Cat. No. Name Size Price Add Cart
KI2341NSC3197265 mg$176
NSC31972625 mg$752

Chemical Characteristic

Product NameNSC319726
SynonymsN/A
CAS No.71555-25-4
Molecular Weight 234.32
FormulaC11H14N4S
Chemical Name1-Azetidinecarbothioic acid [1-(2-pyridinyl)ethylidene]hydrazide
SmilesN1(CCC1)C(=S)N/N=C(\C)/c1ccccn1
Chemical Structure

Biological activities

NSC319726 is a p53R175 mutant reactivator. NSC319726 exhibits growth inhibition in cells expressing p53R175 mutant protein with an IC50 of 8 nM. Treatment of TOV112D cells with NSC319726 decreases the stabilization of the p53 mutant protein. NSC319726 kills p53R172H knockin mice with extensive apoptosis and inhibits xenograft tumor growth in a 175-allele-specific mutant p53-dependent manner.[1] NSC319726 restores p53 activity in a manner dependent on the zinc and redox state, displays specific activity in R172H (equivalent to human R175H) in genetically engineered mice, and selectively inhibits xenograft tumor growth of R175H-mutant p53 cells.[2]

References

[1] Yu X, et al. Allele-specific p53 mutant reactivation. Cancer Cell. 2012, 21(5): 614-625.
[2] Lehmann BD, et al. Targeting mutant p53 in human tumors. J Clin Oncol. 2012, 30(29): 3648-3650.

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