Inhibitors, Agonists, Screening Libraries
https://www.sodocs.net/doc/3e12218504.html, Data Sheet
BIOLOGICAL ACTIVITY:
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.
References:
[1]. Cheney IW, et al. Identification and structure–activity relationships of substituted pyridones as inhibitors of Pim–1 kinase. Bioorg Med Chem Lett. 2007Mar 15;17(6):1679–83.
Product Name:
TCS PIM–1 1Cat. No.:
HY-18086CAS No.:
491871-58-0Molecular Formula:
C 18H 11BrN 2O 2Molecular Weight:
367.20Target:
Pim Pathway:
JAK/STAT Signaling Solubility:
DMSO: ≥ 52 mg/mL
Caution: Product has not been fully validated for medical applications. For research use only.
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https://www.sodocs.net/doc/3e12218504.html,