Formulation: A solid
Formal Name: N4-(2-methylpropyl)-N2-[(2-phenyl-4-thiazolyl)methyl]-2,4-pyrimidinediamine
Purity: ≥98%
Formula Markup: C18H21N5S
CAS Number: 1262770-73-9
Notes: KHS-101 is an inhibitor of heat shock protein 60 (Hsp60), also known as HSPD1, and an inducer of neuronal differentiation.{51593,51592} 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.{51593} 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.{51592} 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.{51593}
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