| Chemical Properties | Back Directory | [Boiling point ]
562.0±60.0 °C(Predicted) | [density ]
1.137±0.06 g/cm3(Predicted) | [storage temp. ]
2-8°C | [solubility ]
DMSO: 2mg/mL, clear (warmed) | [form ]
powder | [pka]
8.66±0.10(Predicted) | [color ]
white to beige | [InChI]
1S/C22H35N5O2/c1-5-6-7-8-11-23-22-25-18-15-20(29-4)19(28-3)14-17(18)21(26-22)24-16-9-12-27(2)13-10-16/h14-16H,5-13H2,1-4H3,(H2,23,24,25,26) | [InChIKey]
ZYNUWSFRZCRKSN-UHFFFAOYSA-N | [SMILES]
CN(CC1)CCC1NC2=C3C(C=C(OC)C(OC)=C3)=NC(NCCCCCC)=N2 |
| Hazard Information | Back Directory | [Description]
MS012 is a Potent and Selective Inhibitors for G9a-Like Protein (GLP) Lysine Methyltransferase. MS012 exhibited stronger binding affinity to GLP (Kd = 46 ± 15 nM) than G9a (Kd = 610 ± 68 nM). MS012 was 13-fold selective for GLP over G9a. G9a-like protein (GLP) and G9a are highly homologous protein lysine methyltransferases (PKMTs) sharing approximately 80% sequence identity in their catalytic domains. GLP and G9a form a heterodimer complex and catalyze mono- and dimethylation of histone H3 lysine 9 and nonhistone substrates. | [Uses]
MS012 is a selective GLP inhibitor (IC50=7 nM). MS012 can be used in research of GLP dysregulation, including cancer, inflammatory diseases, and neuroregenerative disorders[1]. | [References]
[1] Xiong Y, et al. Discovery of Potent and Selective Inhibitors for G9a-Like Protein (GLP) Lysine Methyltransferase. J Med Chem. 2017 Mar 9;60(5):1876-1891. DOI:10.1021/acs.jmedchem.6b01645 |
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| Company Name: |
Energy Chemical
|
| Tel: |
021-58432009 400-005-6266 |
| Website: |
http://www.energy-chemical.com |
| Company Name: |
Merck KGaA
|
| Tel: |
21-20338288 |
| Website: |
www.sigmaaldrich.cn |
|