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NSC668394

SKU: orb2655717

Description

NSC668394 (NSC 668394) is a small molecule inhibitor of ezrin, directly bind to ezrin with Kd of 12.59 uM; inhibits T567 phosphorylation and actin binding of endogenous ezrin at 10 μM without altering cellular ezrin levels, inhibits PKC-Ι phosphorylation of recombinant ezrin with IC50 of 8.1 uM; inhibits ezrin-mediated invasion of K7M2 OS cells, inhibits cell motility during zebrafish and Xenopus embryonic development; also inhibits ezrin-dependent in vivo OS metastatic growth in mouse lung.

Images & Validation

Key Properties

CAS Number382605-72-3
MW452.102
Purity>98% (HPLC)
FormulaC17H12Br2N2O3
SMILESO=C(C=C1NCCC2=CC(Br)=C(O)C(Br)=C2)C3=C(N=CC=C3)C1=O
TargetEzrin
SolubilityIn Vitro: DMSO : 50 mg/mL (110.60 mM)

Bioactivity

In Vivo
Animal model: Female BALB/c and SCID/Beige mice were injected with K7M2 or MNNG-HOS tumor cells. Dosage: 0.226 mg/kg/day. Administration: i.p. 5-days a week for 66 days. Result: Showed an increase in survival. Decreased the number of the green fluorescent protein (GFP)-expressing metastatic foci in the lung tissues.
In Vitro
Western blot analysis. Cell line: K7M2 OS cells. Concentration: 10 μM. Incubation time: 6 hours. Result: Inhibited T567 phosphorylation and actin binding of endogenous ezrin without altering cellular ezrin levels.

Storage & Handling

StorageStorage temperature: -20°C. Stability: ≥ 2 years
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

NSC 668394 | NSC-668394

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Protocol Information