponding isotype control being Human IgG1 kappa, Isotype Control [1] .
- GC79326Tirzepatide sodiumPurity: >98.00%
Tirzepatide sodium (LY3298176 sodium) is a dual glucose-dependent insulinotropic polypeptide ( GIP ) and glucagon-like peptide-1 ( GLP-1 ) receptor agonist.
- GC79330Pseudoginsenoside RT4CAS: 98474-77-2Purity: >97.00%
Pseudoginsenoside RT4 is an orally active anti-inflammatory agent.
- GC79336TLR9 antagonist 1 diformatePurity: >98.00%
TLR9 antagonist 1 diformate is a selective hTLR9 antagonist with an IC 50 of 0.1 nM against hTLR9.
- GC79338PL120131 acetatePurity: >99.50%
PL120131 acetate is a PD-1 antagonist, can specifically blocking the interaction between PD-1 and PD-L1, thereby effectively inhibiting the PD-1-mediated apoptosis signaling pathway.
- GC79339Anti-CD160 Antibody (MAT 302)Purity: >97.00%
Anti-CD160 Antibody (MAT 302) (CL1-R2) is a human monoclonal antibody targeting CD160.
- GC79340Anti-Mouse TREM2 Antibody (178)Purity: >98.50%
Anti-Mouse TREM2 Antibody (178) is an antibody targeting mouse TREM2, which blocks the binding of ligands to TREM2 and inhibits TREM2 -mediated signaling pathways.
- GC79370PD-L1/HDAC6-IN-1 TFAPurity: >99.50%
PD-L1/HDAC6-IN-1 TFA is an orally active dual inhibitor of PD-L1 and HDAC6, with IC 50 values of 26.8 nM and 78 nM, respectively.
- GC79372Rosnilimab (Mouse IgG2a)Purity: >98.00%
Rosnilimab (Mouse IgG2a ) is a mouse-derived IgG2a antibody, Rosnilimab.
- GC79374PD-1/PD-L1-IN-63CAS: 2691796-92-4Purity: >98.00%
PD-1/PD-L1-IN-63 is an orally active PD-1/PD-L1 inhibitor with an IC 50 of 9.1 nM.
- GC79379Anti-Mouse IFN Beta Antibody (MIB-5E9.1)Purity: >96.00%
Anti-Mouse IFN Beta Antibody (MIB-5E9.1) is an antibody targeting mouse IFN-β. Anti-Mouse IFN Beta Antibody (MIB-5E9.1) blocks the IFN-β signaling pathway, abolishes LPS-induced upregulation of B7H1 and GITRL in dendritic cells, restores dendritic cell-dependent T cell proliferation impaired by LPS exposure, and reverses LPS-induced upregulation of PD-1 on splenic T cells.
- GC79417Biotin-itaconateCAS: 3086566-93-7Purity: >93.00%
Biotin-itaconate is a biotin-labeled itaconic anhydride that targets PD-L1.
- GC79465STAT3-IN-52 hydrochloridePurity: >96.00%
STAT3-IN-52 hydrochloride is an orally active STAT3 inhibitor with a K i value of 2.42 μM.
| Catalog No. | Product Name | CAS No. | Purity | Structure |
|---|---|---|---|---|
| GC79230 | BBO-11818 | 3029443-36-2 | >99.50% | |
BBO-11818 is an orally active, highly selective (relative to NRAS and HRAS ), non-covalent pan- KRAS inhibitor ( IC 50 =28-120 nM). | ||||
| GC79231 | RMC-4998 TFA | - | >99.00% | |
RMC-4998 TFA is an orally active inhibitor targeting the active or GTP-bound state of the KRAS G12C mutant. | ||||
| GC79277 | Solaprubart | 3057433-10-7 | >99.50% | |
Solaprubart (STAR-0310) is a fully human IgG1 subtype monoclonal antibody targeting OX40 (CD134/TNFRSF4), with a K d of 7.2 nM. | ||||
| GC79278 | Vedastotug | 2878367-20-3 | >99.50% | |
Vedastotug is a human monoclonal antibody targeting TNFRSF4/OX40/CD134, with its corresponding isotype control being Human IgG1 kappa, Isotype Control [1] . | ||||
| GC79326 | Tirzepatide sodium | - | >98.00% | |
Tirzepatide sodium (LY3298176 sodium) is a dual glucose-dependent insulinotropic polypeptide ( GIP ) and glucagon-like peptide-1 ( GLP-1 ) receptor agonist. | ||||
| GC79330 | Pseudoginsenoside RT4 | 98474-77-2 | >97.00% | |
Pseudoginsenoside RT4 is an orally active anti-inflammatory agent. | ||||
| GC79335 | LC-PDA-01 | - | >98% | |
LC-PDA-01 is a selective peroxiredoxin 1 (PRDX1) activator with an EC 50 of 111.8 nM and a human K D of 123.2 nM. | ||||
| GC79336 | TLR9 antagonist 1 diformate | - | >98.00% | |
TLR9 antagonist 1 diformate is a selective hTLR9 antagonist with an IC 50 of 0.1 nM against hTLR9. | ||||
| GC79337 | ZSTK3744 | - | >98.00% | |
ZSTK3744 is an aryl hydrocarbon receptor ( AhR ) agonist. | ||||
| GC79338 | PL120131 acetate | - | >99.50% | |
PL120131 acetate is a PD-1 antagonist, can specifically blocking the interaction between PD-1 and PD-L1, thereby effectively inhibiting the PD-1-mediated apoptosis signaling pathway. | ||||
| GC79339 | Anti-CD160 Antibody (MAT 302) | - | >97.00% | |
Anti-CD160 Antibody (MAT 302) (CL1-R2) is a human monoclonal antibody targeting CD160. | ||||
| GC79340 | Anti-Mouse TREM2 Antibody (178) | - | >98.50% | |
Anti-Mouse TREM2 Antibody (178) is an antibody targeting mouse TREM2, which blocks the binding of ligands to TREM2 and inhibits TREM2 -mediated signaling pathways. | ||||
| GC79370 | PD-L1/HDAC6-IN-1 TFA | - | >99.50% | |
PD-L1/HDAC6-IN-1 TFA is an orally active dual inhibitor of PD-L1 and HDAC6, with IC 50 values of 26.8 nM and 78 nM, respectively. | ||||
| GC79372 | Rosnilimab (Mouse IgG2a) | - | >98.00% | |
Rosnilimab (Mouse IgG2a ) is a mouse-derived IgG2a antibody, Rosnilimab. | ||||
| GC79374 | PD-1/PD-L1-IN-63 | 2691796-92-4 | >98.00% | |
PD-1/PD-L1-IN-63 is an orally active PD-1/PD-L1 inhibitor with an IC 50 of 9.1 nM. | ||||
| GC79379 | Anti-Mouse IFN Beta Antibody (MIB-5E9.1) | - | >96.00% | |
Anti-Mouse IFN Beta Antibody (MIB-5E9.1) is an antibody targeting mouse IFN-β. Anti-Mouse IFN Beta Antibody (MIB-5E9.1) blocks the IFN-β signaling pathway, abolishes LPS-induced upregulation of B7H1 and GITRL in dendritic cells, restores dendritic cell-dependent T cell proliferation impaired by LPS exposure, and reverses LPS-induced upregulation of PD-1 on splenic T cells. | ||||
| GC79389 | ETI41 | 2773474-99-8 | >98% | |
ETI41 is an orally active, selective TLR inhibitor that targets the nucleoside-binding Site I on TLR7 ( IC 50 = 0.63 μM) and TLR9 ( IC 50 = 0.16 μM), sparing surface TLRs (including TLR1/TLR2, TLR2/TLR6, TLR4 and TLR5). | ||||
| GC79390 | ETI60 | 2773475-11-7 | >99.50% | |
ETI60 is an orally active, selective TLR inhibitor that targets the nucleoside-binding Site I on TLR7 ( IC 50 = 0.68 μM) and TLR9 ( IC 50 = 0.12 μM), sparing surface TLRs (including TLR1/TLR2, TLR2/TLR6, TLR4 and TLR5). | ||||
| GC79406 | SMU-Z1 | 2410782-66-8 | >99.00% | |
SMU-Z1 is a TLR1/2 heterodimer agonist with an EC 50 of 4.88 nM. | ||||
| GC79417 | Biotin-itaconate | 3086566-93-7 | >93.00% | |
Biotin-itaconate is a biotin-labeled itaconic anhydride that targets PD-L1. | ||||
| GC79421 | LM-299 | - | >95.50% | |
LM-299 is a bispecific antibody targeting PD-1 and VEGF with anti-tumor activity. | ||||
| GC79451 | JP-11646 | 1902983-63-4 | >98.50% | |
JP-11646 is a pan-PIM inhibitor with increased potency against PIM2 ( IC 50 = 0.5 nM). | ||||
| GC79463 | NGI-189 | 2763063-26-7 | >99.00% | |
NGI‑189 is a selective OST‑A inhibitor. | ||||
| GC79465 | STAT3-IN-52 hydrochloride | - | >96.00% | |
STAT3-IN-52 hydrochloride is an orally active STAT3 inhibitor with a K i value of 2.42 μM. | ||||
