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(114)
- Pyroptosis(37)
- 14.3.3 Proteins(1)
- Apoptosis Inducers(42)
- Bax(6)
- Bcl-2 Family(154)
- Bcl-xL(8)
- c-RET(8)
- IAP(31)
- KEAP1-Nrf2(81)
- MDM2(12)
- p53(145)
- PC-PLC(4)
- PKD(6)
- RasGAP (Ras- P21)(1)
- Survivin(12)
- Thymidylate Synthase(10)
- TNF-α(189)
- Other Apoptosis(877)
- APC(6)
- PD-1/PD-L1 interaction(106)
- ASK1(4)
- PAR4(2)
- RIP kinase(55)
- FKBP(23)
- Cuproptosis(4)
Products Related to Apoptosis(3030)
- GC81305Tyrosine kinase-IN-11CAS: 3031972-21-8Purity: >98.50%
Tyrosine kinase-IN-11 (Compound 4b) is a tyrosine kinase inhibitor.
- GC81306PRT-060318 dihydrochlorideCAS: 3032567-93-1Purity: >98.50%
PRT-060318 (PRT318) dihydrochloride is a potent, selective and orally active tyrosine kinase Syk inhibitor with an IC 50 of 3 nM.
- GC81312PARP1/c-Met-IN-3CAS: 3123529-62-1Purity: >98%
PARP1/c-Met-IN-3 (Compound L19) is a selective c-Met and PARP1 inhibitor, with an IC 50 of 5.4 nM against c-Met and an IC 50 of 3.7 nM against PARP1.
- GC81320PapaverolineCAS: 574-77-6Purity: >98%
Papaveroline is a Fyn tyrosine kinase inhibitor, Na +,K + -ATPase inhibitor with an IC 50 of 0.20 mM, Mg 2+ -ATPase inhibitor, K + -activated pNPPase inhibitor with an IC 50 of 1.51 mM, and apoptosis inducer [1] [2] [3] . Papaveroline binds to the active site of Fyn tyrosine kinase and forms stable interactions with pocket amino acid residues [1] . Papaveroline induces cell apoptosis, produces pycnotic and fragmented cell nuclei, and does not reduce intracellular ATP levels [3] . Papaveroline is a dopamine-derived neurotoxin candidate associated with the pathogenesis of Parkinson's disease [3] . Papaveroline can be used in the research of Alzheimer's disease and Parkinson's disease [3] .
- GC81323PDGFRA/CAIX/XII-IN-1Purity: >98.00%
PDGFRA/CAIX/XII-IN-1 is an inhibitor of PDGFRA, CA IX and CA XII, with an IC 50 of 20 nM against PDGFRA, a K i of 93.3 nM against CA IX, and a K i of 80.0 nM against CA XII.
- GC81335MST3-IN-1 TFAPurity: >99.00%
MST3-IN-1 TFA (Compound LD-1) is a selective and orally active MST3 inhibitor, with an IC 50 of 122.4 nM.
- GC813928-Oxo-dGTP trisodium solution (100 mM)Purity: >98.50%
8-Oxo-dGTP (8-Oxo-Deoxyguanosine triphosphate) trisodium solution (100mM) is an oxidized guanine nucleotide formed by ROS-mediated oxidative modification of dGTP, and it also serves as a key substrate for 8-oxo-dGTP pyrophosphohydrolases (such as hMTH1 and E.
- GC81420(-)-Aspartic acid-d 3CAS: 1202063-44-2Purity: >99.50%
(-)-Aspartic acid -d 3 ((R)-Aspartic acid-d 3 ) is the deuterium labeled (-)-Aspartic acid.
- GC81446ARF(26-44), cell-permeable acetatePurity: >99.00%
ARF(26-44), cell-permeable acetate is a cell-penetrating peptide derived from a specific amino acid sequence of the p14ARF tumor suppressor protein.
- GC81522WWZ-11-098Purity: >98.00%
WWZ-11-098 is a selective CDK6 PROTAC degrader with DC 50 of 2.6 nM.
- GC81541BMAP-27 acetatePurity: >98.00%
BMAP-27 acetate is a cationic amphipathic α-helical antimicrobial peptide with anticancer activity.
| Catalog No. | Product Name | CAS No. | Purity | Structure |
|---|---|---|---|---|
| GC81305 | Tyrosine kinase-IN-11 | 3031972-21-8 | >98.50% | |
Tyrosine kinase-IN-11 (Compound 4b) is a tyrosine kinase inhibitor. | ||||
| GC81306 | PRT-060318 dihydrochloride | 3032567-93-1 | >98.50% | |
PRT-060318 (PRT318) dihydrochloride is a potent, selective and orally active tyrosine kinase Syk inhibitor with an IC 50 of 3 nM. | ||||
| GC81312 | PARP1/c-Met-IN-3 | 3123529-62-1 | >98% | |
PARP1/c-Met-IN-3 (Compound L19) is a selective c-Met and PARP1 inhibitor, with an IC 50 of 5.4 nM against c-Met and an IC 50 of 3.7 nM against PARP1. | ||||
| GC81316 | RC148 | - | >99.50% | |
RC148 is a humanized IgG1 bispecific antibody targeting VEGF and PD-1. | ||||
| GC81320 | Papaveroline | 574-77-6 | >98% | |
Papaveroline is a Fyn tyrosine kinase inhibitor, Na +,K + -ATPase inhibitor with an IC 50 of 0.20 mM, Mg 2+ -ATPase inhibitor, K + -activated pNPPase inhibitor with an IC 50 of 1.51 mM, and apoptosis inducer [1] [2] [3] . Papaveroline binds to the active site of Fyn tyrosine kinase and forms stable interactions with pocket amino acid residues [1] . Papaveroline induces cell apoptosis, produces pycnotic and fragmented cell nuclei, and does not reduce intracellular ATP levels [3] . Papaveroline is a dopamine-derived neurotoxin candidate associated with the pathogenesis of Parkinson's disease [3] . Papaveroline can be used in the research of Alzheimer's disease and Parkinson's disease [3] . | ||||
| GC81323 | PDGFRA/CAIX/XII-IN-1 | - | >98.00% | |
PDGFRA/CAIX/XII-IN-1 is an inhibitor of PDGFRA, CA IX and CA XII, with an IC 50 of 20 nM against PDGFRA, a K i of 93.3 nM against CA IX, and a K i of 80.0 nM against CA XII. | ||||
| GC81324 | FGF7p | 2758194-43-1 | >99.00% | |
FGF7p is a small molecule peptide and a potential bladder protector. | ||||
| GC81328 | GZD-552 | - | >98% | |
GZD-552 is a potent orally active FAK inhibitor with a human FAK IC 50 of 5.8 nM. | ||||
| GC81335 | MST3-IN-1 TFA | - | >99.00% | |
MST3-IN-1 TFA (Compound LD-1) is a selective and orally active MST3 inhibitor, with an IC 50 of 122.4 nM. | ||||
| GC81350 | THR-123 TFA | - | >99.50% | |
THR-123 TFA is an orally active ALK3 peptide agonist. | ||||
| GC81392 | 8-Oxo-dGTP trisodium solution (100 mM) | - | >98.50% | |
8-Oxo-dGTP (8-Oxo-Deoxyguanosine triphosphate) trisodium solution (100mM) is an oxidized guanine nucleotide formed by ROS-mediated oxidative modification of dGTP, and it also serves as a key substrate for 8-oxo-dGTP pyrophosphohydrolases (such as hMTH1 and E. | ||||
| GC81420 | (-)-Aspartic acid-d 3 | 1202063-44-2 | >99.50% | |
(-)-Aspartic acid -d 3 ((R)-Aspartic acid-d 3 ) is the deuterium labeled (-)-Aspartic acid. | ||||
| GC81439 | SZ0232 | 924851-91-2 | >99.00% | |
SZ0232 is a selective mPGES-2 inhibitor. | ||||
| GC81446 | ARF(26-44), cell-permeable acetate | - | >99.00% | |
ARF(26-44), cell-permeable acetate is a cell-penetrating peptide derived from a specific amino acid sequence of the p14ARF tumor suppressor protein. | ||||
| GC81447 | ALDOA-IN-1 | - | >98.00% | |
ALDOA-IN-1 is an aldolase A (ALDOA) inhibitor. | ||||
| GC81453 | FOXM1-IN-3 | - | >98% | |
FOXM1-IN-3 is a potent FOXM1 inhibitor. | ||||
| GC81461 | FPP29 | - | >99.00% | |
FPP29 is a potent peptide-based FOXM1 PROTAC degrader. | ||||
| GC81481 | SKLB06489 | - | >98% | |
SKLB06489 is a selective and orally active inhibitor of type I PRMT enzymes, with IC 50 values of 64.55 nM ( PRMT1 ), 4.21 nM ( PRMT6 ), and 51.27 nM ( PRMT8 ). | ||||
| GC81499 | CT-179 | 1996636-69-1 | >99.50% | |
CT-179 is a brain-penetrant and orally active OLIG2 inhibitor with a human IC 50 of 1250 nM. | ||||
| GC81512 | dCDK9-202 | - | >98.50% | |
dCDK9-202 is a CDK9 PROTAC degrader with a DC 50 of 3.5 nM. | ||||
| GC81522 | WWZ-11-098 | - | >98.00% | |
WWZ-11-098 is a selective CDK6 PROTAC degrader with DC 50 of 2.6 nM. | ||||
| GC81531 | PBX-7016 | 3003834-34-9 | >98.00% | |
PBX-7016 is a DNA topoisomerase I inhibitor and DDX5 degrader. | ||||
| GC81532 | Auristatin S TFA | - | >99.00% | |
Auristatin S TFA is a potent Auristatin payload. | ||||
| GC81541 | BMAP-27 acetate | - | >98.00% | |
BMAP-27 acetate is a cationic amphipathic α-helical antimicrobial peptide with anticancer activity. | ||||
