Apoptosis

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  1. XIAP/cIAP1 antagonist

    Birinapant, also known as TL32711, is a synthetic small molecule and peptido mimetic of second mitochondrial-derived activator of caspases (SMAC) and inhibitor of IAP (Inhibitor of Apoptosis Protein) family proteins, with potential antineoplastic activity.
  2. cIAP-2 antagonist

    SM-164 is a potent cell-permeable and bivalent Smac mimetic which bind to a XIAP protein with a Ki value of 0.56 nM, and binds to cIAP-1 and cIAP-2 proteins with Ki values of 0.31 and 1.1 nM, respectively.
  3. 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).
  4. Survivin Inhibitor

    YM155 is a novel small molecule survivin suppressant with an IC50 of 0.54 nM for the inhibition of survivin promoter activity.
  5. 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).
  6. HO-1 inhibitor

    Zinc Protoporphyrin (Zn(II)-protoporphyrin IX) is a competitive heme oxygenase-1 (HO-1) inhibitor, markedly attenuates the protective effects of Phloroglucinol (PG) against H2O2.
  7. Caspase-1 inhibitor

    Z-YVAD-FMK is a potent cell-permeable and irreversible inhibitor of caspase-1.
  8. NF-κB inhibitor

    QNZ inhibits the activation of the transcription factor NF-κB and has been used to investigate NF-κB signaling.
  9. PERK inhibitor

    GSK2606414 is an orally available, potent, and selective PERK inhibitor with IC50 of 0.4 nM.
  10. p53 activator

    JNJ-26854165 is one of p53-activating agents and synergizes with AraC or doxorubicin to induce p53-mediated apoptosis and may provide a novel therapeutic approach for the treatment of acute leukemias.
  11. RIPK1 inhibitor

    Necrostatin-1 is an ATP-competitive, allosteric inhibitor of receptor-interacting protein kinase 1 (RIPK1) (EC50 = 182 nM).
  12. Bcl-2 inhibitor

    ABT-199 is a so-called BH3-mimetic drug, which is designed to block the function of the protein Bcl 2.
  13. 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.
  14. Antagonist of IAPs inhibitor

    LCL161 is an orally bioavailable second mitochondrial-derived activator of caspases (SMAC) mimetic and inhibitor of IAP (Inhibitor of Apoptosis Protein) family of proteins, with potential antineoplastic activity.
  15. 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.
  16. eIF2α dephosphorylation inhibitor

    Salubrinal is a cell-permeable, selective inhibitor of cellular phosphatase complexes that dephosphorylate eukaryotic translation initiation factor 2 subunit α (eIF2α). Protects cells from endoplasmic reticulum stress-induced apoptosis (EC50 ~ 15 μM).
  17. Caspase activator

    PAC-1 is an activator of procaspase-3 induces apoptosis in cancer cells with EC50 of 2.08 μM.
  18. p53 activator

    Tenovin-6 is a analog of tenovin-1. Tenovin-6 inhibits the protein deacetylase activities of purified human SIRT1, SIRT2, and SIRT3 in vitro with IC50 values of 21, 10, and 67 uM, respectively.
  19. p53 Inhibitor

    Pifithrin-beta is a small molecule inhibitor of p53.
  20. Caspase-3 inhibitor

    Z-DQMD-FMK is a synthetic peptide that irreversibly inhibits the activity of Caspase-3.
  21. caspase 8 inhibitor

    Z-IETD-FMK is a specific inhibitor of caspase 8.
  22. Caspase-9 Inhibitor

    Z-LEHD-FMK is a synthetic peptide that irreversibly inhibits caspase-9 and related caspase activity.
  23. PERK Inhibitor

    GSK2656157 is an ATP-competitive inhibitor of PERK enzyme activity with an IC(50) of 0.9 nmol/L. It is highly selective for PERK with IC(50) values >100 nmol/L against a panel of 300 kinases.
  24. 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).
  25. Ubiquitin ligase inducer

    Lenalidomide is a derivative of thalidomide. In vitro, lenalidomide has three main activities: direct anti-tumor effect, inhibition of the micro environment support for tumor cells, and immunomodulatory role. It induces tumor cell apoptosis directly and indirectly by inhibition of bone marrow stromal cell support, by anti-angiogenic and anti-osteoclastogenic effects, and by immunomodulatory activity.
  26. IMPDH inhibitor

    AVN-944 (also known as VX-944) serves as an effective oral inhibitor, specifically targeting and inhibiting IMPDH (inosine monophosphate dehydrogenase). This enzyme plays a crucial role as a rate-limiting factor in the synthesis of guanine nucleotides from scratch. Additionally, AVN-944 acts against the synthesis of RNA in arenaviruses, effectively preventing arenavirus infections. Demonstrating a wide spectrum of anti-cancer properties, AVN-944 is utilized in research related to multiple myeloma (MM) and acute myeloid leukemia (AML).

  27. Mdm2 inhibitor

    YH239-EE is a potent p53-MDM2 antagonist and an apoptosis inducer.
  28. N-SMase inhibitor

    GW4869 is a cell permeable, selective inhibitor of N-SMase (neutral sphingomyelinase).

  29. PERK inhibitor

    ISRIB is a potent and selective PERK inhibitor with IC50 of 5 nM.
  30. VEGFR inhibitor

    Regorafenib (BAY 73-4506) is a multikinase inhibitor with IC50 of 17, 40 and 69 nM c-KIT, VEGFR2, B-Raf. Regorafenib (BAY 73-4506) is an orally bioavailable multikinase inhibitor targeting both the tumor and its vasculature.
  31. MDM2 degrader

    MD-224 is a first-in-class and highly potent small-molecule human murine double minute 2 (MDM2) degrader based on the proteolysistargeting chimera (PROTAC) concept. MD-224 has the potential to be a new class of anticancer agent.
  32. ASK1 inhibitor

    Selonsertib is an orally bioavailable inhibitor of apoptosis signal-regulating kinase 1 (ASK1), with potential anti-inflammatory, antineoplastic and anti-fibrotic activities.
  33. p53 activator

    RITA, also referred to as NSC 652287, is a trycyclic thiophene derivative that binds to MDM2, disrupting the MDM2-p53 complex and subsequently activating p53 and inducing apoptosis.
  34. Aloe emodin is a anthraquinone present in aloe latex, an exudate from the aloe plant. It has a strong stimulant-laxative action.

  35. Mdm2 antagonist

    MDM2 antagonist nutlin-3 is a potent inducer of apoptosis.
  36. Caspase-3 Inhibitor

    Z-DEVD-FMK is a specific, irreversible Caspase-3 inhibitor.
  37. 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). it 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.
  38. GPX4 inhibitor

    ML-210??the most potent compound in the nitroisoxazole series?? is a selective covalent inhibitor of glutathione peroxidase 4 (GPX4) by binding the selenocysteine residue.
  39. 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.
  40. MDMX inhibitor

    SJ 172550 is the first MDMX inhibitor with EC50 of 0.84 uM; binds reversibly to MDMX and effectively kills retinoblastoma cells in which the expression of MDMX is amplified.
  41. HDAC inhibitor

    Sulforaphane activates Nrf2 and inhibits high glucose-induced progression of pancreatic cancer via AMPK dependent signaling. Sulforaphane has shown anti-cancer and anti-inflammatory activities.
  42. MDM2 inhibitor

    Nutlin 3a is a potent inhibitor of MDM2 (mouse double minute 2) binding to p53 that induces the expression of p53 regulated genes, and shows potent antiproliferative activity in cells expressing functional p53.
  43. Caspase inhibitor

    Nivocasan is a novel caspase-inhibitor has demonstrated hepatoprotective activity in fibrosis/apoptosis animal models.
  44. Bax channel blocker

    Bax channel blocker is a potent inhibitor of Bax-mediated mitochondrial cytochrome C release (IC50 = 0.52 μM).
  45. 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.
  46. 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).
  47. 5-Fluorouridine is a metabolite of 5-fluorouracil with anticancer activity.
  48. Aurora inhibitor

    Danusertib (PHA-739358) is an Aurora kinase inhibitor for Aurora A/B/C with IC50 of 13 nM/79 nM/61 nM in cell-free assays, modestly potent to Abl, TrkA, c-RET and FGFR1, and less potent to Lck, VEGFR2/3, c-Kit, CDK2, etc. Phase 2
  49. 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.
  50. 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)

Items 1-50 of 1195

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