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Epigenetic Reader Domain

Epigenetic Reader Domain

Cat. No. Product Name CAS No. Information
CSN22303 ZXH-3-26 N/A ZXH-3-26 is a BRD4 heterobifunctional small-molecule ligand PROTAC shows activity exclusively on the BRD4 BD1 DC505h5 nM and spares degradation of BRD2 or BRD3 in cellular degradation assays ZXH-3-26 represents the first small molecule to allow pharmacologic targeting of BRD4 without significant inhibition or degradation of BRD2 and BRD3
CSN20473 UNC 926   1184136-10-4 UNC 926 hydrochloride binds to MBT domain of L3MBTL protein Kd 39 M and block the interaction with methylated lysine on histone 4 H4K20
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.
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.
CSN13852 PFI-4   900305-37-5 PFI-4 selectively inhibits BRPF1 bromodomain with IC50 of 80 nM
CSN17164 PFI-1 1403764-72-6 PFI-1 is a highly selective BET bromodomain-containing protein inhibitor for BRD4 with IC50 of 022 M and for BRD2 with IC50 of 98 nM in a cell-free assay
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.
CSN16354 OF-1 919973-83-4 OF-1 is an inhibitor of the proteins BRPF1B Kd 100 nM and BRPF2 Kd 500 nM bromodomain
CSN20525 NI-57 1883548-89-7 NI-57 is an orally active pan-BRPF chemical probe of the bromodomain BRD of the BRPFs
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
CSN21386 L-45 2079885-05-3 L-45 is the first potent selective and cell-active p300CBP-associated factor PCAF bromodomain Brd inhibitor with a Kd of 12615 nM
CSN22252 KG-501   18228-17-6 KG-501 is histochemical substrate of alkaline phosphatases and can inhibit CREB-CBP interaction
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
CSN17207 I-BRD9   1714146-59-4 I-BRD9 is a BRD9 bromodomain inhibitor with pIC50 value of 73 and pKd of 87 BRD9 fuctions as part of the SWISNF complex in chromatin remolding
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.
CSN18953 GSK6853 1910124-24-1 GSK6853 selectively inhibits the BRPF1 bromodomain with the pKd value of 95
CSN16355 GSK5959 901245-65-6 GSK5959 is a potent selective and cell permeable BRPF1 bromodomain inhibitor with IC50 80 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
CSN20172 EML631 2101206-36-2 EML631 interacts with the Tudor-domain-containing protein Spindlin1 SPIN1 blocking its ability to read H3K4me3 marks and inhibit its transcriptional-coactivator activity
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
CSN22301 dBET23 1957234-83-1 dBET23 is a BRD4 heterobifunctional small-molecule ligand PROTAC exhibits significant and selective degradation of BRD4 BD1 DC505h50 nM in cellular degradation assays
CSN19072 CPI-637 1884712-47-3 CPI-637 is an efficient inhibitor of CBPEP300 bromodomain with IC50 of 003 001M
CSN17768 CPI-0610 1380087-89-7 CPI-0610 is an inhibitor of BET bromodomains BRD2 BRD3 BRD4 and BRDT via binding to the acetylated lysine recognition motifs
CSN16219 CPI-203   1446144-04-2 CPI 203 is a potent selective and cell permeable inhibitor of the bromodomain and extra terminal BET family protein BRD4 with an IC50 of 37 nM BRD4 -screen assay
CSN19752 CD161 1627716-22-6 CD161 is a potent selective and orally active BET inhibitor
CSN18952 BI-9564 1883429-22-8 BI-9564 is an inhibitor of BRD9 IC50 75 nM and BRD7 IC50 34 M
CSN18673 BI-7273 1883429-21-7 BI-7273 is a potent selective and cell-permeable BRD9 BD Inhibitor
CSN17831 BET-IN-1 1422554-34-4 BET-IN-1 is a bromodomain inhibitor with a plC50 in the range 60 - 70
CSN18957 BET-BAY 002 S-Enantiomer 2070009-49-1 BET-BAY 002 S-enantiomer is the S-enantiomer of BET-BAY 002
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
CSN20607 AZD5153 6-Hydroxy-2-Naphthoic Acid 1869912-40-2 AZD5153 is an inhibitor of BETBRD4 bromodomain the IC50 for BRD4 is 17 nM
CSN19702 AZD5153 1869912-39-9 AZD5153 exhibits excellent pharmacokinetic profile and high potency in vitro and in vivo effecting c-Myc downregulation and tumor growth inhibition in xenograft studies
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.
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 cell-permeable inhibitor of cAMP-response element binding protein (CREB) with efficacious anti-cancer activity both in vitro and in vivo.
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.
CSN21058 PLX51107 1627929-55-8
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