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Histone Methyltransferase

Histone Methyltransferase

Cat. No. Product Name CAS No. Information
CSN26505 VTP-50469 2169916-18-9 VTP-50469 is a novel, potent, selective, orally-available MeninMLL1 inhibitor, being effectively against MLL-rearranged and NPM1c+ leukemia, selectively killing cell lines with MLLrearrangements and NPM1c+ mutations.
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.
CSN26408 Pf-06726304 1616287-82-1 PF-06726304 is a potent and selective EZH2 inhibitor with Ki value of 0.7 nM.
CSN27839 NSD2-PWWP1 antagonist 3f 1210906-48-1 NSD2-PWWP1 antagonist 3f can bind to the NSD2-PWWP1 domain with Kd value of 3.4μM and abrogates histone H3K36me2 binding to the PWWP1 domain in cells.
CSN27203 ms1943 2225938-17-8 MS1943 is a first-in-class EZH2 selective degrader that effectively reduces EZH2 levels in cells.
CSN20284 MM-589 Trifluoroacetate 2253167-09-6 MM-589 trifluoroacetate is a potent inhibitor of the WD repeat domain 5 protein WDR5mixed lineage leukemia MLL interaction and may yield a therapy for acute leukemia
CSN20283 MM-589 2097887-20-0 MM-589 is a potent inhibitor of the WD repeat domain 5 protein WDR5mixed lineage leukemia MLL interaction and may yield a therapy for acute leukemia
CSN19671 MI-538 1857417-10-7 MI-538 is a potent and selective MLL inhibitor (mixed lineage leukemia inhibitor).
CSN26672 M-808 2377335-74-3 M-808 is a highly potent and efficacious covalent Menin-MLL interaction inhibitor, with IC50 values of 1 nM and 4 nM in MV4;11 cells and MOLM-13 cells, respectively[1].
CSN22449 LLY-283 2040291-27-6 LLY-283 is a potent selective and oral protein arginine methyltransferase 5 PRMT5 inhibitor with an IC50 of 22 nM and a Kd of 6 nM for PRMT5MEP50 complex and shows antitumor activity
CSN22869 JQEZ5 1913252-04-6 JQEZ5 is a potent and selective SAM-competitive EZH2 lysine methyltransferase inhibitor with IC50 of 11 nM.
CSN17955 GSK591 1616391-87-7 GSK591 is a potent and selective inhibitor of H4 histone methylation by PRMT5MEP50 complex.
CSN26479 GSK3368715 free base 1629013-22-4 GSK3368715, aslo known as EPZ019997, is a potent, reversible type I PRMT inhibitor with anti-tumor effects in human cancer models. Inhibition of PRMT5, the predominant type II PRMT, produces synergistic cancer cell growth inhibition when combined with GSK3368715. Interestingly, deletion of the methylthioadenosine phosphorylase gene (MTAP) results in accumulation of the metabolite 2-methylthioadenosine, an endogenous inhibitor of PRMT5, and correlates with sensitivity to GSK3368715 in cell lines.
CSN26480 GSK3368715 2HCl 2227587-25-7 GSK3368715 dihydrochloride is a novel potent type-I protein arginine methyltransferases (PRMTs) inhibitor.
CSN23320 GSK3326595 1616392-22-3 GSK3326595 is a potent specific and reversible PRMT5 inhibitor which can decrease the levels of both monomethylated and dimethylated arginine residues in histones H2A H3 and H4
CSN22899 GSK2807 Trifluoroacetate 2245255-66-5 GSK2807 Trifluoroacetate is a SMYD3 SAM-competitive inhibitor with Ki of 14 nM
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.
CSN22826 Furamidine 2HCl 55368-40-6 Furamidine 2HCl is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor with IC50 of 9.4 μM.
CSN22212 EZM 2302 1628830-21-6 EZM 2302 is the first potent and selective inhibitor of CARM1 enzymatic activity with IC50 value of 6 nM.
CSN26674 EZH2-​IN-​2 2238821-31-1 EZH2-IN-2 is a EZH2 inhibitor extracted from patent WO2018133795A1, Compound Example 69, with an IC50 of 64 nM. EZH2-IN-2 can be used for the research of cancer or precancerous condition related to EZH2 activity[1].
CSN18964 EPZ031686 2095161-11-6 EPZ031686 is a noncompetitive inhibitor for SMYD3 and MEKK2 with a Ksubisub12 nM and 11 nM respectively
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.
CSN21098 EBI-2511 2098546-05-3 EBI-2511 is a Highly Potent and Orally Active EZH2 Inhibitor for the Treatment of Non-Hodgkins Lymphoma EBI-2511 showed enzymatic activity and cellular activity of 40 and 60nM respectively EBI-2511 demonstrated excellent in vivo efficacy in Pfeiffer tumor Xenograft models in mouse and is under preclinical development for the treatment of cancers associated with EZH2 mutations
CSN26671 CMP-5 HCl 1030021-40-9 CMP5 is a potent and selective PRMT5 Inhibitor. CMP5 showed to occupy hPRMT5 catalytic site and block symmetrically dimethylated S2Me-H4R3 & S2Me-H3R8 with no effect on the asymmetric methylation of H4R3 in lymphoblastoid cell lines at 40 µM. CMP-5 shows promise as a novel therapeutic approach for B-cell lymphomas.
CSN26670 CMP-5 880813-42-3 CMP-5 is a potent, specific, and selective PRMT5 inhibitor, while displays no activity against PRMT1, PRMT4, and PRMT7 enzymes. CMP-5 selectively blocks S2Me-H4R3 by inhibiting PRMT5 methyltransferase activity on histone preparations. CMP-5 prevents Epstein-Barr virus (EBV)-driven B-lymphocyte transformation but leaving normal B cells unaffected[1][2].
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.
CSN22321 BAY-598 1906919-67-2 BAY-598 is an inhibitor of SMYD2 It can inhibit in vitro methylation of p53 at lysine 370 with IC50 value of 27 nM
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.
CSN27520 AMI-1 free acid 134-47-4 AMI-1 free acid is a potent, cell-permeable and reversible inhibitor of protein arginine N-methyltransferases (PRMTs), with IC50s of 8.8 μM and 3.0 μM for human PRMT1 and yeast-Hmt1p, respectively. AMI-1 free acid exerts PRMTs inhibitory effects by blocking peptide-substrate binding.
CSN20242 A-893 1868232-32-9 A-893 is a potent and selective SMYD2 inhibitor IC50 28 nM
CSN21388 A-395 2089148-72-9 A-395 is a antagonist of Polycomb repressive complex 2 PRC2 proteinprotein interactions that potently inhibits the trimeric PRC2 complex EZH2EEDSUZ12 with an IC50 of 18 nM
CSN19081 A-196 1982372-88-2 A-196 is a potent and selective inhibitor of SUV420H1 and SUV420H2 with IC50s of 25 and 144 nM respectively
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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