KHS-101

KHS-101 is an inhibitor of heat shock protein 60 (Hsp60), also known as HSPD1, and an inducer of neuronal differentiation. It inhibits the refolding activity of the complex of Hsp60 with the co-chaperone Hsp10, also known as HSPE1, in a cell-free assay (IC50 = 14.4 µM) and induces autophagy in GBM1 glioblastoma cells. KHS-101 induces differentiation of primary rat hippocampal neural progenitor cells (NPCs) into neurons (EC50 = ~1 µM) and inhibits BMP4-induced differentiation induced of primary rat hippocampal NPCs into astrocytes when used at a concentration of 5 µM. It increases nuclear localization of the transforming acidic coiled-coil containing protein 3 (Tacc3) target aryl hydrocarbon receptor nuclear translocator 2 (Arnt2) in HEK293T cells expressing the rat proteins when used at a concentration of 5 µM. KHS-101 reduces tumor burden and increases survival in a patient-derived xenograft (PDX) mouse model of giant cell glioblastoma.Formal Name: N4-(2-methylpropyl)-N2-[(2-phenyl-4-thiazolyl)methyl]-2,4-pyrimidinediamine. CAS Number: 1262770-73-9. Molecular Formula: C18H21N5S. Formula Weight: 339.5. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMF: 10 mg/ml, DMSO: 10 mg/ml, Ethanol: Slightly soluble. SMILES: CC(C)CNC1=NC(NCC2=CSC(C3=CC=CC=C3)=N2)=NC=C1. InChi Code: InChI=1S/C18H21N5S/c1-13(2)10-20-16-8-9-19-18(23-16)21-11-15-12-24-17(22-15)14-6-4-3-5-7-14/h3-9,12-13H,10-11H2,1-2H3,(H2,19,20,21,23). InChi Key: DGRJOOOHPBSAHD-UHFFFAOYSA-N.