| Cat.No. | Name | Information |
|---|---|---|
| M2167 | (+)-JQ1 | (+)-JQ1 is a BET bromodomain inhibitor that acts on BRD4(2) with an IC50 of 33 nM and binds to all bromodomain domains in the BET family, but not to bromodomain domains outside the BET family. JQ1 down-regulates CD47 expression through a C-MYC-mediated pathway, and JQ1 down-regulates CD47 expression through a C-MYC-mediated pathway. |
| M6118 | 666-15 | 666-15 is a potent and selective CREB inhibitor with an IC50 of 81 nM. |
| M2096 | I-BET151 | I-BET151 (GSK1210151A) is an inhibitor of the BET family with IC50 of 0.5 μM, 0.25 μM and 0.79 μM for BRD2, BRD3 and BRD4, respectively. |
| M2903 | OTX015 (Birabresib) | OTX015 is a potent BET bromodomain inhibitor with EC50 ranging from 10 to 19 nM for BRD2, BRD3, and BRD4. |
| M2190 | I-BET-762 | I-BET-762 (GSK525762) is a selective small molecule BET inhibitor. |
| M7126 | PF CBP1 | PF CBP1 is a selective CBP/p300 bromodomain inhibitor. |
| M9218 | ABBV-744 | ABBV-744 is a first-in-class, orally active and selective inhibitor of the BDII domain of the BET family of proteins with IC50 values of 4-18 nM for BRD2, BRD3, BRD4, and BRDT for AML and metastatic desmoplasia-resistant prostate cancer. |
| M21172 | M-1121 | M‑1121 is a covalent and orally active inhibitor of the menin-MLL interaction capable of achieving complete and persistent tumor regression. |
| M21107 | NVS-BET-1 | NVS-BET-1 is a BET bromodomain inhibitor that regulates keratinocyte plasticity. |
| M21069 | AZ13824374 | AZ13824374 is an in vitro ATAD2 inhibitor with anti-proliferative activity against breast cancer. pIC50 of AZ13824374 against ATAD2 in the ATAD2 FRET and ATAD2 NanoBRET assays were 8.2 and 6.2, respectively. |
| M20780 | CC-90010 | CC-90010 is a reversible, orally active and central nervous system-penetrant inhibitor of bromodomain and extra-terminal (BET) proteins. CC-90010 is applied in the study for advanced solid tumors. |
| M20742 | Y06036 | Y06036 (compound 6i) is a potent and selective inhibitor of BET with antitumor activity. Y06036 binds to the BRD4(1) bromodomain with Kd of 82 nM. |
| M20727 | BI 894999 | BI 894999 is a potent and selective BET inhibitor with IC50 of 5 nM and 41 nM for the binding of BRD4-BD1 and BRD4-BD2 to acetylated histones, respectively. BI 894999 is highly selective for BRD2/3/4 and BRDT (Kd of 0.49-1.6 nM), with at least a 200-fold selectivity vs. BRD4-BD1. |
| M20549 | GSK 5959 | GSK5959 is a potent and selective BRPF1 bromodomain inhibitor with an IC50 of 80 nM and exhibits >100-fold selectivity for BRPF1 over a panel of 35 other bromodomains, including BRPF2/3 and BET family bromodomains. |
| M13826 | TPOP146 | TPOP146 is a selective CBP/P300 benzoxazepine bromodomain inhibitor with Kd values of 134 nM and 5.02 μM for CBP and BRD4. |
| M13825 | Molibresib besylate | Molibresib besylate (GSK 525762C; I-BET 762 besylate) is a BET bromodomain inhibitor with IC50 of 32.5-42.5 nM. |
| M13824 | L-Moses dihydrochloride | L-Moses (L-45) dihydrochloride is the first potent, selective, and cell-active p300/CBP-associated factor (PCAF) bromodomain (Brd) inhibitor with a Kd of 126 nM. |
| M13823 | L-Moses | L-Moses (L-45) is the first potent, selective, and cell-active p300/CBP-associated factor (PCAF) bromodomain (Brd) inhibitor with a Kd of 126 nM. |
| M13822 | INCB054329 | INCB054329 is a potent BET inhibitor. |
| M13821 | HJB97 | HJB97 is a high-affinity BET inhibitor with Kis of 0.9 nM (BRD2 BD1), 0.27 nM (BRD2 BD2), 0.18 nM (BRD3 BD1), 0.21 nM (BRD3 BD2), 0.5 nM (BRD4 BD1), 1.0 nM (BRD4 BD2), respectively. |
| M13820 | GNE-049 | GNE-049 is a highly potent and selective CBP inhibitor with an IC50 of 1.1 nM in TR-FRET assay. GNE-049 also inhibits BRET and BRD4(1) with IC50s of 12 nM and 4200 nM, respectively. |
| M13429 | VTP50469 fumarate | VTP50469 fumarate is a Menin-MLL interaction inhibitor with a Ki of 104 pM. Effective against MLL rearrangement and NPM1c+ leukemia. It has effective anti-leukemia activity. |
| M11032 | Alobresib | Alobresib (GS-5829) is a BET bromine domain inhibitor that can be used in the study of recurrent and drug-resistant overexpressed c-Myc uterine serous carcinoma. |
| M10908 | ZL0420 | ZL0420 is a potent and selective BET bromine domain 4 (BRD4) inhibitor of BRD4 BD1 and BRD4 BD2 IC50 27 nM and 32 nM, respectively. |
| M10862 | MS645 | MS645 is a BET bromodomains (BrD) inhibitor for K of BRD4-BD1/BD2i The value is 18.4 nM. MS645 spatially limits the divalent inhibition of BRD4 BrDs, resulting in sustained inhibition of BRD4 transcriptional activity in solid tumor cells. |
| M10849 | LT052 | LT052 is a highly selective BET BD1 inhibitor with an IC50 of 87.7 nM. LT052 exhibits nanomolar BRD4 BD1 potency and 138-fold selectivity over BRD4 BD2 (IC50=12.130 μM). LT052 has anti-inflammatory activity and can be used for the research of acute gout arthritis. |
| M10828 | GSK778 | GSK778 (iBET-BD1) is a potent and selective inhibitor of the BD1 bromine domain of the BET protein,IC50 The values are 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1). GSK778 phenotyping the role of pan-BET inhibitors in cancer models. |
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