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Histone Methyltransferase

Histone Methyltransferase

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 UNC669 1314241-44-5 UNC669 is a selective inhibitor of MBT (malignant brain tumor) with IC50 of 6 μM for L3MBTL1.
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 Trifluoroacetate 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 UNC0631 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.
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 hydrochloride 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.
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.
CSN13507 MI-2 1271738-62-5 MI-2 can inhibits menin-MLL interaction with IC50 of 446 ± 28 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.
CSN17504 HLCL-61 HCl 1158279-20-9 HLCL-61 hydrochloride is an inhibitor of PRMT5 that is used for the treatment of acute myeloid leukemia.
CSN17955 GSK591 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.
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.
CSN16553 GSK503 1346572-63-1 GSK-503 is a selective EZH2 inhibitor with anticancer effect.
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.
CSN13673 EPZ004777 1338466-77-5 EPZ004777 is a potent, selective DOT1L inhibitor with IC50 of 0.4 nM in a cell-free assay and demonstrates > 1,200-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 0.4 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.
CSN16353 CPI-360 1802175-06-9 CPI-360 is a potent, selective EZH2 inhibitor with IC50 of 0.5 nM and 2.5 nM for wt EZH2 and Y641N EZH2, 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).
CSN12593 C-7280948 587850-67-7 C-7280948 is an inhibitor of PRMT1.
CSN13838 BRD4770 1374601-40-7 BRD4770 is an inhibitor of histone methyltransferase G9a with IC50 of 6.3 μM and it can induce cell senescence.
CSN15913 BIX-01294 3HCl 1392399-03-9 BIX01294 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.
CSN15763 BIX-01294 935693-62-2 BIX-01294 is a G9a histone methyltransferase inhibitor with IC50 of 1.9 μM.
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.
CSN13910 Amodiaquin 2HCl 2H2O 6398-98-7 Amodiaquine dihydrochloride 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 μM for PRMT1 via blocking peptide-substrate binding.
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.
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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