MedChemExpress LLC (MCE)

MedChemExpress - Model PT-262 - 86811-36-1

PT-262 is a potent ROCK inhibitor with an IC50 value of around 5 μM. PT-262 induces the loss of mitochondrial membrane potential and elevates the caspase-3 activation and apoptosis. PT-262 inhibits the ERK and CDC2 phosphorylation via a p53-independent pathway. PT-262 blocks cytoskeleton function and cell migration. PT-262 has anti-cancer activity[1][2].

PT-262

MCE China：PT-262

Brand：MedChemExpress (MCE)

Cat. No.HY-100035

CAS：86811-36-1

Purity：99.21%

Storage：4°C, sealed storage, away from moisture and light *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Shipping：Room temperature in continental US; may vary elsewhere.

Description：PT-262 is a potent ROCK inhibitor with an IC50 value of around 5 μM. PT-262 induces the loss of mitochondrial membrane potential and elevates the caspase-3 activation and apoptosis. PT-262 inhibits the ERK and CDC2 phosphorylation via a p53-independent pathway. PT-262 blocks cytoskeleton function and cell migration. PT-262 has anti-cancer activity.

In Vitro：PT-262 (5-40 μM; 24 h) induces cytotoxicity and proliferation inhibition in human lung cancer cells[1]. PT-262 (2-20 μM; 4-24 h) induces caspase-3 activation, mitochondrial dysfunction and apoptosis in lung cancer cells[1]. PT-262 (10-20 μM; 24 h) induces the accumulation of G2/M phases in both the p53-wild type and p53-null lung cancer cells, and inhibits the phosphorylation of CDC2 proteins[1]. PT-262 (0-10 μM; 24 h) represses ERK phosphorylation in lung cancer cells[1]. PT-262 (2 μM; 24 h) induces the cytoskeleton alteration and cell elongation in lung carcinoma A549 cells[2]. PT-262 (2-10 μM; 6 h) significantly blocks the cell migration in a concentration-dependent manner[2].

IC50 & Target：ROCK 5 μM (IC50) ERK CDK2

References：

[1]. Tzu-Sheng Hsu, et al. 7-Chloro-6-piperidin-1-yl-quinoline-5,8-dione (PT-262), a novel synthetic compound induces lung carcinoma cell death associated with inhibiting ERK and CDC2 phosphorylation via a p53-independent pathway. Cancer Chemother Pharmacol. 2008 Oct;62(5):799-808. [Content Brief]

[2]. Chih-Chien Tsai, et al. 7-Chloro-6-piperidin-1-yl-quinoline-5,8-dione (PT-262), a novel ROCK inhibitor blocks cytoskeleton function and cell migration. Biochem Pharmacol. 2011 Apr 1;81(7):856-65. [Content Brief]

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