Chemical Name: 5,13-Dihydro-4,5,13-trimethyl-2-[[1-(4-piperidinyl)-1H-pyrazol-4-yl]amino]-6H-naphtho[2,3-e]pyrimido[5,4-b][1,4]diazepin-6-one
Purity: ≥98% (HPLC)
Biological Activity
Technical Data
Solubility
Calculators
Datasheets
References
Biological Activity
Potent and selective NUAK1 inhibitor (IC50 = 100 nM). Exhibits no significant inhibition against a panel of 139 kinases, including ten AMPK family members. Inhibits NUAK1-mediated MYPT1 phosphorylation. Also inhibits cell proliferation in U2OS cells in vitro, to a similar extent as NUAK1 knockdown models.
Licensing Information
Sold under license from Dana-Farber Cancer Institute
Compound Libraries
HTH 01-015 is also offered as part of the
Tocriscreen Plus and Tocriscreen Kinase Inhibitor Toolbox II. Find out more about compound libraries available from Tocris.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
Solvent
Max Conc. mg/mL
Max Conc. mM
Solubility
DMSO
46.85
100
ethanol
46.85
100
Preparing Stock Solutions
The following data is based on the product molecular weight 468.55. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass
1 mg
5 mg
10 mg
1 mM
2.13 mL
10.67 mL
21.34 mL
5 mM
0.43 mL
2.13 mL
4.27 mL
10 mM
0.21 mL
1.07 mL
2.13 mL
50 mM
0.04 mL
0.21 mL
0.43 mL
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Product Datasheets
Certificate of Analysis / Product Datasheet
Safety Datasheet
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References
References are publications that support the products' biological activity.
Banerjeeet al (2014) Characterization of WZ4003 and HTH-01-015 as selective inhibitors of the LKB1-tumour-suppressor-activated NUAK kinases. Biochem J. 457 215 PMID: 24171924