WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 406832
Description: HTH-01-015 is a potent and selective inhibitor of NUAK1 (IC50 = 100 nM) and does not affect the activity of a panel of 139 other kinases, including additional AMPK family members. The administration of HTH-01-015 to MEFs (mouse embryonic fibroblasts) significantly inhibits migration in a wound-healing assay to a similar extent as NUAK1-knockout. HTH-01-015 also inhibit proliferation of MEFs to the same extent as NUAK1 knockout and U2OS cells to the same extent as NUAK1 shRNA knockdown. HTH-01-015 impaired the invasive potential of U2OS cells in a 3D cell invasion assay to the same extent as NUAK1 knockdown. HTH-01-015 will serve as useful chemical probes to delineate the biological roles of the NUAK kinases.
MedKoo Cat#: 406832
Chemical Formula: C26H28N8O
Exact Mass: 468.2386
Molecular Weight: 468.565
Elemental Analysis: C, 66.65; H, 6.02; N, 23.91; O, 3.41
Synonym: HTH-01-015; HTH01-015; HTH 01-015; HTH-01015; HTH01015; HTH 01015.
IUPAC/Chemical Name: 4,5,13-trimethyl-2-((1-(piperidin-4-yl)-1H-pyrazol-4-yl)amino)-5,13-dihydro-6H-naphtho[2,3-e]pyrimido[5,4-b][1,4]diazepin-6-one
InChi Key: CHSDJDLAKKAWCI-UHFFFAOYSA-N
InChi Code: InChI=1S/C26H28N8O/c1-16-23-24(31-26(29-16)30-19-14-28-34(15-19)20-8-10-27-11-9-20)32(2)22-13-18-7-5-4-6-17(18)12-21(22)25(35)33(23)3/h4-7,12-15,20,27H,8-11H2,1-3H3,(H,29,30,31)
SMILES Code: CC1=C(N(C)C(C2=CC(C=CC=C3)=C3C=C2N4C)=O)C4=NC(NC5=CN(N=C5)C6CCNCC6)=N1
1: Banerjee S, Zagórska A, Deak M, Campbell DG, Prescott AR, Alessi DR. Interplay
between Polo kinase, LKB1-activated NUAK1 kinase, PP1βMYPT1 phosphatase complex
and the SCFβTrCP E3 ubiquitin ligase. Biochem J. 2014 Jul 15;461(2):233-45. doi:
10.1042/BJ20140408. PubMed PMID: 24785407; PubMed Central PMCID: PMC4109838.
2: Banerjee S, Buhrlage SJ, Huang HT, Deng X, Zhou W, Wang J, Traynor R, Prescott
AR, Alessi DR, Gray NS. Characterization of WZ4003 and HTH-01-015 as selective
inhibitors of the LKB1-tumour-suppressor-activated NUAK kinases. Biochem J. 2014
Jan 1;457(1):215-25. doi: 10.1042/BJ20131152. PubMed PMID: 24171924; PubMed
Central PMCID: PMC3969223.