TCS PIM-1 1

TCS PIM-1 1 (SC 204330) is a potent and selective inhibitor of ATP-competitive Pim-1 kianse with IC50 of 50 nM, shows good selectivity over Pim-2 and MEK1/MEK2 with IC50 > 20000 nM.

Product information

CAS Number: 491871-58-0

Molecular Weight: 367.20

Formula: C18H11BrN2O2

Synonym:

TCS PIM-1 1

SC 204330

SC204330

SC-204330

Chemical Name:    3-Cyano-4-phenyl-6-(3-bromo-6-hydroxy)phenyl-2(1H)-pyridone

Smiles: N#CC1C(=O)NC(=CC=1C1C=CC=CC=1)C1=CC(Br)=CC=C1O

InChiKey: SVSYJTYGPLVUOZ-UHFFFAOYSA-N

InChi: InChI=1S/C18H11BrN2O2/c19-12-6-7-17(22)14(8-12)16-9-13(11-4-2-1-3-5-11)15(10-20)18(23)21-16/h1-9,22H,(H,21,23)

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: ≥12 months 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:

TCS PIM-1 1 (compound 1), a substituted pyridone scaffold, binds convincingly within the ATP-binding site of Pim-1 suggesting an ATP-competitive inhibitory mechanism. Preliminary data further suggests that TCS PIM-1 1 lacked in vitro inhibitory activity toward related serine/threonine kinases Pim-2 and MEK1/2. Hence, small molecules similar to TCS PIM-1 1 may serve as useful starting scaffolds for the development of other improved yet selective Pim-1 inhibitors. TCS PIM-1 1 serves both as a starting point for SAR chemical syntheses and was used for co-crystallization with Pim-1 protein.

References:

1. Cheney et al (2007) Identification and structure-activity relationships of substituted pyridones as inhibitors of Pim-1 kinase. Bioorg.Med.Chem.Letts. 17 1679 PMID: 17251021

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