NEDISERTIB

NEDISERTIB : Inhibitor of PRKDC

Structure

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Information

PRKDC

Inhibitor

up to 1 uM

Probe Availability:

MedChemExpress

In Vitro Validations

Uniprot ID: P78527

Target Class: Kinase

Target SubClass: PI3/PI4

Potency: IC50

Potency Value: 0.6 nM

Potency Assay: DNA-PK enzymatic assay at 10 uM ATP

PDB ID for probe-target interaction (3D structure): 7Z87, 7Z88, 7OTY

Target aliases:

DNA-dependent protein kinase catalytic subunit, HY ...

DOI Reference: 10.1158/1535-7163.MCT-19-0734

Uniprot ID: P78527

Target Class: Kinase

Target SubClass: PI3/PI4

Potency: IC50

Potency Value: 20 nM

Potency Assay: DNA-PK enzymatic assay at 1 uM ATP

PDB ID for probe-target interaction (3D structure): 7Z87, 7Z88, 7OTY

Target aliases:

DNA-dependent protein kinase catalytic subunit, HY ...

DOI Reference: 10.1158/1535-7163.MCT-19-0734

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): Selectivity within target family: IC50s ATM 10,000 nM, ATR 2,800 nM, hPI3Kalpha 330 nM, hPI3Kbeta 250 nM, hPI3Kgamma >1,000 nM, hPI3Kdelta 95 nM. Protein kinases panel profiling: 276/284 not inhibited ≥50% at 1 μmol/L

Potency assay, off target (cells): In bleomycin-treated HCT-116 cells, M3814 did not inhibit phosphorylation of the ATM kinase substrate CHK2. M3814 did not block CHK1 phosphorylation, suggesting that ATR is not inhibited in cells. M3814 only moderately inhibited the phosphorylation of AKT, which is consistent with its weak inhibitory activity on the PI3K isoforms. HU-induced pS345-CHK1 >25,000 nM, Bleomycin-induced pT68-CHK2 >5,000 nM, Constitutive pS473-AKT in PC3 3,800 nM.

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(last updated: 9 Apr 2024 )