PT-262 (C09-1164-700)

PT-262 is a potent ROCK inhibitor with an IC 50 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 activityIn VitroPT-262 (5-40 μM; 24 h) induces cytotoxicity and proliferation inhibition in human lung cancer cells. PT-262 (2-20 μM; 4-24 h) induces caspase-3 activation, mitochondrial dysfunction and apoptosis in lung cancer cells. PT-262 (10-20 μM; 24 h) induces the accumulation of G2/M phases in both the p53-wild type and p53- lung cancer cells, and inhibits the phosphorylation of CDC2 proteins. PT-262 (0-10 μM; 24 h) represses ERK phosphorylation in lung cancer cells. PT-262 (2 μM; 24 h) induces the cytoskeleton alteration and cell elongation in lung carcinoma A549 cells. PT-262 (2-10 μM; 6 h) significantly blocks the cell migration in a concentration-dependent manner. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: A549 cells Concentration: 5-40 μM Incubation Time: 24 h Result: Reduced the cell viability via a concentration-dependent manner in A549 cells. The IC 50 value toward human normal lung fibroblast was >20 μM. Apoptosis AnalysisCell Line: A549 cells Concentration: 2-20 μM Incubation Time: 4-24 h Result: The apoptotic cells were increased after treatment at 10 μM for 8-24 h. The active forms of caspase-3 (12 and 17 kD) were induced following treatment with 2-20 μM for 24 h. Cell Cycle AnalysisCell Line: A549 and H1299 cells Concentration: 10-20 μM Incubation Time: 24 h Result: Significantly decreased the G1 fractions while increased the G2/M fractions in both A549 and H1299 cells with 10 μM for 24 h. Decreased the protein levels of cyclin B1 and phospho-CDC2 at Thr14, Tyr15, and Thr161 via a concentration-dependent manner in A549 cells. Western Blot AnalysisCell Line: A549 cells Concentration: 0-10 μM Incubation Time: 24 h Result: Significantly inhibited the phosphorylation of ERK.Form:SolidIC50& Target:ROCK|5 μM (IC|50|)|ERK|CDK2. Specifications and Purity: 99%. Molecular Formula: C14H13ClN2O2. Molecular Weight: 276.72. PubChem CID: 12424014. Isomeric SMILES: C1CCN(CC1)C2=C(C(=O)C3=C(C2=O)C=CC=N3)Cl.