Bcl-2 Family

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  1. 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).
  2. Bcl-2 inhibitor

    ABT-199 is a so-called BH3-mimetic drug, which is designed to block the function of the protein Bcl 2.
  3. 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.
  4. 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.
  5. 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).
  6. 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).

  7. 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.
  8. Bax channel blocker

    Bax channel blocker is a potent inhibitor of Bax-mediated mitochondrial cytochrome C release (IC50 = 0.52 μM).
  9. 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.
  10. 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).
  11. 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.
  12. 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)
  13. 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.
  14. Bcl-2 inhibitor

    HA14-1 interacts with Bcl-2 and inhibits the antiapoptotic effect of Bcl-2.
  15. 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.
  16. Bcl-2/Bcl-xL inhibitor

    BM-1074 is a potent and efficacious Bcl-2/Bcl-xL inhibitor with Ki of <1 nM.
  17. Bcl-XL inhibitor

    WEHI539 is a selective inhibitor of Bcl-XL with IC50 of 1.1 nM.
  18. 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
  19. 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.
  20. 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.
  21. FX1

    BCL6 inhibitor

    FX1 is an inhibitor of the transcription factor B cell lymphoma 6 (BCL6) with IC50 value of ~35 μM.
  22. Bcl-2/Bcl-XL inhibitor

    AZD-4320 is a BH3 mimetic and dual Bcl-2/Bcl-XL inhibitor.
  23. Mcl-1 inhibitor

    Marinopyrrole A, aslo known as Maritoclax, is a selective inhibitor of Mcl-1 with IC50 value of 10.1μM.
  24. BT2

    BCKDC kinase (BDK) inhibitor

    BT2 is a BCKDC kinase (BDK) inhibitor with an IC50 of 3.19 μM.
  25. myeloid cell leukemia 1 (MCL1) inhibitor

    S63845 is a potent and selective myeloid cell leukemia 1 (MCL1) inhibitor with a Kd of 0.19 nM for human MCL1.
  26. Mcl-1 inhibitor

    (R)-MIK665 is the less active enantiomer of MIK665. MIK665 is a special Mcl-1 inhibitor with an IC50 of 1.81 nM.
  27. MCL-1 inhibitor

    AMG-176 is a potent, selective and orally bioavailable MCL-1 inhibitor, with a Ki of 0.13 nM.
  28. BCL-2 inhibitor

    S55746 (BLC201) is a potent, orally active and selective BCL-2 inhibitor, with a Ki of 1.3 nM and a Kd of 3.9 nM. S55746 (BLC201) has antitumor activity with low toxicity.
  29. Mcl-1 inhibitor

    MIK665 (S-64315) is a special Mcl-1 inhibitor extracted from patent WO2016207225A1, compound Preparation 13, has an IC50 of 1.81 nM.
  30. MCL-1 Inhibitor

    VU661013 is a MCL-1 Inhibitor Combined with Venetoclax Rescues Venetoclax Resistant Acute Myelogenous Leukemia.
  31. Mcl-1/Bim interaction inhibitor

    ML311 is a potent and selective inhibitor of the Mcl-1/Bim interaction
  32. Thevetiaflavone could upregulate the expression of Bcl?2 and downregulate that of Bax and caspase?3.
  33. Mcl-1 inhibitor

    Mcl1-IN-2 is a selective Mcl-1 inhibitor.
  34. Mcl-1 inhibitor

    Mcl1-IN-1 is a potent and selective inhibitor of the apoptosis regulating proteins Mcl-1.
  35. Mcl-1-PUMA interface inhibitor

    Mcl1-IN-8 (Comp8) is a Mcl-1-PUMA interface inhibitor, with a Ki of 0.3 μM. Mcl1-IN-8 (Comp8) exhibits dual activity on reduce PUMA-dependent apoptosis while deactivating Mcl-1-mediated anti-apoptosis in cancer cells.
  36. Mcl-1 Inhibitor

    Mcl1-IN-9 is a potent myeloid cell leukemia-1 (Mcl-1) Inhibitor with an IC50 of 446 nM in reengineered BCR-ABL+ B-ALL cells and a Ki of 0.03 nM.
  37. Mcl-1 inhibitor

    PROTAC Mcl1 degrader-1 (compound C3), a proteolysis targeting chimera (PROTAC), is a potently and selectively Mcl-1 inhibitor with an IC50 of 0.78 μM.
  38. NPB

    BAD phosphorylat inhibitor

    NPB is a specific and potent inhibitor of BAD phosphorylation at Ser99, with an IC50 of 0.41 μM.
  39. Mcl-1 antagonist 1

    Mcl-1 antagonist 1 is a Mcl-1 protein antagonist extracted from patent WO2019173181, compound 200.
  40. Androstane receptor agonist

    TCPOBOP is an agonist of the constitutive androstane receptor (CAR) (EC50 = 20 nM). TCPOBOP enhances the nuclear receptor CAR transactivation of cytochrome P450 (CYP), as dose-dependent direct agonist of CAR.
  41. Mcl-1 inhibitor

    Mcl1-IN-11 (Compound G) is a selective Mcl-1 inhibitor, less potent at Bcl-2, with Kis of 0.06 and 4.2 μM, respectively.
  42. MCL-1/PROTAC degrader

    dMCL1-2 is a potent and selective degrader of myeloid cell leukemia 1 (MCL1) based on PROTAC, which binds to MCL1 with a KD of 30 nM. dMCL1-2 activats the cellular apoptosis machinery by degradation of MCL1.
  43. Mcl-1 inhibitor

    Mcl1-IN-12 (Compound F) is a selective Mcl-1 inhibitor, less potent at Bcl-2, with Kis of 0.29 and 3.1 μM, respectively. Anti-tumor activity.
  44. Mcl-1 and Bcl-2 dual inhibitor

    MCL-1/BCL-2-IN-4 (Compound 7) is a potent and selective Mcl-1 and Bcl-2 dual inhibitor.
  45. Bcl-2 Family activator

    (E)-Ferulic acid is a isomer of Ferulic acid which is an aromatic compound, abundant in plant cell walls. (E)-Ferulic acid shows a potent ability to remove reactive oxygen species (ROS) and inhibits lipid peroxidation. (E)-Ferulic acid exerts both anti-proliferation and anti-migration effects in the human lung cancer cell line H1299.
  46. antiarthritic drugs

    Dihydrokaempferol is isolated from Bauhinia championii (Benth). Dihydrokaempferol induces apoptosis and inhibits Bcl-2 and Bcl-xL expression. Dihydrokaempferol is a good candidate for new antiarthritic drugs.
  47. insecticidal and anticancer

    Destruxin B, isolated from entomopathogenic fungus Metarhizium anisopliae, is one of the cyclodepsipeptides with insecticidal and anticancer activities. Destruxin B induces apoptosis via a Bcl-2 Family-dependent mitochondrial pathway in human nonsmall cell lung cancer cells.
  48. Mcl-1 and Bcl-2 dual inhibitor

    MCL-1/BCL-2-IN-3 (Compound 2) is a potent and selective Mcl-1 and Bcl-2 dual inhibitor with IC50s of 5.95 and 4.78 μM, respectively.
  49. Mcl-1 inhibitor

    Mcl1-IN-4 is an inhibitor of Mcl1 with an IC50 of 0.2 μM.
  50. Bcl-2 and Bcl-xL inhibitor

    BM 957 is a potent Bcl-2 and Bcl-xL inhibitor, with Kis of 1.2, <1 nM and IC50s of 5.4, 6.0 nM respectively.

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