299421-08-2
Chemical Structure
NSC-368262
- CAS No.: 299421-08-2
- Formula:C22H22N2O6
- Molecular Weight:410.43
IUPAC Name: 6-((pyridin-2-ylamino)(3,4,5-trimethoxyphenyl)methyl)benzo[d][1,3]dioxol-5-ol
InChIKey: LAMGRAMZRMRRMH-UHFFFAOYSA-N
SMILES: OC=1C=C2OCOC2=CC1C(NC3=NC=CC=C3)C4=CC(OC)=C(OC)C(OC)=C4
Biological Activity: NSC-368262 is a STAT3 inhibitor. NSC-368262 selectively alkylates and covalently modifies STAT3 Cys468 at the DNA-binding interface of STAT3, blocks the DNA-binding activity of STAT3, and inhibits the phosphorylation of STAT3. NSC-368262 blocks the accumulation of activated STAT3 in the nucleus of cancer cells, induces PARP cleavage and apoptosis in cells, and inhibits tumor growth in mouse models. NSC-368262 can be used in research related to breast cancer and cervical cancer[1][2].
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NSC-368262 | NSC-368262 is a STAT3 inhibitor. NSC-368262 selectively alkylates and covalently modifies STAT3 Cys468 at the DNA-binding interface of STAT3, blocks the DNA-binding activity of STAT3, and inhibits the phosphorylation of STAT3. NSC-368262 blocks the accumulation of activated STAT3 in the nucleus of cancer cells, induces PARP cleavage and apoptosis in cells, and inhibits tumor growth in mouse models. NSC-368262 can be used in research related to breast cancer and cervical cancer. | |||||||||||||||||||||
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References
- [1]. Buettner R, et al. Alkylation of cysteine 468 in Stat3 defines a novel site for therapeutic development. ACS Chem Biol. 2011;6(5):432-443. [Content Brief]
- [2]. Huang Q, et al. Revisiting signal transducer and activator of transcription 3 (STAT3) as an anticancer target and its inhibitor discovery: Where are we and where should we go?. Eur J Med Chem. 2020;187:111922. [Content Brief]
