PRMT1-2e, Protein Arginine Methyltransferase 1 (PRMT1) Inhibitor

PRMT1-2e is a potent, specific and cell permeable inhibitor of protein arginine methyltransferase 1 (PRMT1) with an IC50 ~1.5 μM. It has no activity against CARM1 and Set7/9 methyltransferases. It inhibits growth of MCF7a breast cancer cells (IC50 ~1.97 μM) and LNCaP prostate cancer cells (IC50 ~4.49 μM). It can attenuate androgen-induced gene expression in LNCaP cells.

Product information

CAS Number: 17328-16-4

Molecular Weight: 401.26

Formula: C16H14Cl2N2O4S

Chemical Name: N,N'-(sulfonylbis(4,1-phenylene))bis(2-chloroacetamide)

Smiles: O=S(=O)(C1C=CC(=CC=1)NC(=O)CCl)C1C=CC(=CC=1)NC(=O)CCl

InChiKey: SHRCVZJKZJGIHQ-UHFFFAOYSA-N

InChi: InChI=1S/C16H14Cl2N2O4S/c17-9-15(21)19-11-1-5-13(6-2-11)25(23,24)14-7-3-12(4-8-14)20-16(22)10-18/h1-8H,9-10H2,(H,19,21)(H,20,22)

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO up to 50 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: ≥360 days 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:

PRMT1-2e was used at 10 µM in vitro.

References:

1. Bissinger EM, et al. Acyl derivatives of p-aminosulfonamides and dapsone as new inhibitors of the arginine methyltransferase hPRMT1. (2011) Bioorg Med Chem. 19(12):3717-31.

Products are for research use only. Not for human use.