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Inhibitors
| Cat.No. | Name | Information |
|---|---|---|
| M9515 | MS417 | MS417 (also known as GTPL7512) is a potent and selective BRD4 inhibitor, which binds to BRD4-BD1 and BRD4-BD2 with IC50s of 30 and 46 nM, respectively. |
| M9471 | FL-411 | FL-411 is a selective BRD4 inhibitor. |
| M9396 | A1874 | A1874 is a BRD4-degrading PROTAC which inhibits many cancer cell lines proliferation, with DC50 of 32 nM (induce BRD4 degradation in cells). |
| M9238 | dBET6 | dBET6 is a highly potent, selective and cell-permeable degrader of BET with an IC50 of 14 nM. |
| M9237 | dBET1 | dBET1 is a potent BRD4 protein degrader with an EC50 of 430 nM. |
| M9218 | ABBV-744 | ABBV-744 is a BDII-selective BET bromodomain inhibitor that is used in the research of AML and metastic castration-resistant prostate cancer. |
| M9152 | CPI-637 | CPI-637 is a potent and selective CBP/EP300 bromodomains inhibitor with IC50 of 0.03±0.01μM and 11.0±0.6 μM for CBP/EP300 and BRD4, respectively. |
| M9146 | GSK1324726A | GSK1324726A (I-BET726) is a highly selective inhibitor of BET family proteins with IC50 of 41 nM, 31 nM, and 22 nM for BRD2, BRD3, and BRD4, respectively. |
| M9144 | PFI-3 | PFI-3 is a selective chemical probe for SMARCA bromodomains, including SMARCA2, SMARCA4 and PB1(5) bromodomains with a Kd of 89 nM. |
| M9141 | SGC-CBP30 | SGC-CBP30 is a potent CREBBP/EP300 inhibitor with IC50 of 21 nM and 38 nM in cell-free assays, respectively. |
| M9105 | ARV-771 | ARV-771 is a small-molecule pan-BET degrader with Kd values of 4.7, 7.6, 7.6 nM against BRD2, BRD3 and BRD4, respectively. |
| M9100 | PLX51107 | PLX51107 is a potent and selective BET inhibitor, with Kds of 1.6, 2.1, 1.7, and 5 nM for BD1 and 5.9, 6.2, 6.1, and 120 nM for BD2 of BRD2, BRD3, BRD4, and BRDT, respectively. |
| 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. |
| M3106 | UNC1215 | UNC1215 is a potent and selective MBT (malignant brain tumor) antagonist, which binds L3MBTL3 with IC50 of 40 nM and Kd of 120 nM, 50-fold selective versus other members of the human MBT family. |
| 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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