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Epigenetic Reader Domain
货号 | 产品名 | CAS号 | 信息 |
---|---|---|---|
CSN20473 | UNC926 | 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. |
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 | 2-(4-(2-Hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one | 1044870-39-4 | RVX-208 is an inhibitor of BET bromodomain BD2 with IC50 of 0.510 μM. |
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. |
CSN19071 | PF-CBP1 HCl | 2070014-93-4 | PF-CBP1 HCl is a highly selective inhibitor of the bromodomain of CREB-binding protein (CREBBP).It inhibits CREBBP and p300 bromodomains with IC50 of 125 and 363 nM respectively. |
CSN13739 | Birabresib | 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. |
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. |
CSN13840 | I-CBP112 | 1640282-31-0 | I-CBP112 is a specific and potent acetyl-lysine competitive protein-protein interaction inhibitor, that targets the CBP/p300 bromodomains. |
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-BET151 | 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 | Molibresib | 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 | GSK-5959 | 901245-65-6 | GSK5959 is a potent, selective and cell permeable BRPF1 bromodomain inhibitor with IC50 ~ 80 nM. |
CSN17637 | GSK 525768A | 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). |
CSN20172 | EML-631 | 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. |
CSN18854 | EED226 | 2083627-02-3 | EED226 is a potent and selective PRC2 inhibitor that directly binds to the H3K27me3 binding pocket of EED. |
CSN19072 | CPI-637 | 1884712-47-3 | CPI-637 is an efficient inhibitor of CBP/EP300 bromodomain with IC50 of 0.03 ± 0.01μM. |
CSN17768 | (S)-2-(6-(4-Chlorophenyl)-1-methyl-4H-benzo[c]isoxazolo[4,5-e]azepin-4-yl)acetamide | 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 | I-BET282 | 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 | (R)-4-(2-(4-(1-(3-Methoxy-[1,2,4]triazolo[4,3-b]pyridazin-6-yl)piperidin-4-yl)phenoxy)ethyl)-1,3-dimethylpiperazin-2-one | 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. |
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. |
CSN13913 | (R)-(-)-JQ1 Enantiomer | 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 | (S)-tert-Butyl 2-(4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)acetate | 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 | (S)-2-(4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)acetic 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. |