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Chemical Structure| 487021-52-3 Chemical Structure| 487021-52-3
Chemical Structure| 487021-52-3

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CAS No.: 487021-52-3

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AR-A014418 is a selective inhibitor of GSK3β with IC50 of 104 ± 27 nM.

Synonyms: GSK 3β inhibitor VIII; AR 0133418; GSK-3beta Inhibitor VIII.

4.5 *For Research Use Only !

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Product Details of AR-A014418

CAS No. :487021-52-3
Formula : C12H12N4O4S
M.W : 308.31
SMILES Code : O=C(NC1=NC=C([N+]([O-])=O)S1)NCC2=CC=C(OC)C=C2
Synonyms :
GSK 3β inhibitor VIII; AR 0133418; GSK-3beta Inhibitor VIII.
MDL No. :MFCD08277040
InChI Key :YAEMHJKFIIIULI-UHFFFAOYSA-N
Pubchem ID :448014

Safety of AR-A014418

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of AR-A014418

PI3K-AKT
Hedgehog

Isoform Comparison

Biological Activity

Target

  • GSK-3β

    GSK-3β, Ki:38 nM

In Vitro:

Cell Line
Concentration Treated Time Description Reference
Hippocampal neurons 10 μM 1 hour AR-A014418 significantly inhibited AMPA-induced GluR1 receptor internalization by 48%. PMC2895136
A375 20 μM 12 hours To detect the effect of AR-A014418 on PD-L1 expression, it was found that AR-A014418 inhibited PD-L1 expression. PMC10174041
Hela 40 μM 16 hours To detect the effect of AR-A014418 on PD-L1 expression, it was found that AR-A014418 inhibited PD-L1 expression. PMC10174041
IEC-6 cells 10 μM 24 hours To investigate the effect of AR-A014418 on the migration of IEC-6 cells, results showed that AR-A014418 inhibited cell migration under all conditions. PMC11136338
NRCMs 1 μM 24 hours To study the function of eEF2K in DIC, it was found that eEF2K overexpression alleviated DOX-induced cardiomyocyte injury and atrophy PMC11663172
22Rv1 0.25 μM 30 hours AR-A014418 activates AR in the absence of androgens, increasing AR reporter gene activity. PMC2386547
PC3 0.5 μM 4 hours AR-A014418 stimulates nuclear translocation of AR in the absence of androgens. PMC2386547
LUHMES cells 2 μM 6 hours To measure the effect of GSK-3 inhibitors on tau phosphorylation, results showed that AR-A014418 at 2 μM did not significantly reduce tau phosphorylation levels. PMC2078230
LNCaP 0.25 μM 96 hours AR-A014418 stimulates the proliferation of LNCaP cells in the absence of androgens. PMC2386547
primary cultured neurons 33 μM Inhibition of GSK-3β significantly reduced the levels of full-length fractalkine in total cell extracts, mainly affecting the plasma membrane-associated form of the protein. PMC5309299
HEK293 cells 33 μM GSK-3β inhibition led to decreased levels of fractalkine at the plasma membrane, which in turn reduced the levels of soluble fractalkine. PMC5309299

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description Reference
C57BL/6 mice 5-HT2A receptor function model Intraperitoneal injection 10 or 20 mg/kg Single administration To test the effect of AR-A014418 on DOI-induced head-twitch response (HTR) and ear-scratch response (ESR). Results showed that AR-A014418 did not significantly affect the DOI-induced HTR or ESR. PMC6003638
Mice seipin-nKO mice Intraperitoneal injection 1 mg/kg Once daily for 28 days AR-A014418 treatment partially reduced the level of cleaved caspase-3 and alleviated the deficits in motor coordination. PMC5906676
Mice Tail suspension test and forced swim test 30 μmol/kg 14 days AR-A014418 enhanced surface GluR1 levels in the hippocampal region and showed antidepressant-like effects in the tail suspension and forced swim tests. PMC2895136
Rats 12-day old postnatal rat model Oral 30 mg/kg Single dose, duration of 2, 4, 6 hours To evaluate the effect of AR-A014418 on tau phosphorylation in vivo, results showed that AR-A014418 did not significantly reduce tau phosphorylation levels in the cortex or hippocampus at any time point. PMC2078230
C57BL/6 mice acute DIC model intraperitoneal injection 15 mg/kg single injection, lasting 5 days To study the role of eEF2K in DIC, it was found that eEF2K overexpression alleviated DOX-induced cardiac dysfunction and myocardial mass loss PMC11663172
Rabbit Preterm rabbit model of intraventricular hemorrhage Intramuscular injection 20 mg/kg Twice a day for seven days GSK-3 β inhibition accelerated OPC maturation, myelination, and neurological recovery, and reduced microglia infiltration and IL1 β expression PMC6673662
Rats Hindlimb suspension model Intraperitoneal injection 4 mg/kg Once daily for 7 days To investigate the effect of AR-A014418 on ribosome biogenesis and protein synthesis rates in rat soleus muscle under hindlimb suspension conditions. Results showed that AR-A014418 partially attenuated the unloading-induced decline in markers of ribosome biogenesis and protein synthesis rates. PMC8911371

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.24mL

0.65mL

0.32mL

16.22mL

3.24mL

1.62mL

32.43mL

6.49mL

3.24mL
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

References

 

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