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Product name : TCS PIM-1
Item : CR1800
Price : 200mg, $659;500mg, $1150; 1g, $1595; 2g, $2355
contact : Send inquiry to: info@acesobio.com
CAS : 491871-58-0
Molecular Weight : 367.2
Formula : C₁₈H₁₁BrN₂O₂
Storage : at -20°C
Additional information : We offer significant discount for bulky quantity order
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 Chemical Information
M.Wt 367.2 Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Formula C18H11BrN2O2
CAS No 491871-58-0

Soluble in DMSO (100 mM)

Biological Activity of TCS PIM-1 1


TCS PIM-1 1(sc-204330) is a potent and selective ATP-competitive Pim-1 kianse inhibitor with IC50 of 50 nM, displays good selectivity over Pim-2 and MEK1/MEK2(IC50s >20,000 nM).
IC50 value: 50 nM [1]
Target: Pim-1
TCS PIM-1 1 bound convincingly within the ATP-binding site of Pim-1 suggesting an ATP-competitive inhibitory mechanism. Preliminary data further suggested that 1 lacked in vitro inhibitory activity toward related serine/threonine kinases Pim-2 and MEK1/2 (IC50 > 20 lM). 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.


[1]. Cheney IW, et al. Identification and structure-activity relationships of substituted pyridones as inhibitors of Pim-1 kinase. Bioorg Med Chem Lett. 2007 Mar 15;17(6):1679-83.
A novel series of highly potent substituted pyridone Pim-1 kinase inhibitors is described. Structural requirements for in vitro activity are outlined as well as a complex crystal structure with the most potent Pim-1 inhibitor reported (IC(50)=50 nM). A hydrogen bond matrix involving the Pim-1 inhibitor, two water molecules, and the catalytic core, together with a potential weak hydrogen bond between an aromatic hydrogen on the R(1) phenyl ring and a main-chain carbonyl of Pim-1, accounts for the overall potency of this inhibitor.

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