PT262 free base · Synonyms: PT-262 · PT 262

PT-262 is a potent ROCK inhibitor.

For research use only. Not for human or veterinary use.

Target ROCK ERK CDK Apoptosis

Research area Cancer

Purity >98% Stock Inquire

Data Sheet SDS COA

PT262 structure

CAS No.: 86811-36-1

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
100 mg	USD 420.00	BP-00020-100mg	In stock	Get quote
250 mg	USD 840.00	BP-00020-250mg	In stock	Get quote
500 mg	USD 1,340.00	BP-00020-500mg	In stock	Get quote
1 g	USD 2,150.00	BP-00020-1g	In stock	Get quote
2 g	USD 3,440.00	BP-00020-2g	In stock	Get quote
3 g	USD 4,130.00	BP-00020-3g	In stock	Get quote
5 g	Inquire	BP-00020-5g	In stock	Inquire

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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.

Biological activity

In Vitro PT-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-null 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.

Identifiers

SMILES: O=C1C(Cl)=C(C(=O)C2=CC=CN=C12)N3CCCCC3
InChIKey: XBHXHCMFAUSIKK-UHFFFAOYSA-N

Specifications

MW (average): 276.7180
Formula: C₁₄H₁₃ClN₂O₂
CAS No.: 86811-36-1
Physical state: Solid
Color: Brown to reddish brown
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder 4°C, sealed storage, away from moisture and light ; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO : 100 mg/mL

Documents

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.

[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.

Same target

Search ROCK

Same research area

Search Cancer