HTH-01-015 - CAS 1613724-42-7
Catalog number: 1613724-42-7
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C26H28N8O
Molecular Weight:
468.55
COA:
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Targets:
AMPK
Description:
HTH-01-015 is a potent and selective inhibitor of NUAK1 with IC50 of 100 nM, does not significantly inhibit NUAK2 (IC50 of >10 μM).
Purity:
>98%
Synonyms:
HTH 01 015
MSDS:
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InChIKey:
CHSDJDLAKKAWCI-UHFFFAOYSA-N
InChI:
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)
Canonical SMILES:
CC1=C2C(=NC(=N1)NC3=CN(N=C3)C4CCNCC4)N(C5=CC6=CC=CC=C6C=C5C(=O)N2C)C
1.Characterization of WZ4003 and HTH-01-015 as selective inhibitors of the LKB1-tumour-suppressor-activated NUAK kinases.
Banerjee S1, Buhrlage SJ, Huang HT, Deng X, Zhou W, Wang J, Traynor R, Prescott AR, Alessi DR, Gray NS. Biochem J. 2014 Jan 1;457(1):215-25. doi: 10.1042/BJ20131152.
The related NUAK1 and NUAK2 are members of the AMPK (AMP-activated protein kinase) family of protein kinases that are activated by the LKB1 (liver kinase B1) tumour suppressor kinase. Recent work suggests they play important roles in regulating key biological processes including Myc-driven tumorigenesis, senescence, cell adhesion and neuronal polarity. In the present paper we describe the first highly specific protein kinase inhibitors of NUAK kinases namely WZ4003 and HTH-01-015. WZ4003 inhibits both NUAK isoforms (IC50 for NUAK1 is 20 nM and for NUAK2 is 100 nM), whereas HTH-01-015 inhibits only NUAK1 (IC50 is 100 nM). These compounds display extreme selectivity and do not significantly inhibit the activity of 139 other kinases that were tested including ten AMPK family members. In all cell lines tested, WZ4003 and HTH-01-015 inhibit the phosphorylation of the only well-characterized substrate, MYPT1 (myosin phosphate-targeting subunit 1) that is phosphorylated by NUAK1 at Ser(445).
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CAS 1613724-42-7 HTH-01-015

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