Home PI3K/Akt/mTOR AMPK inhibitor HTH-01-015

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HTH-01-015 AMPK inhibitor

Cat.No.S7318

HTH-01-015 is a potent and selective NUAK1 inhibitor with IC50 of 100 nM, >100-fold selectivity over NUAK2.
HTH-01-015 AMPK inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 468.55

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Chemical Information, Storage & Stability

Molecular Weight 468.55 Formula

C26H28N8O

 Storage (From the date of receipt)
CAS No. 1613724-42-7 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles CC1=C2C(=NC(=N1)NC3=CN(N=C3)C4CCNCC4)N(C5=CC6=CC=CC=C6C=C5C(=O)N2C)C

Solubility

In vitro
Batch:

DMSO : 93 mg/mL (198.48 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 47 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Mechanism of Action

Targets/IC50/Ki
NUAK1 [1]
100 nM
In vitro
In HEK-293 cells express NUAK1 as well as NUAK2, HTH-01-015 suppresses NUAK1-mediated MYPT1 phosphorylation. This compound suppresses cell migration In NUAK1+/+ MEFs, and inhibit U2OS cell invasion. Moreover, it inhibits cell proliferation in both cell lines. [1] This inhibitor markedly restricted cells from entering into mitosis in U2OS cells. [2]
Kinase Assay
Kinase activity assays
In vitro activities of purified GST–NUAK1 and GST–NUAK1[A195T] are measured using Cerenkov counting of incorporation of radioactive 32P from [γ-32P]ATP into Sakamototide substrate peptide. Reactions are carried out in a 50 μL reaction volume for 30 min at 30°C and reactions are terminated by spotting 40 μL of the reaction mix on to P81 paper and immediately immersing in 50 mM orthophosphoric acid. Samples are washed three times in 50 mM orthophosphoric acid followed by a single acetone rinse and air drying. The kinase-mediated incorporation of [γ-32P]ATP into Sakamototide is quantified by Cerenkov counting. One unit of activity is defined as that which catalyses the incorporation of 1 nmol of [32P]phosphate into the substrate over 1 h.
References

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