Description
KHS-101 is a selective inducer of neuronal differentiation. KHS101 induces neuronal differentiation in cultured hippocampal neural progenitor cells (NPCs) by interacting with TACC3 (EC50 ~1 μM). KHS101 disrupts energy metabolism in human glioblastoma cells and reduces tumor growth in mice. KHS101 promoted tumor cell death in diverse GBM cell models. KHS101 exerted cytotoxic effects by disrupting the mitochondrial chaperone heat shock protein family D member 1 (HSPD1). In GBM cells, KHS101 promoted aggregation of proteins regulating mitochondrial integrity and energy metabolism.
Product information
CAS Number: 1262770-73-9
Molecular Weight: 339.46
Formula: C18H21N5S
Chemical Name: N4-isobutyl-N2-((2-phenylthiazol-4-yl)methyl)pyrimidine-2,4-diamine
Smiles: CC(C)CNC1=CC=NC(NCC2=CSC(=N2)C2C=CC=CC=2)=N1
InChiKey: DGRJOOOHPBSAHD-UHFFFAOYSA-N
InChi: 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)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: To be determined
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
References:
- Guo Y, Partch CL, Key J, Card PB, Pashkov V, Patel A, Bruick RK, Wurdak H, Gardner KH. Regulating the ARNT/TACC3 axis: multiple approaches to manipulating protein/protein interactions with small molecules. ACS Chem Biol. 2013 Mar 15;8(3):626-35. doi: 10.1021/cb300604u. Epub 2012 Dec 26. PMID: 23240775; PMCID: PMC3600089.
- Polson ES, Kuchler VB, Abbosh C, Ross EM, Mathew RK, Beard HA, da Silva B, Holding AN, Ballereau S, Chuntharpursat-Bon E, Williams J, Griffiths HBS, Shao H, Patel A, Davies AJ, Droop A, Chumas P, Short SC, Lorger M, Gestwicki JE, Roberts LD, Bon RS, Allison SJ, Zhu S, Markowetz F, Wurdak H. KHS101 disrupts energy metabolism in human glioblastoma cells and reduces tumor growth in mice. Sci Transl Med. 2018 Aug 15;10(454):eaar2718. doi: 10.1126/scitranslmed.aar2718. PMID: 30111643.
Products are for research use only. Not for human use.
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