| 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. |
| M13387 | Revumenib (SNDX-5613) | Revumenib (SNDX-5613) is a first-in-class, effective and selective Menin-MLL binding inhibitor with Ki of 0.15 nM. Revumenib (SNDX-5613) can be used to study MLL gene rearrangement in acute leukemia, including acute lymphoblastic leukemia (ALL) and acute myeloid leukemia (AML). |
| M13373 | MI-3454 | MI-3454 is a highly potent and selective inhibitor of Menin-MLL1 interaction with an IC50 of 0.51 nM. |
| M11463 | MI-3 | Mi-3 (Menin-mLL inhibitor 3) is an effective and high affinity menin-MLL inhibitor with IC50 value of 648 nM and Kd value of 201 nM. |
| M11416 | FHD-286 | FHD-286 is a BRG1/BRM ATPase inhibitor, which can be used in the study of BAF-related diseases. Fdd-286 is also the first SMARCA2/SMARCA4 dual inhibitor. It can be used in the study of metastatic melanoma and advanced hematologic tumors. |
| M10822 | GNE-781 | GNE-781 (compound 19) is a highly potent, orally active, selective bromodomain inhibitor against cyclic adenosine monophosphate response element binding protein (CBP). The IC50 value is 0.94 nM (in TR-FRET assay). GNE-781 also suppresses BRET and BRD4(1), with IC50s of 6.2 nM and 5100 nM, respectively. GNE-781 has antitumor activity. |
| M10760 | GSK620 | GSK620 is a potent orally active pan-BD2 inhibitor with good broad-spectrum selectivity, developability, and in vivo oral pharmacokinetics, and is highly selective against the BET-BD2 family protein, with a selectivity of more than 200 times that of all other BET bromodomains. GSK620 exhibits an anti-inflammatory phenotype in human whole blood. |
| M10759 | GSK046 | GSK046 (iBET-BD2) is an effective, selective and orally active inhibitor of the BD2 bromine domain of the BET protein,IC50 The values are 264 nM (BRD2 BD2), 98 nM (BRD3 BD2), 49 nM (BRD4 BD2), and 214 nM (BRDT BD2). GSK046 has immunomodulatory activity. |
| M10668 | BRM/BRG1 ATP Inhibitor-1 | BRM/BRG1 ATP Inhibitor-1 is an orally active inhibitor (IC50 below 5 nM) of Brahma Homolog (BRM)/SMARCA2 ATPase activity for the treatment of Brahma Related Gene 1 (BRG1)/SMARCA4-Mutant cancers. |
| M10645 | MS402 | MS402 is a novel BD1-selective BET BrD inhibitor, inhibiting primarily Th17 cell differentiation with a little or almost no effect on Th1 or Th2 and Treg cells. MS402 has Ki values of 77 nM, 718 nM, 110 nM, 200 nM, 83 nM, and 240 nM for BRD4(BD1), BRD4(BD2), BRD3(BD1), BRD3(BD2), BRD2(BD1) and BRD2(BD2), respectively. |
| M10489 | NEO2734 (EP31670) | NEO2734 (EP31670) is a novel, orally active and selective dual inhibitor of p300/CBP and BET bromodomain with IC50 of both <30 nM. |
| M10388 | (+)-JQ1 PA | (+)-JQ1 PA is a derivative of the Bromodomain and extra-terminal (BET) inhibitor JQ1 with IC50 of 10.4 nM. |
| M10182 | KG-501 | KG-501 is a cAMP response element-binding protein (CREB) inhibitor with IC50 of 6.89 μM. |
| M9754 | AZD5153 | AZD5153 is a potent bivalent triazolopyridazine based Bromodomain and Extraterminal (BET) Inhibitor, with IC50 value of 5 nM. |
| 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. |
| M9237 | dBET1 | dBET1 is a potent BRD4 protein degrader with an EC50 of 430 nM. dBET1 is a PROTAC that composes of (+)-JQ1 linked to NSC 527179 with a linker. |
| 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. |
| 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. |
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