539214
PRMT Inhibitor VI
别名:
PRMT Inhibitor VI, 1-(1,2,3-Benzothiadiazol-6-yl)-3-[2-(1-cyclohexen-1-yl)ethyl]urea, Protein Arginine Methyltransferase Inhibitor VI, 1-(Benzo[d][1,2,3]thiadiazol-6-yl)-3-(2-cyclohexenylethyl)urea
assay
≥99% (HPLC)
form
solid
potency
1.6 μM IC50
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
off-white
solubility
DMSO: 100 mg/mL
shipped in
ambient
Quality Level
General description
A benzothiadiazolyl-cyclohexenylethylurea compound that binds to protein arginine methyltransferase 3 at the dimer interface and selectively inhibits PRMT3 activity in an allosteric manner (IC50 = 1.6 µM), while being non-competitive with respect to AdoMet (S-adenosyl-L-methionine; SAM) or peptide substrates (Ki = 2.9 and 4.2 mM, respectively). Exhibits little or no inhibitory activity against PRMT1/4/5/8 or protein lysine methyltransferases, EHMT1, SUV39H2, SETD7, and SETD8, even at concentrations above 100 µM. Although cell-permeable, it is metabolically unstable and therefore not recommended for cell cultures or in vivo applications.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
PRMT3
PRMT3
Reversible: yes
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Siarheyeva, A., et al. 2012. Structure20, 1425.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
存储类别
11 - Combustible Solids
wgk
WGK 1
flash_point_f
Not applicable
flash_point_c
Not applicable
法规信息
新产品
此项目有
Alena Siarheyeva et al.
Structure (London, England : 1993), 20(8), 1425-1435 (2012-07-17)
PRMT3, a protein arginine methyltransferase, has been shown to influence ribosomal biosynthesis by catalyzing the dimethylation of the 40S ribosomal protein S2. Although PRMT3 has been reported to be a cytosolic protein, it has been shown to methylate histone H4
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