Histone Methyltransferase

Histone Methyltransferase
第页，共 4 页

货号	产品名	CAS号	信息
CSN17962	XY1	1624117-53-8	XY1 is a negative control of SGC 707 which works as a potent and selective allosteric inhibitor of PRMT3, while XY1 shows almost no activity.
CSN17252	WDR5-0103	890190-22-4	WDR5-0103 is a selective antagonist of WD repeat-containing protein 5 (WDR5) with Kd of 450 nM.
CSN16357	(5-Bromopyridin-3-yl)(4-(pyrrolidin-1-yl)piperidin-1-yl)methanone	1314241-44-5	UNC669 is a selective inhibitor of MBT (malignant brain tumor) with IC50 of 6 μM for L3MBTL1.
CSN18843	UNC3866	1872382-47-2	UNC3866 is a high-affinity CBX4 and CBX7 inhibitor with Ki values of 94 and 97 nM, respectively.
CSN17166	UNC1999	1431612-23-5	UNC1999 is a potent, orally bioavailable and selective inhibitor of EZH2 and EZH1 with IC50 of 2 nM and 45 nM, respectively.
CSN15916	UNC1215	1415800-43-9	UNC1215 is a chemical probe for the methyllysine (Kme) reader domain of L3MBTL3 with Kd of 120 nM.
CSN15901	UNC0646	1320288-17-2	UNC0646 is a potent and selective G9a inhibitor with IC50 of 6 nM.
CSN17894	UNC0642	1481677-78-4	UNC0642 is a selective inhibitor of G9a/GLP with IC50 of < 15 nM.
CSN16350	UNC0638	1255580-76-7	UNC0638 is an inhibitor of protein lysine methyltransferases G9a and GLP with IC50 of < 15 nM, 19 nM, respectively.
CSN17958	UNC0379 TFA	1620401-83-3	UNC0379 trifluoroacetate is a selective, substrate-competitive inhibitor of the lysine methyltransferase SETD8 with IC50 of 7.3±1.0 μM and is selective over 15 other methyltransferases.
CSN15846	UNC0379	1620401-82-2	UNC0379 is a selective inhibitor of the lysine methyltransferase SETD8 with IC50 of 7.3 ± 1.0 μM.
CSN17608	UNC0321	1238673-32-9	UNC0321 is a potent and selective G9a inhibitor with Ki of 63 pM, UNC0321 is the first G9a inhibitor with picomolar potency and the most potent G9a inhibitor to date.
CSN17546	UNC0224	1197196-48-7	UNC0224 is a selective inhibitor of G9a with IC50 of 15 nM.
CSN17278	UNC 0631	1320288-19-4	UNC 0631 is a potent G9a inhibitor with IC50 value of 4 nM.
CSN16351	SGC707	1687736-54-4	SGC707 is a chemical probe of PRMT3 with IC50 of 31 nM.
CSN18955	SGC2085	1821908-48-8	SGC2085 is a selectivel and potent CARM1 inhibitor with IC50 value of 50 nM.
CSN17931	SGC0946	1561178-17-3	SGC0946 is a selective inhibitor of DOT1L methyltransferase with IC50 of 0.3 nM and can kill mixed lineage leukaemia cells.
CSN17964	PFI-2	1627676-59-8	PFI-2 is an a first-in-class, potent, highly selective, and cell-active inhibitor of the methyltransferase activity of SETD7 with IC50 of 2 nM, 500 fold active than (S)-PFI-2.
CSN16349	PFI-2 HCl	1627607-87-7	PFI-2 HCl is an a first-in-class, potent, highly selective, and cell-active inhibitor of the methyltransferase activity of SETD7 with IC50 of 2 nM, 500 fold active than (S)-PFI-2.
CSN16359	OICR-9429	1801787-56-3	OICR-9429 is an antagonist of the interaction of WDR5 with peptide regions of MLL and Histone 3.
CSN18048	MS023	1831110-54-3	MS023 is a potent and selective chemical probe for Type I PRMTs with IC50 values of 30, 119, 83, 8, and 8 nM for PRMTs 1,3,4,6,and 8, respectively. MS023 is active in cells.
CSN18954	MS049	1502816-23-0	MS 049 is a potent, selective, and cell-active dual inhibitor of PRMT4 and PRMT6 with IC 50 of 34 nM and 43 nM respectively.
CSN18956	MM-102 TFA	1883545-52-5	MM-102 trifluoroacetate is a potent WDR5/mLL interaction inhibitor, achieves IC50 = 2.4 nM with an estimated Ki < 1 nM in WDR5 binding assay, which is > 200 times more potent than the ARA peptide.
CSN17822	MM-102	1417329-24-8	MM-102 is a high-affinity peptidomimetic MLL1 inhibitor with IC50 of 0.4 μM in a cell-free assay.
CSN13934	MI-503	1857417-13-0	MI-503 is a small molecule inhibitor of themenin-MLL interaction.
CSN17202	MI-463	1628317-18-9	MI-463 is an effective inhibitor of themenin-MLL interaction.
CSN17651	MI-3	1271738-59-0	MI-3 is a Menin-MLL interaction inhibitor with IC50 value of 648 ± 25 nM.
CSN17201	MI-136	1628316-74-4	MI-136 can selectively inhibit the interaction of menin and MLL. It also suppresses DHT-induced expression of androgen receptor (AR) target genes.
CSN18032	LLY-507	1793053-37-8	LLY-507 is a potent and selective protein-lysine methyltransferase SMYD2 inhibitor with IC50 <15 nM, which can inhibit p53K370 monomethylation in cells with an IC50 ~600 nM.
CSN17504	HLCL-61 HCl	1158279-20-9	HLCL-61 HCl is an inhibitor of PRMT5 that is used for the treatment of acute myeloid leukemia.
CSN17955	(S)-2-(Cyclobutylamino)-N-(3-(3,4-dihydroisoquinolin-2(1H)-yl)-2-hydroxypropyl)isonicotinamide	1616391-87-7	GSK591 is a potent and selective inhibitor of H4 histone methylation by PRMT5/MEP50 complex.
CSN15907	GSK343	1346704-33-3	GSK343 is a potent and selective EZH2 inhibitor with IC50 of 4 nM, showing 60 fold selectivity against EZH1, and > 1000 fold selectivity against other histone methyltransferases.
CSN16553	GSK503	1346572-63-1	GSK-503 is a selective EZH2 inhibitor with anticancer effect.
CSN18874	GNA002	1385035-79-9	GNA002 binds to Cys668 within the EZH2-SET domain, triggering EZH2 degradation through COOH terminus of Hsp70‐interacting protein (CHIP)‐mediated ubiquitination.
CSN18873	Gambogenic acid	173932-75-7	Gambogenic acid binds to Cys668 within the EZH2-SET domain, triggering EZH2 degradation through COOH terminus of Hsp70‐interacting protein (CHIP)‐mediated ubiquitination.
CSN18002	EPZ020411	1700663-41-7	EPZ020411 is a potent and selective small molecule PRMT6 inhibitor with an IC50 of 10 nM.
CSN18855	EPZ020411 HCl	2070015-25-5	EPZ020411 HCl is a potent and selective inhibitor of PRMT6 with IC50 of 10 nM, has > 10 fold selectivity for PRMT6 over PRMT1 and PRMT8.
CSN17943	EPZ011989 trifluoroacetate	1598383-41-5	EPZ011989 trifluoroacetate is a potent, selective orally bioavailable EZH2 inhibitor with Ki < 3 nM for EZH2 wt and EZH2 Y646, exhibiting 15-fold selectivity over EZH1 and > 3000-fold selectivity over other HMTase.
CSN16997	EPZ011989	1598383-40-4	EPZ011989 is a potent, selective orally bioavailable EZH2 inhibitor with Ki < 3 nM for EZH2 wt and EZH2 Y646 with 15-fold selectivity over EZH1 and > 3000-fold selectivity over other HMTase.
CSN17168	EPZ005687	1396772-26-1	EPZ005687 is a potent inhibitor of PRC2 with IC50 value of 54±5nM (measured by PRC2 enzymatic activity), with selectivity >500-fold over other HMTs, ~50-fold over EZH1. EPZ005687 can specifically inhibit H3K27 methylation.
CSN16352	Pinometostat	1380288-87-8	EPZ-5676 is an aminonucleoside inhibitor of DOT1L with Ki of 80 pM.
CSN17825	6-Cyano-N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-1-(pentan-3-yl)-1H-indole-4-carboxamide	1418308-27-6	EI1 is a selective inhibitor of wild type EZH2 and EZH2 Y641F mutant with IC50 values of 15 nM and 13 nM, respectively.
CSN17397	CARM1-IN-1	1020399-49-8	CARM1-IN-1 is a potent and specific CARM1 (Coactivator-associated arginine methyltransferase 1) inhibitor with IC50 of 8.6 μM and shows very low activity against PRMT1 and SET7 (IC50 > 600 μM).
CSN15763	N-(1-Benzylpiperidin-4-yl)-6,7-dimethoxy-2-(4-methyl-1,4-diazepan-1-yl)quinazolin-4-amine	935693-62-2	BIX-01294 is a G9a histone methyltransferase inhibitor with IC50 of 1.9 μM.
CSN15913	BIX-01294 3HCl	1392399-03-9	BIX-01294 3HCl is an inhibitor of G9a histone methyltransferase with IC50 of 2.7 μM in a cell-free assay, reduces H3K9me2 of bulk histones, also weakly inhibits GLP (primarily H3K9me3), no significant activity observed at other histone methyltransferases.
CSN17412	AZ505	1035227-43-0	AZ505 is a potent and highly selective inhibitor of the oncogenic protein SMYD2 (IC50=0.12 μM) with potential anticancer activity, > 600 fold than SMYD3 (IC50> 83.3 μM), DOT1L (IC50> 83.3 μM), EZH2 (IC50> 83.3 μM).
CSN17413	AZ505 ditrifluoroacetate	1035227-44-1	AZ505 ditrifluoroacetate selectively inhibits SMYD2 with IC50 of 0.12 μM.
CSN17908	A-366	1527503-11-2	A-366 is a peptide-competitive inhibitor of G9a/GLP with IC50 of ~3 nM.
CSN17152	3-Deazaneplanocin A	102052-95-9	3-Deazaneplanocin A is an attractive epigenetic anticancer agent through the inhibition of the cellular enhancer of zeste homolog 2 (EZH2) protein.

<< PREV 1 2 3 4 NEXT >>

Histone Methyltransferase 第 1 2 3 4 页，共 4 页

Histone Methyltransferase
第页，共 4 页