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Chemical Structure| 1613724-42-7 Chemical Structure| 1613724-42-7

Structure of HTH-01-015
CAS No.: 1613724-42-7

Chemical Structure| 1613724-42-7

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HTH-01-015 is a selective NUAK1 inhibitor, but not NUAK2, with IC50 of 100 nM, suppressing NUAK1-mediated MYPT1 phosphorylation.

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Product Details of HTH-01-015

CAS No. :1613724-42-7
Formula : C26H28N8O
M.W : 468.55
SMILES Code : O=C1C2=CC3=CC=CC=C3C=C2N(C)C4=NC(NC5=CN(C6CCNCC6)N=C5)=NC(C)=C4N1C
MDL No. :MFCD28167816
InChI Key :CHSDJDLAKKAWCI-UHFFFAOYSA-N
Pubchem ID :78357766

Safety of HTH-01-015

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302
Precautionary Statements:P280-P305+P351+P338

Related Pathways of HTH-01-015

epigenetics
PI3K-AKT

Isoform Comparison

Biological Activity

Target
  • AMPK

    NUAK1 , IC50:100 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
HEK-293 cells 10 μM 16-24 hours Inhibited NUAK1 activity, reduced phosphorylation of MYPT1 at Ser445 PMC3969223
MEFs cells 10 μM 16 hours Inhibited NUAK1 activity, reduced cell proliferation PMC3969223
U2OS cells 10 μM 16 hours Inhibited NUAK1 activity, reduced cell proliferation PMC3969223
U2OS cells 3 μM 1000 minutes Significantly suppressed cells from entering mitosis, an effect comparable to the RO3306 CDK1 inhibitor PMC4109838
U2OS cells 3 μM 8 hours Inhibition of NUAK1 activity reduced the population of cells in S-phase by approximately 50% PMC4109838
Human motor neurons 0.25–32 μM 72 hours To evaluate the neuroprotective effects of HTH-01-015 in ER stress-mediated neurodegeneration. HTH-01-015 did not rescue CPA toxicity at any of the concentrations tested and was toxic to motor neurons at concentrations above 2 μM even in the absence of CPA. PMC7253076

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
C57BL/6J mice CCl4-induced liver fibrosis model Intraperitoneal injection 10 or 20 mg/kg Every other day for 5–8 weeks To evaluate the therapeutic effect of HTH-01-015 on liver fibrosis PMC9655442

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.13mL

0.43mL

0.21mL

10.67mL

2.13mL

1.07mL

21.34mL

4.27mL

2.13mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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