Description
GSK3368715 is a potent inhibitor of type I protein arginine methyltransferases (PRMT) that inhibits PRMT1, 3, 4, 6 and 8 with Kiapp vaules ranging from 1.5 to 81 nM.
Product information
CAS Number: 2227587-26-8
Molecular Weight: 475.92
Formula: C20H41Cl3N4O2
Chemical Name: ({5-[4, 4-bis(ethoxymethyl)cyclohexyl]-1H-pyrazol-4-yl}methyl)(methyl)[2-(methylamino)ethyl]amine trihydrochloride
Smiles: Cl.Cl.Cl.CNCCN(C)CC1C=NNC=1C1CCC(COCC)(COCC)CC1
InChiKey: KBFPGRMCKLUHTA-UHFFFAOYSA-N
InChi: InChI=1S/C20H38N4O2.3ClH/c1-5-25-15-20(16-26-6-2)9-7-17(8-10-20)19-18(13-22-23-19)14-24(4)12-11-21-3;;;/h13,17,21H,5-12,14-16H2,1-4H3,(H,22,23);3*1H
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: Solubility (25°C). DMSO: 81 mg/mL(170.19 mM). Water: 81 mg/mL(170.19 mM).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
GSK3368715 is a potent, reversible, SAM uncompetitive inhibitor of type I PRMTs that produces a shift in arginine methylation states on hundreds of substrates from ADMA to MMA and SDMA. As a monotherapy, GSK3368715 induces anti-proliferative effects on cell lines from a broad range of hematological and solid tumor types in vitro.
In Vivo:
GSK3368715 has potent, anti-proliferative activity across cell lines representing a range of solid and hematological malignancies and can completely inhibit tumor growth or cause regressions of tumor models in vivo.
Products are for research use only. Not for human use.
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