| 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 | GSK1210151A | GSK1210151A (I-BET151) 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. |
| M25521 | OXFBD04 | OXFBD04 is a potent and selective BRD4 inhibitor with an IC50 of 166 nM. OXFBD04 is a potent BET bromodomain ligand with additional modest affinity for the CREBBP bromodomain. OXFBD04 has anti-cancer activity. |
| M25515 | GSK 4027 | GSK 4027 is a chemical probe for the PCAF/GCN5 bromodomain with an pIC50 of 7.4±0.11 for PCAF in a time-resolved fluorescence resonance energy transfer (TR-FRET) assay. |
| M25514 | GNE-272 | GNE-272 is a potent and selective CBP/EP300 inhibitor with IC50 values of 0.02, 0.03 and 13 μM for CBP, EP300 and BRD4, respectively. GNE-272 is also a selective in vivo probe for CBP/EP300. |
| M25513 | GNE-207 | GNE-207 is a potent, selective and orally bioavailable inhibitor of the bromodomain of CBP, with an IC50 of 1 nM, exhibits a selectively index of >2500-fold against BRD4(1). GNE-207 shows excellent CBP potency, with an EC50 of 18 nM for MYC expression in MV-4-11 cells. |
| M25506 | DC-CPin711 | DC-CPin711 is a potent and selective inhibitor of CREB-binding protein (CBP) bromodomain with an IC50 of 0.0626 μM. DC-CPin711 arrests cell cycle at G1 phase and induces apoptosis. |
| M25394 | BPTF-IN-1 | BPTF-IN-1 (compound AU1) is a selective bromodomain and PHD finger containing transcription factor (BPTF) bromodomain inhibitor with a Kd of 2.8 μM. BPTF-IN-1 shows to be selective for BPTF over BRD4 bromodomain. |
| M21322 | GNE-064 | GNE-064 is an orally administered brominated structural inhibitor of SMARCA2/4 and PBRM1 and is being developed as a tool compound.GNE-064 inhibits SMARCA4 with an IC50 value of 0.035 μM and also SMARCA2 with an EC50 value of 0.10 μM. |
| M21277 | GSK232 | GSK232 is a highly selective inhibitor of cell permeation of non-BET CECR2 brominated structures with >500-fold selectivity for BET family brominated structures. |
| M21182 | GSK852 | GSK852 is a very potent selective BET inhibitor of BD2 (pIC50 = 7.9). |
| 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. |
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