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Results for "

PKMT

" in MedChemExpress (MCE) Product Catalog:

9

Inhibitors & Agonists

1

Peptides

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-13808
    UNC 0631
    3 Publications Verification

    		 Histone Methyltransferase Cancer
    UNC 0631 is a potent histone methyltransferase G9a inhibitor with an IC50 of 4 nM. UNC 0631 potently reduces H3K9me2 levels in MDA-MB-231 cells with an IC50 of 25 nM .
    UNC 0631
  • HY-150510
    MS8511

    		Histone Methyltransferase Neurological Disease Cancer
    MS8511 is a selective G9a/GLP covalent irreversible inhibitor by targeting a cysteine residue at the substrate binding site, with IC50 values of 100 nM (G9a) and 140 nM (GLP), and Kd values of 44 nM (G9a) and 46 nM (GLP). MS8511 reduces the cellular H3K9me2 level and enhances antiproliferation activity. MS8511 can be used for the research of several types of cancers including brain, breast, ovarian, lung, bladder, melanoma, colorectal cancer, and other disease such as Alzheimer’s disease (AD), sickle cell disease, Prader−Willi syndrome (PWS) .
    MS8511
  • HY-13807
    UNC0646
    1 Publications Verification

    		 Histone Methyltransferase Cancer
    UNC0646 is a potent and selective histone methyltransferase G9a inhibitor with an IC50 of 6 nM. UNC0646 is also a potent GLP inhibitor (IC50 <15 nM) and highly selective for G9a/GLP over SETD7, SUV39H2, SETD8 and PRMT3. UNC0646 reduces H3K9me2 levels in MDA-MB-231 cells with an IC50 of 26 nM .
    UNC0646
  • HY-10929
    UNC0224
    2 Publications Verification

    		 Histone Methyltransferase Cancer
    UNC0224 is a potent and selective histone methyltransferase G9a inhibitor with a Ki of 2.6 nM, an IC50 of 15 nM and a Kd of 23 nM. UNC0224 also potently inhibits b>GLP with assay-dependent IC50 values of 20-58 nM. UNC0224 is inactive against SET7/9, SET8/PreSET7, PRMT3 and JMJD2E .
    UNC0224
  • HY-10930
    UNC0321
    2 Publications Verification

    		 Histone Methyltransferase GCGR Apoptosis Cancer
    UNC0321 is a potent and selective histone methyltransferase G9a inhibitor with a Ki of 63 pM and with assay-dependent IC50 values of 6-9 nM. UNC0321 also inhibits GLP with assay-dependent IC50 values of 15-23 nM. UNC0321 has anti-apoptotic activity and has potential application in diabetic vascular complications .
    UNC0321
  • HY-P10463
    ssK36

    		Histone Methyltransferase Cancer
    ssK36 is a supersubstrate peptide of the histone methyltransferase (SET) domain protein 2 (SETD2), and ssK36 is designed for the SETD2 protein, a specific PKMT. It is responsible in human cells for adding methyl groups to the 36th lysine residue of histone H3 (H3K36) to form H3K36me3. ssK36 can be methylated by SETD2 at a rate more than 100 times faster than the natural substrate H3K36. ssK36 can be used to study the catalytic mechanism of PKMTs, especially substrate specificity and catalytic efficiency .
    ssK36
  • HY-149005
    PRMT5-IN-19

    		Histone Methyltransferase Cancer
    PRMT5-IN-19 (Compound 41) is an selective orally active non-nucleoside PRMT5 inhibitor with IC50 values of 23.9 nM (radioactive biochemical assay) and 47 nM (AlphaLISA assay). PRMT5-IN-19 can occupy the SAM-binding pocket in PRMT5 and block methyltransferase activity, which displays good selectivity over other PRMTs and PKMTs. PRMT5-IN-19 inhibits cell proliferation by inducing cell apoptosis, and can be used for cancer-related research .
    PRMT5-IN-19
  • HY-155154
    PRMT4-IN-2

    		Others Cancer
    PRMT4-IN-2 (compound 55) is a pan-inhibitor of protein arginine methyltransferase (PRMT) with IC50s of 92 nM (PRMT4), 436 nM (PRMT6), 460 nM (PRMT1), 823 nM ( PRMT8), 1.386 μM (PRMT3) .
    PRMT4-IN-2
  • HY-155154A
    PRMT4-IN-3

    		Histone Methyltransferase Cancer
    PRMT4-IN-3 (compound 56) is a potent inhibitor of class I protein arginine methyltransferase (PRMT), targeting PRMT4 (IC50: 37 nM) and PRMT4 (IC50: 253 nM) .
    PRMT4-IN-3

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