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SGC707 --- Allosteric PRMT3 Inhibitor

Overview
Catalog # bs-60243c-2-mg-solid
Product Name SGC707 --- Allosteric PRMT3 Inhibitor
Specifications
Storage Buffer Powder
Storage Condition Store in dry, dark place at -20C for 1 year.
Target
Product Information Molecular Weight: 298.34

Formula: C16 H18 N4 O2

CAS Number: 1687736-54-4

InChi Key: DMIDPTCQPIJYFE-UHFFFAOYSA-N

InChi: InChI=1S/C16H18N4O2/c21-15(20-7-1-2-8-20)11-18-16(22)19-14-4-3-13-10-17-6-5-12(13)9-14/h3-6,9-10H,1-2,7-8,11H2,(H2,18,19,22)

Smiles: O=C(CNC(=O)NC1C=C2C=CN=CC2=CC=1)N1CCCC1

Purity: 98.0

Solubility: DMSO up to 100 mM

Appearance: Solid Power.

Shelf Life: 1.0 years
Description SGC707 is a potent, selective and cell-active allosteric inhibitor of protein arginine methyltransferase 3 (PRMT3). SGC707 is a potent PRMT3 inhibitor (IC50 =31±2 nM, KD =53±2 nM) with outstanding selectivity (selective against 31 other methyltransferases and more than 250 non-epigenetic targets). The mechanism of action studies and crystal structure of the PRMT3-SGC707 complex confirm the allosteric inhibition mode. Importantly, SGC707 engages PRMT3 and potently inhibits its methyltransferase activity in cells. It is also bioavailable and suitable for animal studies. This well-characterized chemical probe is an excellent tool to further study the role of PRMT3 in health and disease.