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KRIBB11
- Soluble in DMSO
- MF: C13H12N6O2
- MW: 284.27
Description
HSF1 inhibitor (IC50 value 1.2 µM for inhibition of heat shock-induced luciferase activity). KRIBB11 blocks the induction of HSF1 downstream target proteins such as HSP27 and HSP70, and induces growth arrest and apoptosis in HCT-116 cells. KRIBB11 inhibits HSF1-dependent recruitment of positive transcription elongation factor b (p-TEFb) to the hsp70 promoter, and tumor growth is inhibited without body weight loss upon intraperitoneal treatment of nude mice with KRIBB11. KRIBB11 enhances the cytotoxicity of nocodazole and parbendazole.
More Information
| Parent CAS No. | 342639-96-7 |
|---|---|
| Chemical Name | N2-(1H-indazol-5-yl)-N6-methyl-3-nitropyridine-2,6-diamine |
| SMILES | C1C([N+]([O-])=O)=C(NC2C=C3C=NNC3=CC=2)N=C(NC)C=1 |
| MFCD | N.A. |
| InChi | InChI=1S/C13H12N6O2/c1-14-12-5-4-11(19(20)21)13(17-12)16-9-2-3-10-8(6-9)7-15-18-10/h2-7H,1H3,(H,15,18)(H2,14,16,17) |
| InChiKey | NDJJEQIMIJJCLL-UHFFFAOYSA-N |
| CID | 69894253 |
| Short Description | HSF1 inhibitor |
References
- YL Yoon et al. KRIBB11 inhibits HSP70 synthesis through inhibition of heat shock factor 1 function by impairing the recruitment of positive transcription elongation factor b to the hsp70 promoter. J Biol Chem. 2011 Jan 21;286(3):1737-47.
- CT Wales et al. ERK-dependent phosphorylation of HSF1 mediates chemotherapeutic resistance to benzimidazole carbamates in colorectal cancer cells. Anticancer Drugs. 2015 Jul;26(6):657-66.
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