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Histone Methyltransferase
T3984 GLP-1(7-36) GLP-1 (7-36) amide is a peptide hormone released from intestinal L-cells upon nutrient consumption. It binds the GLP-1 receptor in the pancreas and displays various antidiabetic effects by potentiating glucose-induced secretion of insulin from pancreatic β-cells, increasing insulin expression.
T6857 HLCL-61 HLCL-61 hydrochloride is a potent and selective PRMT5 inhibitor for the treatment of acute myeloid leukemia.
T3257 UNC0638 UNC0638 is an inhibitor of β-protein lysine methyltransferases G9a(IC50<15 nM) and GLP(IC50=19 nM) with excellent potency and selectivity over a wide range of epigenetic and non-epigenetic targets.
T6790 BMS-911543 BMS-911543 is a potent and selective inhibitor of JAK2 with IC50 of 1.1?nM, ~350-, 75- and 65-fold selective to JAK1, JAK3 and TYK2, respectively. Phase 1/2.
T2643 MI-3 MI-3 (Menin-MLL Inhibitor) is an effective inhibitor of Menin-MLL interaction (IC50: 648 nM).
T2649 MI-2 MI-2 (Menin-MLL Inhibitor) is a potent menin-MLL interaction inhibitor with IC50 of 446 nM.
T2354 UNC 0631 UNC0631 is a effectvie histone methyltransferase G9a inhibitor (IC50=4 nM).
T3081 EPZ004777 EPZ004777 is a potent, selective DOT1L inhibitor with IC50 of 0.4 nM.
T1775 GSK503 GSK-503, a potent EZH2 inhibitor, has potential antitumor activity.
T2079 GSK126 GSK126 is a excellently specific EZH2 methyltransferase inhibitor ( IC50=9.9 nM).
T6059 GSK343 GSK343,a specific and effective EZH2 inhibitor (IC50=4 nM), exhibits 60 fold specificity activity against EZH1, and >1000 fold specificity activity against other histone methyltransferases.
T1923 BRD4770 BRD4770 is a histone methyltransferase G9a inhibitor and induces cell senescence.
T3099 EPZ5676 EPZ5676 has been used in trials studying the treatment of Leukemia, Acute Leukemias, Acute Myeloid Leukemia, Myelodysplastic Syndrome, and Acute Lymphocytic Leukemia, among others.
T3081L EPZ004777 hydrochloride EPZ004777 hydrochloride is a potent, selective?DOT1L?inhibitor with?IC50?of 0.4 nM.
T1959 BIX 01294 Trihydrochloride BIX01294 is an inhibitor of G9a histone methyltransferase.In a cell-free assay, the IC50=2.7 μM for G9a histone methyltransferase.
T1905 EPZ005687 EPZ005687 is a potent and selective inhibitor of EZH2.
T1788 EPZ6438 Tazemetostat is an orally available, small molecule selective and S-adenosyl methionine (SAM) competitive inhibitor of histone methyltransferase EZH2, with potential antineoplastic activity. Upon oral administration, Tazemetostat selectively inhibits the activity of both wild-type and mutated forms
T6333 MM-102 MM-102 is a high-affinity peptidomimetic MLL1 inhibitor with IC50 of 0.4 μM.
T6484 EI1 EI1 is a potent and selective EZH2 inhibitor with IC50 of 15 nM and 13 nM for EZH2 (WT) and EZH2 (Y641F), respectively.
T3057 UNC1999 UNC1999 is a orally bioavailable, effective and specific inhibitor of EZH2 (IC50=2 nM) and EZH1 (IC50=45).
T6809 CPI-169 CPI-169 is a potent, and selective EZH2 inhibitor with IC50 of 0.24 nM, 0.51 nM, and 6.1 nM for EZH2 WT, EZH2 Y641N, and EZH1, respectively.
T4166 UNC-0642 UNC0642 is an effective and specific G9a/GLP inhibitor (IC50< 2.5 nM).
T4378 MS049 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.
T3624 A-366 Potent and selective G9a/GLP histone lysine methyltransferase inhibitor (IC50 = 3.3 nM). Exhibits >1000-fold selectivity for G9a/GLP over 21 other methyltransferases. Decreases levels of lysine 9 dimethylation on histone H3 (H3K9Me2) in PC3 cells.
T3082 SGC0946 SGC0946 is a highly effective and specific DOT1L methyltransferase inhibitor (IC50: 0.3 nM); selectively kill mixed lineage leukemia cells.
T2435 EPZ011989 EPZ011989 is a effective, specific orally bioavailable EZH2 inhibitor with Ki < 3 nM for EZH2 Y646 and EZH2 wt; 15-fold selectivity over EZH1 and >3000-fold selectivity over other HMTase.
T6076 EPZ015666 EPZ015666 is an orally available inhibitor of PRMT5 enzymatic activity.
T6853 GSK591 GSK591,Alternative Names are EPZ015866, GSK3203591, is a potent selective inhibitor of the arginine methyltransferase PRMT5 (IC50=11 nM).
T1841 UNC0379 UNC0379 is a selective, substrate-competitive inhibitor of the lysine methyltransferase SETD8.
T1987 PFI-2 PFI-2 is an effective, specific and cell-active lysine methyltransferase SETD7 inhibitor (Ki/IC50: 0.33/2 nM), 1000-fold selectivity over other methyltransferases and other non-epigenetic targets.
T3084 SGC707 SGC707 is a potent, selective, and cell-active allosteric inhibitor of PRMT3.
T4314 EPZ020411 EPZ020411 is a specific and effective inhibitor of PRMT6 (IC50=10 nM).
T6879 LLY-507 LLY-507 is an effective, cell-active, and specific inhibitor of protein-lysine Methyltransferase SMYD2.
T6810 CPI-360 CPI-360 is a potent, selective,and SAM-competitive EZH1 inhibitor with IC50 of 102.3 nM, >100-fold selectivity over other methyltransferases.
T4013 SGC2085 HCl SGC2085 is a potent and selective coactivator associated arginine methyltransferase 1 (CARM1) Inhibitor with an IC50 of 50 nM and more than undred-fold selectivity over other PRMTs. CARM1 is an important positive modulator of Wnt/β-catenin transcription and neoplastic transformation in colorectal c
T6900 MS023 MS023 is a potent, selective, and cell-active Type I PRMT inhibitor with IC50 of 30 nM, 119 nM, 83 nM, 4 nM, and 5 nM for PRMT1, PRMT3, PRMT4, PRMT6 and PRMT8, respectively.
T4021 UNC3866 UNC3866 is a potent antagonist of the CBX7-H3 interaction as determined by AlphaScreen.
T4343 A-196 A-196 is a potent and selective inhibitor of SUV420 h1 and SUV420 h2 with IC50 values of 0.025 and 0.144 μM, respectively; more than 100-fold selective over other histone methyltransferases and non-epigenetic targets.
T1868 JIB-04 (NSC 693627)(E) JIB-04 is a pan-selective Jumonji histone demethylase inhibitor.
T2352 AMI-1 AMI-1 is an effective and selective Histone Methyltransferase (HMT) inhibitor (IC50: 3.0/8.8 μM, for yeast Hmt1p, and human PRMT1).
T6876 Liraglutide Liraglutide is a long-acting GLP-1 receptor agonist.
T3458 EED226 EED226 is a potent, selective, and orally bioavailable embryonic ectoderm development (EED) inhibitor with an IC50 of 22 nM.
T6803 Chaetocin 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.
T0174 Cyproheptadine hydrochloride Cyproheptadine hydrochloride sesquihydrate, an antihistamine, is an antagonist of serotonin and histamine2.
T2097 C7280948 C-7280948 is a PRMT1 inhibitor.
T3896 Shanzhiside methylester Shanzhiside methylester reduces neuropathic pain by activating spinal GLP-1 receptors and subsequently stimulating microglial β-endorphin expression via the p38 MAPK signaling.
T4334 EPZ020411 2HCl (1700663-41-7(free base)) EPZ020411 is an effective and specific small molecule PRMT6 inhibitor (IC50=10 nM).
T4393 MS049 2HCl (1502816-23-0(free base)) MS049 is a potent and selective inhibitor of PRMT4 (IC50 = 34 nM) and PRMT6 (IC50 = 43 nM). It is less active against additional type I PRMTs (IC50s = >130, >220, and 1.6 μM for PRMT1, PRMT3, and PRMT8, respectively) and displays no inhibition against type II or type III PRMTs nor any additional me
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