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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.
M21322 GNE-064 GNE-064 is an orally administered brominated structural inhibitor of SMARCA2/4 and PBRM1 and is being developed as a tool compound.GNE-064 inhibits SMARCA4 with an IC50 value of 0.035 μM and also SMARCA2 with an EC50 value of 0.10 μM.
M21277 GSK232 GSK232 is a highly selective inhibitor of cell permeation of non-BET CECR2 brominated structures with >500-fold selectivity for BET family brominated structures.
M21182 GSK852 GSK852 is a very potent selective BET inhibitor of BD2 (pIC50 = 7.9).
M21172 M-1121 The menin-MLL inhibitor M-1121 is a covalent protein-protein interaction inhibitor with oral activity that achieves complete and durable tumor regression.
M21109 Inobrodib Inobrodib (CCS1477) is an orally active, potent and selective p300/CBP inhibitor. inobrodib binds to p300 and CBP with Kd values of 1.3 and 1.7 nM and has a 170/130 fold selectivity compared to BRD4 with a Kd of 222 nM. ccs1477 acts by inhibiting CCS1477 acts by inhibiting the expression and function of androgen receptor (AR) and by inhibiting c-Myc.
M21107 NVS-BET-1 NVS-BET-1 is a BET bromodomain inhibitor that regulates keratinocyte plasticity.
M21106 E7386 E7386 is an orally active and selective inhibitor of β-catenin/CBP protein interactions and is a key node in the long-studied Wnt/β-catenin cancer pathway.
M21069 AZ13824374 AZ13824374 is an in vitro ATAD2 inhibitor with anti-proliferative activity against breast cancer. pIC50 of AZ13824374 against ATAD2 in the ATAD2 FRET and ATAD2 NanoBRET assays were 8.2 and 6.2, respectively.
M20798 CCS-1477(CBP-IN-1) CCS1477(CBP-IN-1, CBP/p300-IN-4)is a potent and selective inhibitor of p300/CBP bromodomain. CCS1477 works by inhibiting the expression and function of the androgen receptor (AR), as well as inhibiting c-Myc.
M20780 CC-90010 CC-90010 is a reversible, orally active and central nervous system-penetrant inhibitor of bromodomain and extra-terminal (BET) proteins. CC-90010 is applied in the study for advanced solid tumors.
M20742 Y06036 Y06036 (compound 6i) is a potent and selective inhibitor of BET with antitumor activity. Y06036 binds to the BRD4(1) bromodomain with Kd of 82 nM.
M20727 BI 894999 BI 894999 is a potent and selective BET inhibitor with IC50 of 5 nM and 41 nM for the binding of BRD4-BD1 and BRD4-BD2 to acetylated histones, respectively. BI 894999 is highly selective for BRD2/3/4 and BRDT (Kd of 0.49-1.6 nM), with at least a 200-fold selectivity vs. BRD4-BD1.
M20642 ZL0420 ZL0420 is a potent and selective BRD4 inhibitor with IC50 values of 27 nM against BRD4 BD1 and 32 nM against BRD4 BD2 respectively and good selectivity over that of the related BRD2 homolog.
M20613 PF-CBP1 HCl PF-CBP1 HCl is a highly selective inhibitor of the bromodomain of CREB-binding protein(CREBBP).It inhibits CREBBP and p300 bromodomains with IC50 of 125 and 363 nM respectively.
M20549 GSK 5959 GSK5959 is a potent and selective BRPF1 bromodomain inhibitor with an IC50 of 80 nM and exhibits >100-fold selectivity for BRPF1 over a panel of 35 other bromodomains, including BRPF2/3 and BET family bromodomains.
M13826 TPOP146 TPOP146 is a selective CBP/P300 benzoxazepine bromodomain inhibitor with Kd values of 134 nM and 5.02 μM for CBP and BRD4.
M13825 Molibresib besylate Molibresib besylate (GSK 525762C; I-BET 762 besylate) is a BET bromodomain inhibitor with IC50 of 32.5-42.5 nM.
M13824 L-Moses dihydrochloride L-Moses (L-45) dihydrochloride is the first potent, selective, and cell-active p300/CBP-associated factor (PCAF) bromodomain (Brd) inhibitor with a Kd of 126 nM.
M13823 L-Moses L-Moses (L-45) is the first potent, selective, and cell-active p300/CBP-associated factor (PCAF) bromodomain (Brd) inhibitor with a Kd of 126 nM.
M13822 INCB054329 INCB054329 is a potent BET inhibitor.



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