| DC59120 |
BTSA1.2
Featured
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BTSA1.2 is a rationalized BTSA1 analog with improved binding to BAX, cellular cytotoxicity, and better toleratence in vivo. Combination of BTSA1.2 with Navitoclax demonstrates synergistic efficacy in apoptosis-resistant cancer cells, xenografts, and patient-derived tumors while sparing healthy tissues. |
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| DC48386 |
ABBV-167 |
ABBV-167 is a phosphate prodrug of the BCL-2 inhibitor venetoclax. |
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| DC50162 |
Bcl-2/Mcl-1-IN-3 |
Bcl-2/Mcl-1-IN-3 (compound 1) is a Bcl-2/Mcl-1 inhibitor, with Kis of 0.14 μM and 0.23 μM for Mcl-1 and Bcl-2, respectively. Bcl-2/Mcl-1-IN-3 can be used for the research of cancer. |
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| DC50163 |
Mcl-1 inhibitor 7 |
Mcl-1 inhibitor 7 is a potent Mcl-1 inhibitor, example 35, extracted from patent WO2020097577A. |
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| DC50164 |
Bcl-2/Mcl-1-IN-2 |
Bcl-2/Mcl-1-IN-2 (compound 2) is a Bcl-2/Mcl-1 inhibitor, with Kis of 0.88 μM and 4.70 μM for Mcl-1 and Bcl-2, respectively. Bcl-2/Mcl-1-IN-2 can be used for the research of cancer. |
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| DC50165 |
Bcl-2/Mcl-1-IN-1 |
Bcl-2/Mcl-1-IN-1 (compound 3) is a Bcl-2/Mcl-1 inhibitor, with Kis of 1.19 μM and 4.53 μM for Mcl-1 and Bcl-2, respectively. Bcl-2/Mcl-1-IN-1 can be used for the research of cancer. |
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| DC50166 |
Bim-IN-1
Featured
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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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| DC70122 |
BTC-8 |
A derivative of BAM-7 that acts as a nove potent, direct activator of Bax with EC50 of 700 nM; inhibits GBM cell proliferation, arrests the cell cycle, and induces apoptosis through the induction of mitochondrial membrane permeabilization; also blocks proliferation and self-renewal of GSCs and induces their apoptosis; sensitizes both GBM cells and GSCs to the alkylating agent Temozolomide. |
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| DC70246 |
BFL-1 inhibitor 4E14
Featured
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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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| DC70294 |
CCT369347 |
CCT369347 (CCT-369347) is potent selective inhibitor of BCL-6 with TR-FRET IC50 of 26 nM.CCT369347 demonstrated antiproliferative activity in a panel of BCL6-positive lymphoma cell lines (OCI-Ly1, SU-DHL-4, and SU-DHL-6) with IC50 of 1.68-3.45 uM, with weaker activity against low BCL6 expression cells and noncytotoxocity. CCT369347 inhibits BCL6 in a cellular assay with a submicromolar IC50 and shows promising early PK. |
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| DC70365 |
D-NA-NOXA SAHB-15 R31E |
D-NA-NOXA SAHB-15 R31E is a peptidic, functionally selective and cell-permeable BFL-1/A1 inhibitor that is specifically cytotoxic to BFL-1/A1-dependent human cancer cells. |
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| DC70933 |
ZH07 |
ZH07 (Dual Mcl-1/Bfl-1 inhibitor 24) is a potent, selective dual Mcl-1 and Bfl-1 inhibitor, binds both Mcl-1 and Bfl-1 with Ki of 97 nM and 100 nM, respectively.ZH07 displays appreciable selectivity (>250-fold) over Bcl-2/Bcl-xL.ZH07 induces dose-dependent disruption of interactions between BL-Bim and endogenous Mcl-1 and Bfl-1, without affecting the complexes between BL-Bim and Bcl-2 or Bcl-xL.ZH07 demonstrates on-target cellular activity in model lymphoma cell lines. |
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| DC70934 |
ZH97
Featured
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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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| DC71076 |
M24 |
M24 is a Mcl-1 selective inhibitor. M24 exhibits good binding affinity against Mcl-1 with Ki value of 0.33 μM. M24 exhibits good anti-proliferative activity and induce apoptosis in HepG2 cells. |
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| DC71702 |
BM-1074 |
BM-1074 is a potent and specific Bcl-2/Bcl-xL inhibitor with Ki values of < 1 nM and IC50 values of 1.8 nM and 6.9 nM for Bcl-2 and Bcl-xL, respectively. BM-1074 induces apoptosis, and exhibits antiproliferative activity against four small-cell lung cancer cell lines (H146, H1963, H187 and H1417) with IC50 values of 1-2 nM. |
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| DC72108 |
UBX1325 |
UBX1325 is an Bcl-xL inhibitor that promotes apoptosis in senescent cells. UBX1325 is a potent anti-aging agent that can be used in studies of age-related eye diseases such as diabetic macular oedema (DME), age-related macular degeneration (AMD) and diabetic retinopathy (DR). |
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| DC72249 |
TMX-2164 |
TMX-2164 is a potent, irreversible B-cell lymphoma 6 (BCL6) inhibitor with an IC50 value of 152 nM. TMX-2164 displays sustained target engagement and antiproliferative activity in cells. |
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| DC72522 |
CYD-4-61 |
CYD-4-61 is a novel Bax activator used for breast cancer research. CYD-4-61 inhibits triple-negative breast cancer MDA-MB-231 and ER-positive breast cancer MCF-7 cell lines proliferation. CYD-4-61 activates Bax protein to induce cytochrome c release and regulate apoptotic biomarkers, leading to cancer cell apoptosis. |
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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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| 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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| 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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| 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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| 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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| 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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| 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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| DC73097 |
CCT374705 |
CCT374705 is a potent, selective, in-vivo active BCL6 inhibitor with TR-FRET IC50 of 6 nM. |
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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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| 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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| 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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| 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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