KRIBB11

KRIBB11 is an inhibitor of heat shock factor 1 (Hsf1) with an IC50 value of 1.2 µM in a luciferase reporter assay. It blocks heat shock-induced Hsp70, Hsp40, and Hsp27 mRNA expression and down-regulates protein expression of the Hsf1 target proteins Hsp70 and Hsp27 in HCT116 cells in a dose-dependent manner. KRIBB11 specifically binds to Hsf1 over other Hsf1-associated proteins, lacking activity at heat shock protein 90 (Hsp90), Hsf2, and Cdk9 in an in vitro pull-down assay. It inhibits growth of HCT116, Mia-PaCa-2, SW620, HT-29, A549, and MDA-MB-231 cancer cell lines (IC50s = 3-8 µM) via induction of cell cycle arrest at the G2/M phase and apoptosis. In vivo, administration of KRIBB11 decreases tumor growth in a mouse HCT116 xenograft model. KRIB11 administration also attenuates dengue virus progression and reduces mortality without affecting bodyweight in infected mice.Formal Name: N2-1H-indazol-5-yl-N6-methyl-3-nitro-2,6-pyridinediamine. CAS Number: 342639-96-7. Molecular Formula: C13H12N6O2. Formula Weight: 284.3. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, DMSO:PBS(pH 7.2) (1:4): 0.2 mg/ml, Ethanol: 1 mg/ml, PBS (pH 7.2): slightly soluble. lambdamax: 242, 294, 418 nm. SMILES: CNC1=NC(NC2=CC=C(NN=C3)C3=C2)=C([N+]([O-])=O)C=C1. InChi Code: 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). InChi Key: NDJJEQIMIJJCLL-UHFFFAOYSA-N.