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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. |
| 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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