TCS PIM-1 1

Research use only, not for human use.

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

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

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.

——

SC 204330 | TCS PIM 1-1

JAK/STAT Signaling

Pim

Pim1

Cancer

——

491871-58-0

367.1961

C18H11BrN2O2

>98% (HPLC)

DMSO: ≥ 52 mg/mL

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

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

(-20℃)

With Ice Pack

≥ 2 years