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KHS101 hydrochloride
- Parent CAS: 1262770-73-9
- Soluble in water and DMSO
- MF: C18H21N5S.HCl
- MW: 375.92
Description
KHS101 hydrochloride is a brain-penetrable TACC3 inhibitor known to enhance neuronal differentiation (EC50 value of 1 μM in cultured rat NPCs) and inhibit cell cycle progression and proliferation. KHS101 hydrochloride works indirectly on HIF complex formation by destabilizing both TACC3 and the HIF component HIF-1α. KHS101 hydrochloride suppresses proliferation, migration, and invasive capabilities of breast cancer cells, EMT process, and mammosphere forming capability, alters cell cycle progression, and induces apoptosis.
More Information
| Parent CAS No. | 1262770-73-9 |
|---|---|
| Chemical Name | N4-Isobutyl-N2-((2-phenylthiazol-4-yl)methyl)pyrimidine-2,4-diamine hydrochloride |
| SMILES | C1C=CC(C2SC=C(CNC3N=C(NCC(C)C)C=CN=3)N=2)=CC=1.Cl |
| MFCD | MFCD18206916 |
| InChi | InChI=1S/C18H21N5S.ClH/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);1H |
| InChiKey | INVQHPQJFRKGIO-UHFFFAOYSA-N |
| CID | 90488983 |
| Short Description | TACC3 inhibitor |
References
- H. Wurdak et al. A small molecule accelerates neuronal differentiation in the adult rat. Proc Natl Acad Sci U S A. 2010 Sep 21;107(38):16542-7.
- Y Guo et al. 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
- L Campo et al. Inhibition of TACC3 by a small molecule inhibitor in breast cancer. Biochem Biophys Res Commun. 2018 Apr 15;498(4):1085-1092.
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