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Histone Methyltransferase

Histone Methyltransferase

货号 产品名 CAS号 信息
CSN23150 TC-E 5003 17328-16-4 TC-E 5003 is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor.
CSN18955 SGC2085 1821908-48-8 SGC2085 is a selectivel and potent CARM1 inhibitor with IC50 value of 50 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.
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 Trifluoroacetate 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.
CSN22899 GSK2807 Trifluoroacetate 2245255-66-5 GSK2807 Trifluoroacetate is a SMYD3 SAM-competitive inhibitor with Ki of 14 nM.
CSN26668 4,4'-(Furan-2,5-diyl)dibenzimidamide 73819-26-8 Furamidine, also known as DB75, is a cell-permeable inhibitor of protein arginine methyltransferase 1 (PRMT1) that is selective for PRMT1. Furamidine (DB75) binds to strings of AT base pair sequences in DNA′s minor groove. Furamidine was originally developed as an anti-parasitic compound for a variety of diseases including Chagas′ disease. Furamidine targets the enzyme active site and is primarily competitive with the substrate and noncompetitive toward the cofactor. Furthermore, cellular studies revealed that 1 is cell membrane permeable and effectively inhibits intracellular PRMT1 activity and blocks cell proliferation in leukemia cell lines with different genetic lesions.
CSN22826 Furamidine 2HCl 55368-40-6 Furamidine 2HCl is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor with IC50 of 9.4 μM.
CSN26548 EML741 2328074-38-8 for G9a. EML741 also inhibits DNMT1 (IC50, 3.1 μM), with no effect on DNMT3a or DNMT3b. EML741 exhibits low cell toxicity, and is membrane permeable and blood-brain barrier penetrated[1].
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].
CSN19229 Chaetocin 28097-03-2 Chaetocin, a natural product from Chaetomium species, is a histone methyltransferase inhibitor with IC50 of 0.8 μM, 2.5 μM and 3 μM for dSU (VAR)3-9, mouse G9a and Neurospora crassa DIM5, respectively. It also inhibits thioredoxin reductase (TrxR) with an IC50 of 4 μM.
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.
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.
CSN51379 EZH2-IN-6 2702269-27-8
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