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Histone Methyltransferase

Histone Methyltransferase

Cat. No. Product Name CAS No. Information
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 UNC669   1314241-44-5 UNC669 is a selective inhibitor of MBT malignant brain tumor with IC50 of 6 M 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 G9aGLP with IC50 of 15 nM
CSN17958 UNC0379 Trifluoroacetate 1620401-83-3 UNC0379 trifluoroacetate is a selective substrate-competitive inhibitor of the lysine methyltransferase SETD8 with IC50 of 7310 M 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 73 10 M
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 UNC0631 1320288-19-4 UNC 0631 is a potent G9a inhibitor with IC50 value of 4 nM
CSN23170 TP 064 2080306-20-1 TP-064 is a potent and selective PRMT4 inhibitor. The in vitro activity of TP-064 includes inhibition of PRMT4 with IC50 < 10nM for methylation of H3 (1-25) and greater than 100-fold selectivity over other histone methyltransferases and non-epigenetic targets. In cellular assays, TP-064 inhibits the methylation of MED12 with IC50 = 43 nM.
CSN23150 TC-E 5003 17328-16-4 TC-E 5003 is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor.
CSN16351 SGC707 1687736-54-4 SGC707 is a chemical probe of PRMT3 with IC50 of 31 nM
CSN17931 SGC0946 1561178-17-3 SGC0946 is a selective inhibitor of DOT1L methyltransferase with IC50 of 03 nM and can kill mixed lineage leukaemia cells
CSN23083 Ryuvidine 265312-55-8 Ryuvidine is an inhibitor of SETD8 with cellular activity. It also acts as a CDK4 inhibitor and inducer of the DNA damage response.
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
CSN19677 MS453 2059892-29-2 MS453 is a covalent inhibitor of the SET domain-containing protein 8 (SETD8) lysine methyltransferase.
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 1346and 8 respectively MS023 is active in cells
CSN19671 MI-538 1857417-10-7 MI-538 is a potent and selective MLL inhibitor (mixed lineage leukemia inhibitor).
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
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
CSN17955 GSK591 1616391-87-7 GSK591 is a potent and selective inhibitor of H4 histone methylation by PRMT5MEP50 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
CSN13635 GSK126     1346574-57-9 GSK126 is a potent, highly selective EZH2 methyltransferase inhibitor with IC50 of 9.9 nM, > 1000-fold selective for EZH2 over 20 other human methyltransferases.
CSN18874 GNA002 1385035-79-9 GNA002 binds to Cys668 within the EZH2-SET domain triggering EZH2 degradation through COOH terminus of Hsp70interacting protein CHIPmediated ubiquitination
CSN21374 EZH2 Inhibitor 1 1844849-18-8 EZH2 Inhibitor 1 is an inhibitor of EZH2.
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 545nM measured by PRC2 enzymatic activity with selectivity 500-foldoverotherHMTs50-foldoverEZH1 EPZ005687 can specifically inhibit H3K27 methylation
CSN13673 EPZ004777 1338466-77-5 EPZ004777 is a potent selective DOT1L inhibitor with IC50 of 04 nM in a cell-free assay and demonstrates 1200-fold selectivity for DOT1L over all other tested PMTs
CSN13684 EPZ004777 HCl 1380316-03-9 EPZ004777 HCl is a potent selective DOT1L inhibitor with an IC50 of 04 nM in a cell-free assay
CSN13909 EPZ-6438   1403254-99-8 EPZ-6438 is a potent, selective, and orally bioavailable small-molecule inhibitor of EZH2 enzymatic activity with Ki value of 2.5±0.5 nM.
CSN16352 EPZ-5676 1380288-87-8 EPZ-5676 is an aminonucleoside inhibitor of DOT1L with Ki of 80 pM.
CSN17825 EI1 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 86 M and shows very low activity against PRMT1 and SET7 IC50 600 M
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.
CSN23850 BCI-121 432529-82-3 BCI-121 (BCI121) is a substrate-competitive inhibitor of SMYD3 that inhibits SMYD3-substrate interaction and chromatin recruitment It can significantly reduce the proliferation of various cancer cells.
CSN13910 Amodiaquin 2HCl 2H2O   6398-98-7 Amodiaquine 2HCl is an inhibitor of histamine N-methyltransferase inhibitor with antimalarial and anti-inflammatory activities.
CSN12600 AMI-1 20324-87-2 AMI-1 is an inhibitor of protein arginine N-methyltransferases (PRMTs) with IC50 of 8.8 M for PRMT1 via blocking peptide-substrate binding.
CSN17908 A-366 1527503-11-2 A-366 is a peptide-competitive inhibitor of G9aGLP 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.
CSN13890 3-Deazaneplanocin A HCl 120964-45-6 3-Deazaneplanocin A HCl is a cyclopentanyl analog of 3-deazaadenosine that potently interferes with SAH, a component of the methionine cycle, which causes cellular SAH levels to increase, thus repressing the activity of S-adenosyl-l-methionine–dependent histone lysine methyltransferase activity.
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