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NUAK1-IN-2 | NUAK1-IN-2 : Inhibitor of NUAK1
RATINGS:
Cellular Use: (0 reviews)

In Model Organisms: (0 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
NUAK1
  • IC50:3.2 nM
  • IC50:100 nM
Inhibitor
up to 1 uM

Selectivity

In Vitro Selectivity Assessment
Selectivity Assessment Description:
9 fold selective over NUAK2 (IC50 30 nM ADP-Glo Assay)
In Vitro Selectivity Assessment
Potency Assay Off-Target:
ADP-Glo Assay
Selectivity Assessment Description:
Selectivity assessed over MARK1 (2858x), MARK2 (4898x), MARK3 (1905x), MARK4 (3981x) and AMPKA (2818 ...
In Vitro Selectivity Assessment
Potency Assay Off-Target:
Kinase selectivity screening at 1 uM against a general kinase panel of 140 targets in radiometric fi ...

Potency
Cellular
In Vitro

NUAK1

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/acsmedchemlett.4c00579

In Vivo Validations

Mouse
Dose: 5 mg/Kg
Route of delivery: Intraperitoneal
Plasma half life: 0.7 h
Cmax: 220 ng/mL [Brain] at 30 min
Area Under the Curve:: 365 hr·ng/mL
Target engagement assay: Coadministered with ON123300 (Unsuitable) in a mouse PK cassette.

DOI Reference: 10.1021/acsmedchemlett.4c00579

Chemical Information

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Expert Reviews

No SERP comments found for NUAK1-IN-2

Probe NUAK1-IN-2 is in the process of SERP review.

Please continue to check back for new reviews and commentary.