| 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).
|
|
| DCC-073 |
Gossypol-acetic acid |
>98%,Standard References |
|
| DC11613 |
Mcl1-IN-26 |
A novel potent, selective Mcl-1 inhibitor with IC50 of <3 nM in FRET assays. |
|
| DC9768 |
A1155463
Featured
|
A-1155463 is a highly potent and selective BCL-XL inhibitor. |
|
| DC8475 |
A-1210477
Featured
|
A-1210477 is a potent and selective MCL-1 inhibitor. |
|
| DC9296 |
A-1331852
Featured
|
A-1331852 is a high affinity BH3 mimetic Ligand of BCL protein BCL-XL. |
|
| 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. |
|
| 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. |
|
| DC1022 |
ABT-737
Featured
|
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. |
|
| DC2015 |
AT-101 (AT101) |
AT-101 is a BH3 mimetic known to be a potent inhibitor of antiapoptotic Bcl-2 family members. |
|
| DC9695 |
BH3I-1
Featured
|
BH3I-1 is a cell permeable BH3 mimetic that binds to Bcl-xL. BH3I-1 is an inhibitor of Bcl-xL. |
|
| DC10966 |
BRD1991 |
BRD1991 is a small molecule that selectively disrupt Beclin 1/Bcl-2 binding as compared to Bax/Bcl-2 and Bim/Bcl-2 binding and induces autophagic flux at concentrations with minimal cytotoxicity.. |
|
| 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). |
|
| DC9955 |
BCL6 inhibitor(CID5721353)
Featured
|
CID5721353 is a B-Cell Lymphoma 6 Inhibitor (BCL6 inhibitor). |
|
| DC10447 |
FX1
Featured
|
FX1 is a novel specific inhibitor of the B cell lymphoma 6 (BCL6). |
|
| DC10133 |
Gambogic Acid
Featured
|
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 μM, 1.21 μM, 2.02 μM, 0.66 μM, 1.06 μM and 0.79 μM, respectively. |
|
| DCAPI1148 |
Gossypol |
Gossypol |
|
| DC1066 |
HA14-1
Featured
|
HA14-1 is a nonpeptidic ligand of a Bcl-2 surface pocket with IC50 of~9 μM. |
|
| DC8264 |
MM-41 |
MM41 is a quadruplex-interactive compound which binds strongly to the quadruplexes encoded in the promoter sequences of the BCL-2 and k-RAS genes. |
|
| DC7217 |
Obatoclax (GX15-070)
Featured
|
Obatoclax (GX15-070) is 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). |
|
| DC7233 |
Pifithrin-u
Featured
|
Pifithrin-μ is a specific p53 inhibitor by reducing its affinity to Bcl-xL and Bcl-2, and also inhibits HSP70 function and autophagy. |
|
| DC8128 |
Pyridoclax(MR29072)
Featured
|
Pyridoclax(MR-29072) is a potent Mcl-1 inhibitor with Kd value of 25 nM. |
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|
| DC12279 |
S55746 hydrochloride (BLC201 (hydrochloride)) |
S55746 hydrochloride is a potent, orally active and selective BCL-2 inhibitor, with Kis and Kds of 1.3 nM, 520 nM and 3.9 nM, 186 nM for BCL-2 and BCL-XL, respectively. S55746 hydrochloride has antitumor activity. |
|
| DC12163 |
S55746 (BLC201)
Featured
|
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[1]. |
|
| DC10137 |
S63845
Featured
|
S63845 is a potent and selective myeloid cell leukemia 1 (MCL1) inhibitor; binds human MCL1 with a Kd of 0.19 nM. |
|
| DC8444 |
Sabutoclax
Featured
|
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. |
|
| DC10964 |
SW063058 |
SW063058 is a small molecule that selectively disrupt Beclin 1/Bcl-2 binding as compared to Bax/Bcl-2 and Bim/Bcl-2 binding and induces autophagic flux at concentrations with minimal cytotoxicity.. |
|
| DC10965 |
SW076956
Featured
|
SW076956 is a small molecule that selectively disrupt Beclin 1/Bcl-2 binding as compared to Bax/Bcl-2 and Bim/Bcl-2 binding and induces autophagic flux at concentrations with minimal cytotoxicity. |
|
| 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. |
|
| 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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