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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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