PRMT Inhibitor VI

Name: PRMT Inhibitor VI
Brand: MM

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

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

storage temp.

2-8°C

Quality Level

100

Biochem/physiol Actions

Cell permeable: yes

Primary Target
PRMT3

Reversible: yes

Disclaimer

Toxicity: Standard Handling (A)

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.

Other Notes

Siarheyeva, A., et al. 2012. Structure20, 1425.

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.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Storage Class

11 - Combustible Solids

wgk

WGK 1

flash_point_f

Not applicable

flash_point_c

Not applicable

Certificates of Analysis (COA)

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An allosteric inhibitor of protein arginine methyltransferase 3.

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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