TCS PIM-1 1( SC 204330 | TCS PIM 1-1 )

Catalog No. M14650 CAS No. 491871-58-0

COA

Datasheet

HNMR

HPLC

MSDS

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Product Name

TCS PIM-1 1
Note

Research use only, not for human use.
Brief Description

A potent, selective, ATP-competitive Pim-1 kinase inhibitor with IC50 of 50 nM.
Description

A potent, selective, ATP-competitive Pim-1 kinase inhibitor with IC50 of 50 nM; displays >400-fold selectivity over Pim-2 and MEK1/2.
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.
In Vivo

——
Synonyms

SC 204330 | TCS PIM 1-1
Pathway

JAK/STAT Signaling
Target

Pim
Recptor

Pim1
Research Area

Cancer
Indication

——

CAS Number

491871-58-0
Formula Weight

367.1961
Molecular Formula

C18H11BrN2O2
Purity

>98% (HPLC)
Solubility

DMSO: ≥ 52 mg/mL
SMILES

C1=CC=C(C=C1)C2=C(C(=O)NC(=C2)C3=C(C=CC(=C3)Br)O)C#N
Chemical Name

3-Pyridinecarbonitrile, 6-(5-bromo-2-hydroxyphenyl)-1,2-dihydro-2-oxo-4-phenyl-

1. Cheney IW, et al. Bioorg Med Chem Lett. 2007 Mar 15;17(6):1679-83.

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