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Home > Inhibitors & Agonists > Apoptosis > Bcl-2

Bcl-2

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Cat. No. Product Name Field of Application Chemical Structure
DC2002 Venetoclax(ABT-199) Featured
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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DC70934 ZH97 Featured
ZH97 is a selective and covalent small-molecule inhibitor of BFL-1 protein with binding Ki of 0.41 uM, >200-fold selectivity over MCL-1.ZH97 does not bind to BCL-xL, BCL-2, TEAD2, TEAD4, MDM2, MDMX, BRD2 BD1, BRD2 BD2, BRD3 BD1, BRD3 BD2, BCL9, PD1/PD-L1 (Ki>400 uM).ZH97 modifies BFL-1 at the C55 residue, blocks BFL-1/BID interaction in vitro.ZH97 dose-dependently increased cytoplasmic cytochrome c level in U937 cells, has cell growth inhibition with IC50 of 2.8 uM, 5.5 uM, 7.7 uM, 6.8 uM, and 3.9 uM in U937, Kasumi-1, K562, MM.1S, and MV4-11 cell lines, respectively.ZH97 inhibits BFL-1/PUMA interaction in cell lysate and is effective in cancer cells that harboring highexpression level of BFL-1.
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DC4127 ABT-263 (Navitoclax) Featured
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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DC9768 A1155463 Featured
A-1155463 is a highly potent and selective BCL-XL inhibitor.
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DC74626 Lacutoclax
Lacutoclax is a Bcl-2 inhibitor with antineoplastic activity.
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DC73109 WK500B
WK500B is an orally available small molecule BCL6 inhibitor with IC50 of 1.39 uM (HTFR), exhibits potent efficacy against DLBCL in vitro and in vivo.
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DC73108 WK499
WK499 (WK-499) is a small molecule inhibitor of BCL6 with IC50 of 11.7 nM in HTRF assay, directly binds to BCL6 BTB (SPR KD=148 nM), inhibits the BCL6-mediated transcriptional repression activity.
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DC73107 WK369
WK369 (WK-369) is a specific small molecule inhibitor of BCL6, directly binds to the BCL6-BTB domain (SPR KD=2.24 uM) and blocks the interaction between BCL6 and SMRT with IC50 of 0.32 uM in HTRF assays.
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DC73106 Sonrotoclax
Sonrotoclax (BGB-11417) is a potent, selective and second-generation BCL2 inhibitor with IC50 of 0.014 nM and SPR KD value of 0.046 nM, overcomes BCL2 G101V mutation-induced venetoclax resistance.
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DC73105 OICR12694
OICR12694 (OICR 12694, JNJ-65234637) is a potent, selective, and orally bioavailable BCL6-BTB inhibitor with SPR KD value of 5 nM.
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DC73104 Obatoclax
A potent inhibitor of Bcl-2 family with IC50s of 1-7 uM for Bcl-2, Bcl-XL, Bcl-w, Bcl-B, Mcl-1 and Bfl-1.
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DC73103 MI-238
MI-238 (MI 238) is a potent and specific Mcl-1 inhibitor with Ki of 0.45 uM to human Mcl-1 protein in FP assays, disrupts the association of Mcl-1 with BH3-only proteins.
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DC73102 M109S
M109S is a small molecule protecting cells from mitochondria-dependent apoptosis wtih EC50 of 23.4 nM in iBax cells, directly interacts with Bax (Kd=153 nM, MST assay) and inhibits Bax activation.
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DC73101 GSK137
GSK137 is a potent, small-molecule BCL6 inhibitor binding to BCL6 BTB-POZ domain, displaces peptides derived from the human SMRT co-repressor from the BCL6 BTB-POZ domain in a TR-FRET assay with a pIC50 of 8.0.
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DC73100 DC-B01
DC-B01 is a novel small molecule BCL-2 inhibitor that binds to the BH4 domain with KD of 2.16 uM, disrupts the BCL-2/c-Myc interaction and consequently suppresses the transcriptional activity of c-Myc.
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DC73099 CGDF-190-20
CGDF-190-20 is a selective small molecule inhibitor of anti-apoptotic protein BCL2A1/Bfl-1 with IC50 of 365 nM in FP assays.
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DC73098 CGDF-183-20
CGDF-183-20 is a selective small molecule inhibitor of anti-apoptotic protein BCL2A1/Bfl-1 with IC50 of 264 nM in FP assays.
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DC73097 CCT374705
CCT374705 is a potent, selective, in-vivo active BCL6 inhibitor with TR-FRET IC50 of 6 nM.
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DC73094 CCT372064
CCT372064 is a potent, ligand-efficient inhibitor of BCL6 with IC50 of 3.9 nM and 12 nM in TR-FRET and cellular NanoBRET assays, respectively.
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DC73093 BI-5273
BI-5273 is a negative control compound of BI-3802 and BI-3812, which are potent and efficacious BCL6 degrader and inhibitor, respectively.
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DC73092 BDM53787
BDM53787 is a selective small molecule inhibitor of anti-apoptotic protein BCL2A1/Bfl-1 with IC50 of 0.8 uM (inhibition FITC–Bim BH3 binding to Bfl-1).
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DC73091 BDM49234
BDM49234 is a selective small molecule inhibitor of anti-apoptotic protein BCL2A1/Bfl-1 with IC50 of 6.3 uM (inhibition FITC–Bim BH3 binding to Bfl-1).
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DC73090 BDM44931
BDM44931 is a small molecule inhibitor of anti-apoptotic protein BCL2A1/Bfl-1 with IC50 of 1.3 uM.
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DC73089 BDM44898
BDM44898 is a small molecule inhibitor of anti-apoptotic protein BCL2A1/Bfl-1 with IC50 of 1.6 uM.
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DC73088 BAU-243
BAU-243 (BAU243) is a novel BH3 mimetic Bcl-2 inhibitor with a high affinity, effectively reduces overall GBM cell proliferation including a subpopulation of cancer-initiating cells.
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DC11219 BXI-72 Featured
BXI-72 (NSC334072) is a potent, selective small molecule Bcl-XL inhibitor that targets the BH3 domain of Bcl-XL (Kd=0.9 nM).
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DC50166 Bim-IN-1 Featured
Bim-IN-1 is a potent Bim expression inhibitor. Bim-IN-1 reduces Bim expression levels and has little inhibitory effect upon protein kinase A activity and minimal toxicity.
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DC70246 BFL-1 inhibitor 4E14 Featured
BFL-1 inhibitor 4E14 (4E14) is a potent, selective, covalent BFL-1 inhibitor that disrupt BH3-binding activity with IC50 of 1.3 uM, targets a unique C55 residue in the BFL-1 groove.4E14 blocks BFL-1 suppression of BAX-mediated mitochondrial apoptosis.
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DC7950 UMI-77 Featured
UMI-77 is a selective Mcl-1 inhibitor with Ki of 490 nM, showing selectivity over other members of Bcl-2 family.
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DC5005 tw-37 Featured
TW-37 is a novel nonpeptide inhibitor to recombinant Bcl-2, Bcl-xL and Mcl-1 with Ki of 0.29 μM, 1.11 μM and 0.26 μM, respectively.
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