DC9368 |
(S)-Gossypol (acetic acid) |
(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).
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DCC-073 |
Gossypol-acetic acid |
>98%,Standard References |
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DCS-114 |
Embelin |
>98%,Standard References |
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DC11708 |
Mitochonic Acid 35 |
A dual inhibitor of TNF-α and TGF-β1 by inhibiting IκB kinase phosphorylation and Smad3 phosphorylation. |
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DC11637 |
MPK-09 |
A highly potent, selective mutant p53 (R175H, R249S, R273H, R273C) reactivator. |
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DC11613 |
Mcl1-IN-26 |
A novel potent, selective Mcl-1 inhibitor with IC50 of <3 nM in FRET assays. |
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DC11852 |
CTX-1 |
A novel small molecule that overcomes HdmX-mediated p53 repression, binds directly to HdmX (Kd=450 nM) to prevent p53-HdmX complex formation. |
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DC11669 |
CB-002
Featured
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CB-002 is a novel small molecule that restores p53 function in mutant p53-expressing colorectal cancer cells without toxicity to normal human fibroblasts; increases expression of endogenous p53 target genes NOXA, DR5, and p21 and cell death; decreases the stability of mutant p53 in RXF393 cancer cells and an exogenously expressed R175H p53 mutant in HCT116 p53-null cells. |
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DC11865 |
DS-5272 |
A potent and orally active p53-MDM2 interaction inhibitor with IC50 of 2.4 nM. |
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DC11834 |
AM-6761 |
A potent MDM2-p53 interaction inhibitor with remarkable biochemical (HTRF IC50=0.1 nM), cellular potency (SJSA-1 EdU IC50=16 nM), and favorable pharmacokinetic properties. |
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DC11836 |
AM-8735 |
A potent MDM2-p53 interaction inhibitor with remarkable biochemical (HTRF IC50=0.4 nM), cellular potency (SJSA-1 EdU IC50=25 nM), and favorable pharmacokinetic properties. |
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DC11830 |
WK-298 |
A potent small molecule inhibitor that binds and disrupts the MDM2/MDMX-p53 interaction with IC50 of 0.19 uM and 19.7 uM, respectively.. |
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DC11837 |
RO-5963
Featured
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RO-5963 is an inhibitor of the interaction of both MDM2 and MDMX with p53. |
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DC11725 |
BI-0252 |
A potent, highly selective, orally active MDM2-p53 interaction inhibitor with IC50 of 4 nM. |
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DC11695 |
AT-IAP |
A potent, orally bioavailable, dual XIAP/cIAP1 inhibitor with EC50 of 5.1/0.32 nM, respectively. |
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DC11727 |
RO-2468 |
A potent, selective, and orally active p53-MDM2 antagonist with IC50 of 6 nM. |
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DC11728 |
RO-5353 |
A potent, selective, and orally active p53-MDM2 antagonist with IC50 of 7 nM. |
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DC11620 |
RIPK2-IN-8 |
A potent, selective, orally available RIPK2 inhibitor with IC50 of 3 nM. |
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DC11835 |
AM-8553 |
A potent, selective, orally bioavailable MDM2-p53 interaction inhibitor with HTRF IC50 of 1.1 nM, SJSA-1 EdU IC50 of 68 nM. |
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DC11833 |
TDP-665759 |
A small molecule inhibitor of HDM2-p53 interaction with FP IC50 of 0.7 uM. |
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DC11832 |
NU-8165 |
A small molecule inhibitor of MDM2-p53 protein-protein interaction with IC50 of 16 uM.. |
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DC11831 |
NU-8231 |
A small molecule inhibitor of MDM2-p53 protein-protein interaction with IC50 of 5.3 uM in ELISA assay. |
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DC9768 |
A1155463
Featured
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A-1155463 is a highly potent and selective BCL-XL inhibitor. |
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DC8475 |
A-1210477
Featured
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A-1210477 is a potent and selective MCL-1 inhibitor. |
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DC9296 |
A-1331852
Featured
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A-1331852 is a high affinity BH3 mimetic Ligand of BCL protein BCL-XL. |
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DC2002 |
Venetoclax(ABT-199)
Featured
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Venetoclax (ABT-199; GDC-0199) is a highly selective, orally bioavailable small-molecule inhibitor of Bcl-2, exhibiting sub-nanomolar binding affinity with a Ki of less than 0.01 nM. This compound has been demonstrated to induce autophagy, highlighting its role in modulating programmed cell death pathways. In vitro studies reveal that Venetoclax exhibits potent cytotoxic activity against FL5.12-BCL-2 cells, with an EC50 of 4 nM, while showing markedly reduced efficacy against FL5.12-BCL-XL cells (EC50 = 261 nM), underscoring its selectivity for Bcl-2 over Bcl-XL.
The selectivity of Venetoclax is further corroborated in cellular mammalian two-hybrid assays, where it effectively disrupts BCL-2-BIM protein-protein interactions with an EC50 of 3 nM. In contrast, it demonstrates significantly weaker activity against BCL-XL-BCL-XS and MCL-1-NOXA complexes, with EC50 values of 2.2 μM, reinforcing its specificity for Bcl-2-dependent apoptotic regulation.
In vivo efficacy studies utilizing xenograft models derived from RS4;11 cells, a representative model of acute lymphoblastic leukemia (ALL), demonstrate that a single oral dose of Venetoclax (12.5 mg/kg) achieves a maximal tumor growth inhibition (TGImax) of 47% (P < 0.001) and a tumor growth delay (TGD) of 26% (P < 0.05). These results indicate robust anti-tumor activity in a Bcl-2-dependent malignancy. |
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DC4127 |
ABT-263 (Navitoclax)
Featured
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ABT-263 (Navitoclax) is a potent inhibitor of Bcl-xL, Bcl-2 and Bcl-w with Ki of ≤ 0.5 nM, ≤1 nM and ≤ 1 nM, respectively. |
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DC1022 |
ABT-737
Featured
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ABT-737 is a BH3 mimetic inhibitor of Bcl-xL, Bcl-2 and Bcl-w with EC50 of 78.7 nM, 30.3 nM and 197.8 nM, respectively. |
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DC9793 |
AMG232 |
AMG232 is a potent, selective and orally bioavailable inhibitor of MDM2−p53 interaction with IC50 value of 9.1 nM in EdU cells . |
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DC6311 |
Pomalidomide
Featured
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An inhibitor of LPS-induced TNFαrelease.Pomalidomide is thalidomide derivative that displays inhibition of LPS-induced TNFα release. Shows immunomodulator and anticancer effects. |
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