HTH 01-015

Pricing Availability   Qty
Description: Potent and selective NUAK1 inhibitor
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)
Literature (1)
Pathways (1)

Biological Activity for HTH 01-015

HTH 01-015 is a 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 for HTH 01-015

HTH 01-015 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Kinase Inhibitor Library. Find out more about compound libraries available from Tocris.

Technical Data for HTH 01-015

M. Wt 468.55
Formula C26H28N8O
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 1613724-42-7
PubChem ID 78357766
Smiles O=C1N(C)C2=C(N=C(NC3=CN(C4CCNCC4)N=C3)N=C2C)N(C)C5=CC6=CC=CC=C6C=C51

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for HTH 01-015

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 46.85 100
ethanol 46.85 100

Preparing Stock Solutions for HTH 01-015

The following data is based on the product molecular weight 468.55. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
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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References for HTH 01-015

References are publications that support the biological activity of the product.

Banerjee et 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

If you know of a relevant reference for HTH 01-015, please let us know.

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Keywords: HTH 01-015, HTH 01-015 supplier, HTH01-015, potent, selective, NUAK1, family, SNF1-like, kinase-1, inhibitors, inhibits, NUAK, 5622, Tocris Bioscience

Citations for HTH 01-015

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Literature in this Area

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Pathways for HTH 01-015

AMPK Signaling Pathway

AMPK Signaling Pathway

AMPK signaling pathway plays an important role in the cellular reponse to low levels of available ATP, often caused by stresses such as heat shock, ischemia or hypoxia.
Akt Signaling Pathway

Akt Signaling Pathway

The Akt signaling pathway plays a key role in the mediation of protein synthesis, metabolism, proliferation and cell cycle progression. It may be referred to as a 'prosurvival' pathway.