hSMG-1 inhibitor 11j

hSMG-1 inhibitor 11j, a pyrimidine derivative, is a potent and selective inhibitor of hSMG-1, with an IC50 of 0.11 nM. hSMG-1 inhibitor 11j exhibits >455-fold selectivity for hSMG-1 over mTOR (IC50=50 nM), PI3Kα/γ (IC50=92/60 nM) and CDK1/CDK2 (IC50=32/7.1 μM). hSMG-1 inhibitor 11j can be used for the research of cancer.

Product information

CAS Number: 1402452-15-6

Molecular Weight: 566.07

Formula: C27H28ClN7O3S

Chemical Name: 1-{4-[4-(2-{[4-chloro-3-(diethylsulfamoyl)phenyl]amino}pyrimidin-4-yl)pyridin-2-yl]phenyl}-3-methylurea

Smiles: CNC(=O)NC1C=CC(=CC=1)C1=CC(=CC=N1)C1=CC=NC(NC2=CC(=C(Cl)C=C2)S(=O)(=O)N(CC)CC)=N1

InChiKey: RZFJBSIAXYEPBX-UHFFFAOYSA-N

InChi: InChI=1S/C27H28ClN7O3S/c1-4-35(5-2)39(37,38)25-17-21(10-11-22(25)28)32-26-31-15-13-23(34-26)19-12-14-30-24(16-19)18-6-8-20(9-7-18)33-27(36)29-3/h6-17H,4-5H2,1-3H3,(H2,29,33,36)(H,31,32,34)

Technical Data

Appearance: Solid Power

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

Solubility: Soluble in DMSO.

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:

hSMG-1 inhibitor 11j (0.3-3 μM; 6 h) significantly reduces UPF1 phosphorylation at 0.3 μM, and eliminates it at 1 μM in MDA 361 cells. hSMG-1 inhibitor 11j inhibits MDA468 cell proliferation, with an IC50 of 75 nM.

References:

1. Gopalsamy A, et, al. Identification of pyrimidine derivatives as hSMG-1 inhibitors. Bioorg Med Chem Lett. 2012 Nov 1;22(21):6636-41.

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