Apoptosis

There are many forms of cell death, most of which can be triggered by a variety of stimuli and physiological conditions. The often compared are apoptosis and necrosis. Apoptosis has become the focus of research area due to its complex nature and the different roles of maintaining healthy and self-sustaining biological entities. On the other hand, necrosis is a form of cell damage against acute external injury and trauma, leading to passive cell death and causing an inflammatory response. [1]

The BCl-2 family has been identified as its important role in apoptosis. The BH domain promotes interaction of family members with one another and may be indicative of pro-apoptotic or anti-apoptotic functions. Usually the BCL-2 family have been classified into one of three subfamilies; anti-apoptosis,  BH3 only (pro-apoptotic) and pro-apoptotic proteins. The great promise for cancer therapy has been shown in recent research about BCL-2 targeting.[2]

In the cell cycle, apoptosis acts as a fail-safe measure to prevent fidelity and proliferation quality. Although a certain degree of genetic variation is allowed and evolution is promoted, regenerative cells with extensive genetic errors and cell damage are subject to apoptosis. P53 is the Key role in the cell cycle system which  initiate the apoptosis in certain cell types. P53 is a widely studied tumor suppressor. The p53 tumor suppressor gene is most frequently mutated in cancer cells (mutation occurs in more than 50% of human cancers) [3], which makes the restriction mechanism ineffective. Tumorigenesis is likely to commence when the p53-based preventive system loses its function completely.

Expression of stimuli, such as DNA damage, hypoxia and activation of certain oncoproteins (eg, Myc, Ras) are dependent on the apoptotic pathway of p53 [4]. The transactivation function of p53 plays an important role in inducing apoptosis, the pro-apoptotic proteins, Bax and lgF-Bp3, are transcriptional targets of p53.[5] As a well-known tumor suppressor, p53 is recognized for its ability to initiate apoptosis in the cell cycle and its ability to induce cell arrest and DNA repair in regenerative cells. In addition to p53, there are many other cell cycle regulators that can affect apoptosis (eg, pRb, p21).

Many studies have emphasized the importance of apoptosis in the self-defense mechanism or immune system. The immune system is responsible for rendering the host resistant to a variety of external pathogens. Apoptosis is an integral part of the immune system and helps maintain the homeostasis of the immune system.  Secondly, the immune system relies on apoptosis to eliminate unwanted functional maturation of T cells and B cells [6].  Finally, apoptosis confers cytotoxicity to certain cell types (ie, cytotoxic T lymphocytes and natural killer cells). A well-coordinated disruption protocol allows these cells to destroy target cells while the target cells remain intact. Cytotoxic T lymphocytes (CTLs) can induce target cell death in two ways, one of which involves perforin and granzymes.

  • Majno G. and Joris I. (1995) Apoptosis, oncosis, and necrosis. An overview of cell death. Am. J. Pathol. 146, 3–15
  • Zhiqing Liu, et al. Drug Discov Today. 2016 Jun; 21(6): 989–996.
  • Wang X.W. and Harris C.C. (1997) p53 tumor-suppressor gene: clues to molecular carcinogenesis. J. Cell. Physiol. 173, 247–255 10.1002/(SICI)1097-4652(199711)173:2%3c247::AID-JCP30%3e3.0.CO;2-A.
  • Levine A.J. (1997) p53, the cellular gatekeeper for growth and division. Cell 88, 323–331 10.1016/S0092-8674(00)81871-1.
  • Owen-Schaub LB,et al. Owen-Schaub LB,Wild-type human p53 and a temperature-sensitive mutant induce Fas/APO-1 expression. Mol Cell Biol. 1995 Jun; 15(6):3032-40.
  • Russell J.H. (1995) Activation-induced death of mature T cells in the regulation of immune responses. Curr. Opin. Immunol. 7, 382–388 10.1016/0952-7915(95)80114-6.

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  1. ABT-263 (Navitoclax)

    Catalog No. A10022
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    Bcl-2 inhibitor
    ABT-263 also called Navitoclax is a potent and orally bioavailable Bcl-2 family inhibitor (Ki's of <1 nmol/L for Bcl-2, Bcl-xL, and Bcl-w).ABT-263 maintains a high affinity for Bcl-xL, Bcl-2, and Bcl-w, (Ki ≤1 nmol/L), but binds more weakly to Mcl-1 and A1.
    Learn More
  2. ABT-737

    Catalog No. A10255
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    Bcl-2 Inhibitor
    ABT-737 is a pan-Bcl-2 inhibitor. IC50 values ranged from 192 nM (the pre-B cell line Hal-01) to <10 μM (Nalm-6, K562 and HL-60). Learn More
  3. Jaceosidin

    Catalog No. A12080
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    Jaceosidin is a pharmacologically active flavone derived from Artemisia argyi, inhibits phorbol-ester-induced upregulation of COX-2 and MMP-9 by blocking phosphorylation of ERK-1 and -2 in cultured human mammary epithelial cells. Learn More
  4. ABT-199 (Venetoclax)

    Catalog No. A12500
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    Bcl-2 inhibitor
    ABT-199 is a so-called BH3-mimetic drug, which is designed to block the function of the protein Bcl 2. Learn More
  5. WEHI539

    Catalog No. A13005
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    Bcl-XL inhibitor
    WEHI539 is a selective inhibitor of Bcl-XL with IC50 of 1.1 nM. Learn More
  6. AZD5991

    Catalog No. A16880
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    Mcl-1 inhibitor
    AZD-5991 is a potent and selective Mcl-1 inhibitor with an IC50 of 0.7 nM in FRET assay and a Kd of 0.17 nM in surface plasmon resonance (SPR) assay. Learn More
  7. A-385358

    Catalog No. A17064
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    Bcl-XL inhibitor
    A-385358 is an inhibitor of Bcl-XL that enhances the in vitro cytotoxic activity of numerous chemotherapeutic agents (paclitaxel, etoposide, cisplatin, and doxorubicin) in several tumor cell lines. Learn More
  8. Maritoclax (Marinopyrrole A)

    Catalog No. A17206
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    Mcl-1 inhibitor
    Marinopyrrole A, aslo known as Maritoclax, is a selective inhibitor of Mcl-1 with IC50 value of 10.1μM. Learn More
  9. ML311

    Catalog No. A18364
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    Mcl-1/Bim interaction inhibitor
    ML311 is a potent and selective inhibitor of the Mcl-1/Bim interaction Learn More
  10. Obatoclax mesylate (GX15-070)

    Catalog No. A10665
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    Bcl-2 Inhibitor
    Bcl-2 homology domain-3 (BH3) mimetic,antagonize all antiapoptotic Bcl-2 family proteins (average IC50, 3 umol/L), including Mcl-1 (IC50, 2.9 umol/L) and Bfl-1 (IC50, 5 umol/L). Learn More
  11. MIM1

    Catalog No. A16315
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    Mcl-1 inhibitor
    MIM1 is a selective small molecule inhibitor of Mcl-1(IC50= 4.8 μM) that overcomes Mcl-1-dependent leukemia cell survival. Learn More
  12. HA14-1

    Catalog No. A11448
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    Bcl-2 inhibitor
    HA14-1 interacts with Bcl-2 and inhibits the antiapoptotic effect of Bcl-2. Learn More
  13. Sabutoclax

    Catalog No. A12823
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    Bcl-2 inhibitor
    Sabutoclax(BI-97C1) is a pan-Bcl-2 inhibitor, including Bcl-xL, Bcl-2, Mcl-1 and Bfl-1 with IC50 of 0.31 μM, 0.32 μM, 0.20 μM and 0.62 μM, respectively. Learn More
  14. UMI-77

    Catalog No. A14222
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    Mcl-1 inhibitor
    UMI-77 is a selective Mcl-1 inhibitor with Ki of 490 nM, showing selectivity over other members of Bcl-2 family. Learn More
  15. AT-101

    Catalog No. A15004
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    Bcl-2 Inhibitor
    AT101, the R-(-) enantiomer of Gossypol acetic acid, binds with Bcl-2, Bcl-xL and Mcl-1 with Ki of 0.32μM, 0.48μM and 0.18μM. Learn More
  16. AT101 acetic acid

    Catalog No. A13578
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    pan Bcl-2 inhibitor
    AT101, the R-(-) enantiomer of Gossypol acetic acid, binds with Bcl-2, Bcl-xL and Mcl-1 with Ki of 0.32 μM, 0.48 μM and 0.18 μM; does not inhibit BIR3 domain and BID Learn More
  17. A-1155463

    Catalog No. A16112
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    BCL-XL inhibitor
    A-1155463 is a highly potent and selective BCL-XL inhibitor, A-1155463 shows picomolar binding affinity to BCL-XL (Ki = <0.01 nM), and >1000-fold weaker binding to BCL-2 (Ki = 80 nM) and related proteins BCL-W (Ki = 19 nM) and MCL-1 (Ki > 440 nM) Learn More
  18. A-1331852

    Catalog No. A16190
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    BCL-XL inhibitor
    A-1331852 is a potent and selective BCL-XL inhibitor. BCL-XL is the major antiapoptotic survival protein and may be a novel therapeutic target in CML. Learn More
  19. TW-37

    Catalog No. A10955
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    Bcl-2 inhibitor
    TW-37, a small-molecule inhibitor of Bcl-2, inhibits cell growth and induces apoptosis in pancreatic cancer mediated through a novel pathway involving inactivation of Notch-1 and Jagged-1. Learn More
  20. BM-1074

    Catalog No. A12743
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    Bcl-2/Bcl-xL inhibitor
    BM-1074 is a potent and efficacious Bcl-2/Bcl-xL inhibitor with Ki of <1 nM. Learn More
  21. (+)-Apogossypol

    Catalog No. A16316
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    Bcl-2 family inhibitor
    (+)-Apogossypol is a potent inhibitor of Bcl-2 family proteins; competing with the BH3 peptide-binding sites on Bcl-2, Bcl-XL, Mcl-1, Bcl-W, and Bcl-B, but not Bfl-1, with IC50s of 0.5 to 2 μM. Learn More
  22. Acetate gossypol

    Catalog No. A14795
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    Bcl-2 Inhibitor
    Acetate gossypol, a polyphenolic compound isolated from cottonseeds, inhibits Bcl-2 by acting as a BH3 mimetic. Learn More
  23. BH3I-1

    Catalog No. A16061
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    Bcl-XL antagonist
    BH3I-1 is a cell permeable BH3 mimetic that binds to Bcl-xL Learn More
  24. Apogossypolone (ApoG2)

    Catalog No. A16314
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    Bcl-2 inhibitor
    Apogossypolone is a nonpeptidic small-molecule inhibitor of Bcl-2 with Learn More
  25. (S)-Gossypol acetic acid

    Catalog No. A16323
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    (S)-Gossypol acetic acid is a inhibitor of Bcl-2, potently induce cell death in Jurkat cells overexpressing Bcl-2 (IC50, 18.1μM) or Bcl-xL (IC50, 22.9μM). Learn More
  26. A-1210477

    Catalog No. A15545
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    MCL-1 inhibitor
    A-1210477 is a potent and selective MCL-1 inhibitor. A-1210477 induces the hallmarks of intrinsic apoptosis and demonstrates single agent killing of multiple myeloma and non-small cell lung cancer cell lines. Learn More
  27. BDA-366

    Catalog No. A15821
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    Bcl-2 antagonist
    BDA-366 selectively inhibits BCL2, converting it to a cell death inducer. Learn More
  28. WEHI-539 hydrochloride

    Catalog No. A13327
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    Bcl-xL inhibitor
    WEHI-539 hydrochloride is a small-molecule inhibitor of BCL-xL with IC50 value of 1.1 nM. Learn More
  29. BAM 7

    Catalog No. A12907
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    Bax activator
    BAM 7 binds the BAX trigger site with an EC50 ~ 3.3 μM as measured in a competitive FP assay using FITC-BIM SAHB and BAX. Learn More
  30. Bcl-2 Inhibitor

    Catalog No. A13580
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    Bcl-2 Inhibitor
    Bcl-2 Inhibitor contains a mixture of two tautomers. A potent, cell-permeable, Bcl-2 inhibitor competes with Bak BH3 peptide for binding to Bcl-2 and Bcl-XL in vitro (IC50 =10 uM and 7 uM, respectively). Learn More
  31. Gambogic acid

    Catalog No. A11988
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    Bcl-2 inhibitor
    Gambogic acid is a natural product isolated from the Garcinia hanburyi tree. Gambogic Acid activates caspases with EC50 of 0.78-1.64 μM and competitively inhibits Bcl-XL, Bcl-2, Bcl-W, Bcl-B, Bfl-1 and Mcl-1 with IC50 of 1.47, 1.21, 2.02, 0.66, 1.06 and 0.79 μM, respectively. Learn More
  32. Bax channel blocker

    Catalog No. A15335
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    Bax channel blocker
    Bax channel blocker is a potent inhibitor of Bax-mediated mitochondrial cytochrome C release (IC50 = 0.52 μM). Learn More
  33. Bax inhibitor peptide P5

    Catalog No. A15336
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    Bax inhibitor
    Bax inhibitor peptide P5, cell-permeable synthetic peptide inhibitor of Bax translocation to mitochondria; designed from Ku70, a protein that is suggested to suppress the mitochondrial translocation of Bax. Inhibits Bax-mediated apoptosis in vitro. Learn More
  34. Bax inhibitor peptide V5

    Catalog No. A15337
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    Bax inhibitor
    Bax inhibitor peptide V5, cell-permeable synthetic peptide inhibitor of Bax translocation to mitochondria; designed from Ku70, a protein that is suggested to suppress the mitochondrial translocation of Bax. Inhibits Bax-mediated apoptosis in vitro. Learn More
  35. Bax inhibitor peptide, negative control

    Catalog No. A15338
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    Bax inhibitor
    Bax inhibitor peptide, negative control, negative control peptide for the Bax inhibitor peptides V5 and P5 , which inhibit Bax translocation to mitochondria and Bax-mediated apoptosis in vitro. Learn More
  36. Muristerone A

    Catalog No. A15340
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    EcR agonist
    Muristerone A is a phytoecdysteroid analog of ecdysone which induces genes in mammalian cells and causes apoptosis in cells transfected with wild-type Bax. Learn More
  37. CID5721353

    Catalog No. A16192
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    BCL6 inhibitor
    CID5721353 is a B-Cell Lymphoma 6 Inhibitor (BCL6 inhibitor). Learn More
  38. Pyridoclax (MR-29072)

    Catalog No. A16380
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    Mcl-1 inhibitor
    Pyridoclax is a potent Mcl-1 inhibitor with Kd value of 25 nM. Learn More
  39. Z-VAD-FMK

    Catalog No. A12373
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    Pan Caspase Inhibitor
    Z-VAD-FMK is a cell-permeable, irreversible pan-caspase inhibitor. Inhibits caspase processing and apoptosis induction in tumor cells in vitro (IC50 = 0.0015 - 5.8 mM). Active in vivo. Learn More
  40. Nivocasan (GS-9450)

    Catalog No. A14100
    Caspase inhibitor
    Nivocasan is a novel caspase-inhibitor has demonstrated hepatoprotective activity in fibrosis/apoptosis animal models. Learn More
  41. Z-DEVD-FMK

    Catalog No. A13503
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    Caspase-3 Inhibitor
    Z-DEVD-FMK is a specific, irreversible Caspase-3 inhibitor. Learn More
  42. Z-LEHD-FMK

    Catalog No. A14358
    Caspase-9 Inhibitor
    Z-LEHD-FMK is a synthetic peptide that irreversibly inhibits caspase-9 and related caspase activity. Learn More
  43. Q-VD-OPh hydrate

    Catalog No. A14915
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    Caspase inhibitor
    Q-VD-OPH is a selective, brain and cell permeable, highly potent and irreversible inhibitor of caspase-3 ( IC50=25nm), caspase-1 (IC50=50nM), caspase-8 (IC50=100nM) and caspase-9 (IC50=430nM). Learn More
  44. Z-WEHD-FMK

    Catalog No. A14916
    Caspase inhibitor
    Z-WEHD-FMK is a synthetic peptide that irreversibly inhibits caspase-5 and related caspase activity. Learn More
  45. Caspase-3/7 Inhibitor I

    Catalog No. A14919
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    Caspase-3/7 Inhibitor
    Caspase-3/7 Inhibitor I is a potent, cell-permeable, and specific, reversible inhibitor of caspase-3 (Ki = 60 nM) and caspase-7 (Ki = 170 nM). Learn More
  46. Ac-LEHD-AFC

    Catalog No. A15291
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    Fluorogenic caspase substrate
    Ac-LEHD-AFC, fluorogenic caspase substrate. Analog of the caspase-9 substrate, LEHD-AFC. Learn More
  47. AZ 10417808

    Catalog No. A15294
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    Caspase-3 inhibitor
    AZ 10417808, selective non-peptide inhibitor of caspase-3 (Ki = 247 nM); displays > 40-fold selectivity over caspases 1, 2, 6, 7 and 8 (Ki > 10 uM). Learn More
  48. Ivachtin

    Catalog No. A15300
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    Caspase-3 inhibitor
    Ivachtin is a potent, cell-permeable, reversible, non-competitive inhibitor of Caspase-3 (IC50 = 23 nM). Learn More
  49. PETCM

    Catalog No. A15308
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    Caspase-3 activator
    PETCM is an activator of caspase-3 and a stimulator of apoptosome formation in HeLa cell cytosols. Learn More
  50. Ac-IEPD-AFC

    Catalog No. A15319
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    Fluorogenic caspase substrate
    Ac-LEHD-AFC is a fluorogenic substrate for caspase-4, caspase-5, and caspase-9. Learn More

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