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Merck
CN

539214

Sigma-Aldrich

PRMT Inhibitor VI

Synonym(s):

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

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About This Item

Empirical Formula (Hill Notation):
C15H18N4OS
Molecular Weight:
302.39
UNSPSC Code:
12352200

Key Documents

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Assay

≥99% (HPLC)

Quality Level

100

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

storage temp.

2-8°C

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
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)

Storage Class Code

11 - Combustible Solids

WGK

WGK 1

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Regulatory Information

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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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