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Epigenetic Reader Domain

Epigenetic Reader Domain

Cat. No. Product Name CAS No. Information
CSN23787 YF-2 1311423-89-8 YF-2 is a highly selective and blood-brain-barrier permeable histone acetyltransferase activator, it acetylates H3 in the hippocampus.
CSN24058 Y06036 1832671-96-1 Y06036 is a potent and selective BET inhibitor with BRD4(1) bromodomain binding Kd value of 82 nM. It has antitumor activity and could be used for Potential Treatment of Castration-Resistant Prostate Cancer (CRPC).
CSN16089 UNC1079 1418741-86-2 UNC1079 is the piperidine analog of UNC1021, as a structurally similar but significantly less potent inhibitor for use as a negative control in cellular studies.
CSN20473 UNC 926   1184136-10-4 UNC 926 HCl binds to MBT domain of L3MBTL protein (Kd = 3.9 µM) and block the interaction with methylated lysine on histone 4, H4K20.
CSN22087 TPOP146 2018300-62-2 TPOP146 is a selective CBP/P300 benzoxazepine bromodomain inhibitor with Kd of 134 nM and 5.02 μM for CBP and BRD4.
CSN16356 SGC-CBP30   1613695-14-9 SGC-CBP30 is a potent CREBBPEP300 bromodomain inhibitor with IC50 of 21-69 and 38 nM for CREBBP and EP300 bromodomains respectively
CSN13057 RVX-208   1044870-39-4 RVX-208 is an inhibitor of BET bromodomain BD2 with IC50 of 0.510 M.
CSN13913 (-)-JQ-1 1268524-71-5 R---JQ1 enantiomer the stereoisomer-JQ1 showed no significant interaction with any bromodomain -JQ1 is an inhibitor for the BET which targets the BET bromodomain The R---JQ1 enantiomer stereoisomer has no appreciable affinity to BET bromodomains whereas S-enantiomer pure -JQ1 binds to BRD4 bromodomains 1 and 2 with Kd values of 50 and 90 nM respectively
CSN22516 Target Protein-binding Moiety 6 2097512-23-5 PROTAC BRD9-binding moiety 1 is a I-BRD9-based warhead ligand for conjugation reactions of PROTAC targeting on BRD9.
CSN23937 PROTAC BRD9 Degrader-1 2097971-01-0 PROTAC BRD9 Degrader-1 is a PROTAC targeting on BRD9, consist of a BRD9 bromodomain probe I-BRD9 as a warhead ligand and pomalidomide as the CRBN ligand.
CSN21389 BETd-260 2093388-62-4 PROTAC BET Degrader 23 is a highly potent and efficacious PROTAC targeting on BET with DC50 value of 30pM for degradation of BRD4 in RS4;11 leukemia cell line.
CSN21058 PLX51107 1627929-55-8 PLX51107 is a potent and selective BRD4 inhibitor or BET inhibitor with novel in vitro and in vivo pharmacologic properties that emulates or exceeds the efficacy of BCR signaling agents in preclinical models of CLL.
CSN13852 PFI-4   900305-37-5 PFI-4 selectively inhibits BRPF1 bromodomain with IC50 of 80 nM
CSN13739 OTX-015   202590-98-5 OTX-015 is a potent BET bromodomain inhibitor with EC50 ranging from 10 to 19 nM for BRD2, BRD3, and BRD4 in cell-free assays.
CSN20525 NI-57 1883548-89-7 NI-57 is an orally active pan-BRPF chemical probe of the bromodomain BRD of the BRPFs
CSN13300 Naringenin Triacetate 3682-04-0 Naringenin triacetate is a natural product isolated and purified from the fruits of Citrus aurantium L. with a better binding affinity with multiple crystal structures of first bromodomain BRD4 (BRD4 BD1) when compared with the known inhibitors.
CSN21379 MZP-55 2010159-48-3 MZP-55 is a VHL-based PROTAC targeting on BET with pDC50/Dmax (%) values of 8.1/95, 7.5/93, 7.7/92, −/26 for Brd4 short, Brd4 long, Brd3 and Brd2 in HeLa cells, consist of I-BET726 as a warhead ligand linked to VHL ligand VH032.
CSN21378 MZP-54 2010159-47-2 MZP-54 is a PROTAC targeting on BET, consist of a warhead I-BET726 (BET bromodomain inhibitor) linked to a VHL ligand VH032.
CSN17242 MS436 1395084-25-9 MS436, a diazobenzene-based small compound, is an inhibitor of BRD4 bromodomains with Ki values of 30-50 nM.
CSN18822 Mivebresib 1445993-26-9 Mivebresib also known as ABBV-075 is an inhibitor of bormodomain and extra terminal domain BET The Ki values of BRD2 BRD4 BRDT are 1 nM - 22 nM
CSN22252 KG-501   18228-17-6 KG-501 is histochemical substrate of alkaline phosphatases and can inhibit CREB-CBP interaction
CSN22925 INCB054329 1628607-64-6 INCB054329 is a potent and selective BET protein inhibitor that targets BD1 and BD2 of BRD2, BRD3 and BRD4.
CSN13840 I-CBP112 1640282-31-0 I-CBP112 is a specific and potent acetyl-lysine competitive protein-protein interaction inhibitor that targets the CBPp300 bromodomains
CSN13060 I-BET-151 1300031-49-5 I-BET-151 is a selective BET inhibitor for BRD2, BRD3 and BRD4 with IC50 of 0.5 μM, 0.25 μM, and 0.79 μM in cell-free assays, respectively.
CSN13061 I-BET-762 1260907-17-2 I-BET 762 is an inhibitor for BET proteins with IC50 of 35 nM.
CSN17637 GSK525768A 1260530-25-3 GSK525768A is the enantiomer compound of GSK 525762A, which is a potent small molecule inhibitor that disrupt the function of the BET family of bromodomains (Brd2, Brd3, and Brd4) and has NO activity towards BET.
CSN13657 GSK2801   1619994-68-1 GSK2801 inhibits BAZ2 family of bromodomain-containing proteins BAZ2A Kd 260 nM and BAZ2B Kd 140 nM IC50 9-350 nM
CSN16910 GSK1324726A   1300031-52-0 GSK1324726A is an inhibitor of BET proteins BRD2 BRD3 BRD4 with IC50 of 41 nM 31 nM and 22 nM respectively
CSN19674 GNE-272 1936428-93-1 GNE-272 is a potent and selective in Vivo Probe for the Bromodomains of CBPEP300 CBP IC50 002 M EP300 IC50 003 M BRET IC50 041 M BRD41 C50 13 M
CSN21184 FL-411 2118944-88-8 FL-411 selectively inhibits BRD4 with an IC50 of 043 009 M
CSN18854 EED226 2083627-02-3 EED226 is a potent and selective PRC2 inhibitor that directly binds to the H3K27me3 binding pocket of EED.
CSN22308 dBET 6 1950634-92-0 dBET6 is an optimized and highly cell-permeable chemical degrader of BET bromodomain proteins, based on PROTAC.
CSN22300 dBET57 1883863-52-2 dBET57 is a BRD4 heterobifunctional small-molecule ligand PROTAC exhibits significant and selective degradation of BRD4 BD1 DC505h500 nM but is inactive on BRD4 BD2
CSN24814 CPI-268456 1380087-86-4 CPI-268456 is a ligand of BRD4.
CSN20806 CeMMEC1 440662-09-9 CeMMEC1 is an N-methylisoquinolinone that inhibits the second bromodomain of TAF1 with Kd of 1.8 µM and IC50 of 0.9 µM.
CSN21391 AT 1 2098836-45-2 BRD4 degrader AT1 is a highly selective Brd4 degrader based on PROTAC technology, with a Kd of 44 nM for Brd4BD2 in cells.
CSN18673 BI-7273 1883429-21-7 BI-7273 is a potent selective and cell-permeable BRD9 BD Inhibitor
CSN22309 BETd-246 2140289-17-2 BETd-246 is a second-generation BET bromodomain inhibitor. It causes a dose-dependent depletion of BRD2, BRD3 and BRD4 in representative TNBC cell lines with 30-100 nM for 1 h or with 10-30 nM for 3 h incubation.
CSN17940 BET-BAY 002 1588521-78-1 BET-BAY 002 is a potent BET inhibitor and shows efficacy in a multiple myeloma model
CSN20265 BET Inhibitor C3 874594-37-3 BET inhibitor C3 is a BET bromodomain inhibitor of epigenetic regulatory proteins BrdT and Brd4
CSN24478 BET Bromodomain inhibitor 1505453-59-7 BET bromodomain inhibitor is a potent BET inhibitor extracted from patent WO/2015/153871A2, compound example 11.
CSN20607 AZD5153 6-Hydroxy-2-Naphthoic Acid 1869912-40-2 AZD5153 is an inhibitor of BETBRD4 bromodomain the IC50 for BRD4 is 17 nM
CSN21392 AT6 2098836-50-9 AT6 is a PROTAC targeting on Brd4.
CSN18046 ARV-825 1818885-28-7 ARV-825 is a PROTAC targeting on BRD4, consisting of a BRD4-ligand JQ-1 linked to a cereblon E3 ligase ligand Pomalidomide, with Kds values of 90nM and 28nM for affinity to BD1 and BD2.
CSN21253 EED inhibitor-1 1951408-58-4 An inhibitor of embryonic ectoderm development protein EED and allosteric inhibitor of polycomb repressive complex 2 PRC2 with potential antineoplastic activity
CSN21197 ABBV-744 2138861-99-9 ABBV-744 is an inhibitor of BDII-selective BET bromodomain that is being investigated to treat AML and metastic castration-resistant prostate cancer.
CSN24157 666-15 1433286-70-4 666-15 is a potent and selective CREB inhibitor with IC50 value of 81nM.
CSN13058 (+)-JQ-1   1268524-70-4 -JQ1 is a BET bromodomain inhibitor with IC50 of 77 nM33 nM for BRD412 in cell-free assays binding to all bromodomains of the BET family but not to bromodomains outside the BET family
CSN18086 JQ-1 Carboxylic Acid 202592-23-2 (+)-JQ1 carboxylic acid is a warhead ligand with a carboxylic acid functional group for conjugation reactions of PROTAC targeting on BET.
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