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Epigenetic Reader Domain

Epigenetic Reader Domain

货号 产品名 CAS号 信息
CSN20473 UNC 926 1184136-10-4 UNC 926 hydrochloride binds to MBT domain of L3MBTL protein (Kd = 3.9 µM) and block the interaction with methylated lysine on histone 4, H4K20.
CSN16356 SGC-CBP30   1613695-14-9 SGC-CBP30 is a potent CREBBP/EP300 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 μM.
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 0.22 μM 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 - 2.2 nM.
CSN18854 MAK683 2083627-02-3 MAK683 is an inhibitor of embryonic ectoderm development protein (EED) and also can inhibit polycomb repressive complex 2 (PRC2) allosterically which selectively binds to the domain of EED that interacts with H3K27me3.
CSN21386 L-45 2079885-05-3 L-45 is the first potent, selective, and cell-active p300/CBP-associated factor (PCAF) bromodomain (Brd) inhibitor with a Kd of 126±15 nM.
CSN22252 KG-501 18228-17-6 KG-501 is histochemical substrate of alkaline phosphatases and can inhibit CREB-CBP interaction.
CSN17207 I-BRD9 1714146-59-4 I-BRD9 is a BRD9 bromodomain inhibitor with pIC50 value of 7.3 and pKd of 8.7. BRD9 fuctions as part of the SWI/SNF 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 9.5.
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 CBP/EP300 (CBP IC50 = 0.02 μM, EP300 IC50 = 0.03 μM, BRET IC50 = 0.41 μM, BRD4(1) C50 = 13 μM).
CSN21184 FL-411 2118944-88-8 FL-411 selectively inhibits BRD4 with an IC50 of 0.43 ± 0.09 μM.
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.
CSN19072 CPI-637 1884712-47-3 CPI-637 is an efficient inhibitor of CBP/EP300 bromodomain with IC50 of 0.03 ± 0.01μM.
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 α-screen assay).
CSN19752 CD161 1627716-22-6 CD161 is a potent, selective, and orally active BET inhibitor.
CSN15855 Bromosporine 1619994-69-2 Bromosporine inhibits various bromodomains including BRD2, BRD4, BRD9 and CECR2 with IC50s of 0.41 μM, 0.29 μM, 0.122 μM and 0.017 μM respectively.
CSN18952 BI-9564 1883429-22-8 BI-9564 is an inhibitor of BRD9 (IC50 = 75 nM) and BRD7 (IC50 = 3.4 µM).
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 6.0 - 7.0.
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 BET/BRD4 bromodomain, the IC50 for BRD4 is 1.7 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.
CSN21391 AT 1 2098836-45-2 AT1 is a highly selective Brd4 degrader with a modified VHL ligand retained binding to VHL (Kd = 330 nM).
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 MAK-683 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 cell-permeable inhibitor of cAMP-response element binding protein (CREB) with efficacious anti-cancer activity both in vitro and in vivo.
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.
CSN13058 (+)-JQ-1 1268524-70-4 (+)-JQ1 is a BET bromodomain inhibitor, with IC50 of 77 nM/33 nM for BRD4(1/2) 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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