NSC668394 free base · Synonyms: NSC-668394 · NSC 668394

NSC668394 is a potent ezrin phosphorylation inhibitor.

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

Target PKC

Research area Cancer

Purity >98% Stock Inquire

Data Sheet SDS COA

NSC668394 structure

CAS No.: 382605-72-3

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
50 mg	USD 550.00	BP-02168-50mg	In stock	Get quote
100 mg	USD 880.00	BP-02168-100mg	In stock	Get quote
250 mg	USD 1,750.00	BP-02168-250mg	In stock	Get quote
500 mg	USD 2,700.00	BP-02168-500mg	In stock	Get quote

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Description

NSC668394 is a potent ezrin (Thr567) phosphorylation inhibitor, with a Kd of 12.59 μM. NSC668394 inhibit ezrin T567 phosphorylation caused by PKCΙ primarily via their binding to ezrin. NSC668394 can be used to prevent tumor metastasis.

Biological activity

In Vitro NSC668394 (10 μM; pretreated for 15 min) inhibits ezrin T567 phosphorylation (IC50=8.1 μM) and actin binding in vitro. NSC668394 (1-10 μM; 2-6 h) inhibits ezrin-mediated invasion by K7M2 osteosarcoma (OS) cells on the HUVEC monolayer. NSC668394 (20 μM) causes significant decrease in growth in JM1 and JM2 rat hepatoma cell lines. NSC668394 (10 μM) reduces cell motility phenotypes in zebrafish. In Vivo NSC668394 (0.226 mg/kg/day; i.p. 5-days a week) inhibits ezrin-dependent in vivo OS metastatic growth in mouse lung.

Identifiers

SMILES: O=C(C=C1NCCC2=CC(Br)=C(O)C(Br)=C2)C3=C(N=CC=C3)C1=O
InChIKey: OHPHDPYJEHZGDE-UHFFFAOYSA-N

Specifications

MW (average): 452.0970
Formula: C₁₇H₁₂Br₂N₂O₃
CAS No.: 382605-72-3
Physical state: Solid
Color: Orange to red
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 -20℃ 3 years; 4℃, 2 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO : 50 mg/mL

Documents

References

[1]. Bulut G, et, al. Small molecule inhibitors of ezrin inhibit the invasive phenotype of osteosarcoma cells. Oncogene. 2012 Jan 19;31(3):269-81.

[2]. Xue Y, et, al. Phosphorylated Ezrin (Thr567) Regulates Hippo Pathway and Yes-Associated Protein (Yap) in Liver. Am J Pathol. 2020 Jul;190(7):1427-1437.

[3]. Çelik H, et, al. Ezrin Inhibition Up-regulates Stress Response Gene Expression. J Biol Chem. 2016 Jun 17;291(25):13257-70.

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