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Epigenetic Reader Domain Epigenetic Reader Domain

Inhibitors

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.
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 FIC oral BAF chromosomal remodeling complex allosteric inhibitors (via BRG1 and BRM ATPase inhibition) can be used to study metastatic melanoma and advanced hematologic tumors.
M11032 Alobresib Alobresib (GS-5829) is a BET bromine domain inhibitor that can be used in the study of recurrent and drug-resistant overexpressed c-Myc uterine serous carcinoma.
M10908 ZL0420 ZL0420 is a potent and selective BET bromine domain 4 (BRD4) inhibitor of BRD4 BD1 and BRD4 BD2 IC50 27 nM and 32 nM, respectively.
M10862 MS645 MS645 is a BET bromodomains (BrD) inhibitor for K of BRD4-BD1/BD2i The value is 18.4 nM. MS645 spatially limits the divalent inhibition of BRD4 BrDs, resulting in sustained inhibition of BRD4 transcriptional activity in solid tumor cells.
M10849 LT052 LT052 is a highly selective BET BD1 inhibitor IC50 87.7 nM. LT052 exhibits nanomolar-grade inhibitory activity of BRD4 BD1 and is 138 times more selective than BRD4 BD2 (IC).50=12.130 μM)。 LT052 has anti-inflammatory activity and can be used in acute gouty arthritis studies.
M10828 GSK778 GSK778 (iBET-BD1) is a potent and selective inhibitor of the BD1 bromine domain of the BET protein,IC50 The values are 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1). GSK778 phenotyping the role of pan-BET inhibitors in cancer models.
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.
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.



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