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ARUK2001607 | ARUK2001607 : Inhibitor of PIP4K2C
RATINGS:
Cellular Use: (2 reviews)

In Model Organisms: (2 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
PIP4K2C
  • IC50:79.4 nM
  • Kd:7.1 nM
  • IC50:250 nM
Inhibitor
up to 1 uM

Selectivity

In Vitro Selectivity Assessment
PIP5K1C

Gene ID: O60331

Organism: Homo sapiens

Family: None

Potency: Kd - 230 nM

Potency Assay Off-Target:
Selective against isoform PI5P4Kalpha (IC50 >39 uM). Screened in 3 panels: - 140 protein kinases Com ...

Potency
Cellular
In Vitro

PIP4K2C

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/acs.jmedchem.2c01693

In Vivo Validations

Mouse
Dose: 5 mg/Kg
Route of delivery: Intraperitoneal
Plasma half life: 0.74 h
Area Under the Curve:: 4520 hr*ng/mL
Fb : 91.1% Plasma, 94.6% Brain
Target engagement assay: Kpu,u = 0.58

DOI Reference: 10.1021/acs.jmedchem.2c01693

Chemical Information

Molecular Formula C14H13N3O2S2
SMILEs Cc1cc2c(Nc3ccc(S(C)(=O)=O)cc3)ncnc2s1
InChI InChI=1S/C14H13N3O2S2/c1-9-7-12-13(15-8-16-14(12)20-9)17-10-3-5-11(6-4-10)21(2,18)19/h3-8H,1-2H3,(H,15,16,17)
Molecular weight 319.04 Da
AlogP 0.0
HBond acceptors 5
HBond donors 1
Atoms 34

References

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Cross References

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Vendors

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Expert Reviews

by SERP
(on 19 Nov 2023 )
Cellular Use Rating
In Model Organisms
ARUK2001607 is a PI5P4Kγ (PIP4K2C) inhibitor with good potency (79.4 nM) in an enzyme assay conducted on an activated PI5P4Kγ variant (PI5P4Kγ+, see DOI: 10.1021/acs.jmedchem.2c01693). Affinity for the...
by SERP
(on 27 Nov 2023 )
Cellular Use Rating
In Model Organisms
( The reviewer did not leave any comments )
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