A p53 reactivator; selectively inhibits growth of human tumor cell lines containing mutant p53 over those containing wild-type p53 (IC50s = 0.1-1 and >10 μM

NSC 319726 – 25 mg

Brand:
Cayman
CAS:
71555-25-4
Storage:
-20
UN-No:
Non-Hazardous - /

NSC 319726 is a reactivator of p53R175, a p53 conformational mutant that cannot bind DNA.{36321} It selectively inhibits growth of human tumor cell lines containing mutant p53 over those containing wild-type p53 (IC50s = 0.1-1 and >10 μM, respectively). NSC 319726 induces apoptosis in TOV112D (p53R175H), but not OVCAR3 (p53R248W) or SKOV3 (p53-/-), cells at a concentration of 1 μM. It restores a wild-type conformation to human p53175 and mouse p53R172 mutant proteins and induces expression of p53 target genes in TOV112D cells. In vivo, NSC 319726 (1 mg/kg) inhibits tumor growth in TOV112D, but not H460 (p53+/+), mouse xenograft model. NSC 319726 also has broad-spectrum antifungal activity (MIC50s = 0.1-2 μg/ml against a panel of pathogenic fungi) with >800-fold selectivity for fungi over human HUH-7 and HepG2 cells.{36322}  

 

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SKU: 23701 - 25 mg Category:

Description

A p53 reactivator; selectively inhibits growth of human tumor cell lines containing mutant p53 over those containing wild-type p53 (IC50s = 0.1-1 and >10 μM, respectively); induces apoptosis in TOV112D (p53R175H), but not OVCAR3 (p53R248W) or SKOV3 (p53-/-), cells at a concentration of 1 μM; restores a wild-type conformation to human p53175 and mouse p53R172 mutant proteins and induces expression of p53 target genes in TOV112D cells; inhibits tumor growth in TOV112D, but not H460 (p53+/+), mouse xenograft model when administered at a dose of 1 mg/kg; has broad-spectrum antifungal activity (MIC50s = 0.1-2 μg/ml against a panel of pathogenic fungi) with >800-fold selectivity for fungi over human HUH-7 and HepG2 cells

Formal name: 2-[1-(2-pyridinyl)ethylidene]hydrazide, 1-azetidinecarbothioic acid

Synonyms: 

Molecular weight: 234.3

CAS: 71555-25-4

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Antifungals||Product Type|Biochemicals|Small Molecule Activators||Research Area|Cancer|Cell Signaling|p53 Signaling||Research Area|Cancer|Transcription Factors|p53||Research Area|Immunology & Inflammation

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