AZENOSERTIB

AZENOSERTIB : Inhibitor of WEE1

Structure

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Information

WEE1

Inhibitor

up to 1 uM

In Vitro Validations

Uniprot ID: P30291

Target Class: Kinase

Target SubClass: Ser/Thr kinase

Potency: IC50

Potency Value: 3.9 nM

Potency Assay: Enzymatic assay

PDB ID for probe-target interaction (3D structure): 7N3U

Target aliases:

Wee1-like protein kinase, WEE1, WEE1_HUMAN, WEE1hu ...

DOI Reference: 10.1021/acs.jmedchem.1c01121

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): Azenosertib showed excellent kinase selectivity. When screened against a full panel of 476 kinases at 1 μM concentration, ZN-c3 hit 5 kinases (Wee1, PLK2, YSK4, EGFR d747-749/A750P, and PLK3) with ≥90% inhibition and another 5 kinases (EGFR d746-750, PLK1, MAP3K3, NEK1, and LCK) with 75–89% inhibition. A small set of interesting kinases including EGFR (d747-749 A750), YSK4, PLK1, PLK2, and PLK3 were selected to determine IC50. EGFR (d747-749 A750) (IC50 = 60 nM); YSK4 (IC50 = 59 nM); PLK1 (IC50 = 227 nM); PLK2 (IC50 = 40 nM); PLK3 (IC50 = 70 nM); Azenosertib showed >10-fold selectivity against those five selected kinases. Compared with the existing Wee1 inhibitors, ZN-c3 has achieved a much better kinase selectivity.

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