1262770-73-9
Chemical Structure
KHS101
- CAS No.: 1262770-73-9
- Formula:C18H21N5S
- Molecular Weight:339.46
IUPAC Name: N4-isobutyl-N2-((2-phenylthiazol-4-yl)methyl)pyrimidine-2,4-diamine
InChIKey: DGRJOOOHPBSAHD-UHFFFAOYSA-N
SMILES: CC(C)CNC1=NC(NCC2=CSC(C3=CC=CC=C3)=N2)=NC=C1
Biological Activity: KHS101 is a blood-brain barrier-penetrant anticancer agent that primarily functions by inhibiting HSPD1 (IC50 = 14.4 μM) and TACC3 across different cellular backgrounds. KHS101 promotes the aggregation of HSPD1 with client proteins, destabilizes TACC3, and reduces the levels of TACC3, Aurora A and PLK1. KHS101 induces autophagy, apoptosis, cell cycle exit and neuronal differentiation; it suppresses cancer cell growth, motility, EMT and stemness; it also impairs mitochondrial bioenergetics and glycolysis in glioblastoma cells. KHS101 can be used in research related to glioblastoma multiforme and breast cancer[1][2][3].
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KHS101 | KHS101 is a blood-brain barrier-penetrant anticancer agent that primarily functions by inhibiting HSPD1 (IC50 = 14.4 μM) and TACC3 across different cellular backgrounds. KHS101 promotes the aggregation of HSPD1 with client proteins, destabilizes TACC3, and reduces the levels of TACC3, Aurora A and PLK1. KHS101 induces autophagy, apoptosis, cell cycle exit and neuronal differentiation; it suppresses cancer cell growth, motility, EMT and stemness; it also impairs mitochondrial bioenergetics and glycolysis in glioblastoma cells. KHS101 can be used in research related to glioblastoma multiforme and breast cancer. | |||||||||||||||||||||
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References
- [1]. Polson ES, et al. KHS101 disrupts energy metabolism in human glioblastoma cells and reduces tumor growth in mice. Sci Transl Med. 2018;10(454):eaar2718. [Content Brief]
- [2]. Campo L, et al. Inhibition of TACC3 by a small molecule inhibitor in breast cancer. Biochem Biophys Res Commun. 2018;498(4):1085-1092. [Content Brief]
- [3]. Wurdak H, et al. A small molecule accelerates neuronal differentiation in the adult rat. Proc Natl Acad Sci U S A. 2010;107(38):16542-16547. [Content Brief]
