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Histone Methyltransferase Histone methyltransferase

Cat.No.  Name Information
M2358 3-Deazaneplanocin A 3-deazaneplanocin A (DZNeP), an analog of adenosine, is a competitive inhibitor of S-adenosylhomocysteine hydrolase with Ki of 50 pM.
M41692 UNC7096 UNC7096 is a potent and selective NSD2-PWWP1 degrader with a Kd of 46 nM.
M41691 Igermetostat Igermetostat is EZH2 inhibitor, used in cancer research in vivo and in vitro.
M41690 WM-586 WM-586 is a covalent WDR5 inhibitor that disrupts the binding of WDR5 to MYC.
M41689 PRMT5-IN-28 PRMT5-IN-28 is an inhibitor of protein arginine methyltransferase 5 (PRMT5) enzyme.
M41688 EML734 EML734 is a potent and selective PRMT7/9 inhibitor with IC50 values of 315 nM and 0.89 μM, respectively.
M41686 BBDDL2059 BBDDL2059 is a selective covalent inhibitor of histone methyltransferase EZH2 with an IC50 of 1.5 nM for EZH2-Y641F.
M41685 CARM1-IN-3 CARM1-IN-3 is a potent and selective co-activator associated arginine methyltransferase (CARM1) inhibitor with IC50 values of 0.07, >25 µM for CARM1 and CARM3, respectively.
M41346 PRMT5-IN-31 PRMT5-IN-31 is a selective PRMT5 inhibitor (IC50: 0.31 μM).
M40717 UNC0321 UNC0321 is a high affinity inhibitor of GPCRs and can be used in studies related to chromatin remodeling. It is also a selective inhibitor of histone methyltransferase G9a with a Ki of 63 pM and an IC50 value of 6-9 nM.In addition, UNC0321 also inhibits GLP with an IC50 value of 15-23 nM.
M38950 Tanshindiol C Tanshindiol C is a S-adenosylmethionine-competitive EZH2 (Histone Methyltransferase) inhibitor with an IC50 of 0.55 μM for inhibiting the methyltransferase activity. Tanshindiol C is also an activator of both Nrf2 and Sirtuin 1 (Sirt1) in macrophages.
M31020 SETDB1-TTD-IN-1 TFA  SETDB1-TTD-IN-1 TFA is a potent, selective and endogenous binder competitive inhibitor of SET domain bifurcated protein 1 tandem tudor domain (SETDB1-TTD), with a Kd of 88 nM. SETDB1-TTD-IN-1 TFA can be used for the research of biological functions and disease associations of SETDB1-TTD.
M31019 OTS186935 hydrochloride  OTS186935 hydrochloride is a potent protein methyltransferase SUV39H2 inhibitor with an IC50 of 6.49 nM. OTS186935 hydrochloride shows significant inhibition of tumor growth in mouse xenograft models without any detectable toxicity. OTS193320 hydrochloride regulates the production of γ-H2AX in cancer cells.
M30844 CPUY074020  CPUY074020 is a potent and oral bioavailable inhibitor of histone methyltransferase G9a, with an IC50 of 2.18 μM. CPUY074020 possesses anti-proliferative activity.
M30619 DCLX069  DCLX069 is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 value of 17.9 µM. DCLX069 shows less active against PRMT4 and PRMT6. DCLX069 has anticancer effects.
M30098 CSV0C018875  CSV0C018875 is a quinoline-based EHMT2/G9a inhibitor. CSV0C018875 exhibits lesser cytotoxicity than BIX-01294.
M29869 DC-S239  DC-S239 is a selective histone methyltransferase SET7 inhibitor with an IC50 value of 4.59 μM. DC-S239 also displays selectivity for DNMT1, DOT1L, EZH2, NSD1, SETD8 and G9a. DC-S239 has anticancer activity.
M29798 SETDB1-TTD-IN-1  SETDB1-TTD-IN-1 is a potent, selective and endogenous binder competitive inhibitor of SET domain bifurcated protein 1 tandem tudor domain (SETDB1-TTD), with a Kd of 88 nM. SETDB1-TTD-IN-1 can be used for the research of biological functions and disease associations of SETDB1-TTD.
M29754 RK-701  RK-701 is an highly selective and non-genotoxic inhibitor of G9a with IC50 value of 23-27 nM. RK-701 selectively up-regulates HbF, γ- Globin, BGLT3 expression, down-regulates H3K9me2 expression. RK-701 also has inhibition for BCL11A and ZBTB7A.
M29624 WDR5-IN-5  WDR5-IN-5 is an orally active and selective inhibitor of WIN site of WD repeat domain 5 (WDR5). WDR5-IN-5 exhibits anti-proliferative activity towards cancer cells and good pharmacokinetics profile in mice. WDR5-IN-5 shows high affinity to WDR5 and the binding affinity Ki value <0.02 nM.
M29447 MM-589 TFA  MM-589 TFA is a potent inhibitor of WD repeat domain 5 (WDR5) and mixed lineage leukemia (MLL) protein-protein interaction. MM-589 binds to WDR5 with an IC50 of 0.90 nM and inhibits the MLL H3K4 methyltransferase activity with an IC50 of 12.7 nM.




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