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Inhibitors
| Cat.No. | Name | Information |
|---|---|---|
| M9026 | AZD-5153 HNT salt | AZD-5153 HNT salt is a potent, selective and orally available BET/BRD4 bromodomain inhibitor, disrupts BRD4 with an IC50 of 1.7 nM. |
| M8931 | BI-7273 | BI-7273 is a potent and selective BRD9 inhibitor with IC50s of 19 nM and 117 nM for BRD9 and BRD7, respectively. |
| M6206 | ARV-825 | ARV-825 is a BRD4 Inhibitor based on PROTAC technology. ARV-825 shows affinity to BD1 and BD2 of BRD4 with Kds of 90 and 28 nM, respectively. |
| M6118 | 666-15 | 666-15 is a potent and selective CREB inhibitor with an IC50 of 81 nM. |
| M6096 | JQ-1 carboxylic acid | (+)-JQ1 carboxylic acid is the carboxylic acid form of (+)-JQ1 for derivative synthesis. |
| M6083 | AZD9496 | AZD9496 is an oral estrogen receptor inhibitor that blocks the growth of ER-positive and ESR1 mutant breast tumours in preclinical models. |
| M5271 | GSK6853 | GSK6853 is a selective benzimidazolone BRPF1 inhibitor with pIC50 of 8.1(TR-FRET) showing greater than 1600-fold selectivity over all other bromodomains tested. |
| M5258 | Mivebresib | Mivebresib(ABBV-075) is a novel BET family bromodomain inhibitor. It binds bromodomains of BRD2/4/T with similar affinities (Ki of 1-2.2 nM) and highly selective for 18 bromodomain proteins tested (Kd > 1 μM; more than 600-fold selectivity vs. BRD4) |
| M5064 | PFI 4 | PFI-4 is a potent and selective BRPF1 bromodomain inhibitor with IC50 of 80 nM. |
| M4909 | GSK2801 | GSK2801 is a selective bromodomains BAZ2A/B inhibitor with KD of 257 nM and 136 nM, respectively. |
| M3526 | CPI-203 | CPI-203 is a novel potent, selective BET bromodomain inhibitor with IC50 of 37 nM for BRD4. |
| M2932 | PFI-1 | PFI-1 is a selective BET (bromodomain-containing protein) inhibitor for BRD4 with IC50 of 0.22 μM. |
| M2903 | OTX015 | OTX015 is a potent BET bromodomain inhibitor with EC50 ranging from 10 to 19 nM for BRD2, BRD3, and BRD4. |
| M2219 | RVX-208 | RVX-208 is a first-in-class, small molecule inhibitor of BET bromodomain with IC50 of 0.51 μM for BD2. |
| M2202 | CPI-0610 | CPI-0610 is a novel BET protein bromodomain inhibitor. |
| M2190 | I-BET-762 | I-BET-762 (GSK525762) is a selective small molecule BET inhibitor. |
| M2167 | (+)-JQ1 | (+)-JQ1 is a potent, high affinity, selective BET bromodomain inhibitor. |
| 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. |
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