| 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. |
| M9141 | SGC-CBP30 | Sgc-cbp30 is a potent and highly selective CBP/ P300 bromine domain inhibitor (Kd of 21 nM and 32 nM against CBP and P300, respectively), which is 40 times more selective than BRD4 [BRD4(1)]. Sgc-cbp30 strongly reduces the secretion of IL-17A in Th17 cells and has anti-inflammatory effects. |
| 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. |
| M9043 | INCB057643 | INCB057643 is a novel BET inhibitor. |
| 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. |
| M8602 | BI-9564 | BI-9564 is a cell permeable, potent and specific inhibitor of BRD9 and BRD7. |
| M8567 | I-BRD9 | I-BRD9 is a selective cellular chemical probe for bromodomain-containing protein 9 (BRD9), thought to be a member of the chromatin remodelling SWI/SNF BAF complex, which plays a fundamental role in gene expression regulation. |
| M6487 | BAY 299 | BAY 299 is a potent and selective BRD1 and TAF1 inhibitor. |
| 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. |
| M6096 | JQ-1 carboxylic acid | (+)-JQ1 carboxylic acid, the carboxylic acid form of (+)-JQ1, is a potent BET bromodomain inhibitor for downregulating PD-L1 expression on the surface of tumor cells. JQ-1 carboxylic acid can be used as a precursor to synthesize PROTACs, which targets BET bromodomains. |
| M5295 | MI-538 | Mi-538 is an inhibitor of the interaction between MENin and MLL fusion protein with an IC50 value of 21 nM. |
| 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. PFI-4 (1.25 µM; 7 or 11 days) inhibits differentiation of human osteoclasts. |
| M4909 | GSK2801 | GSK2801 is a selective bromodomains BAZ2A/B inhibitor with KD of 257 nM and 136 nM, respectively. |
| M4818 | Bromosporine | Bromosporine is a broad spectrum inhibitor for bromodomains with IC50 of 0.41 μM, 0.29 μM, 0.122 μM and 0.017 μM for BRD2, BRD4, BRD9 and CECR2, respectively. |
| M3526 | CPI-203 | CPI-203 is a novel potent, selective BET bromodomain inhibitor with IC50 of 37 nM for BRD4. |
| M3157 | MS436 | MS436 is a diazobenzene-based small-molecule inhibitor for the BRD4 bromodomains with a Ki value of 30-50 nM. |
| M3109 | UNC669 | UNC669 is a potent and selective MBT (malignant brain tumor) inhibitor with IC50 of 6 μM for L3MBTL1, 5- and 11-fold selective over L3MBTL3 and L3MBTL4. |
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