WEE1/PKMYT1-IN-4

WEE1/PKMYT1-IN-4 (Compound 24) (2 h) potently inhibits PKMYT1 in 293T cells expressing PKMYT1-NanoLuc, with an IC₅₀ of 2.2 nM^[1].
WEE1/PKMYT1-IN-4 (2 h) inhibits WEE1 in 293T cells expressing WEE1-NanoLuc, with an IC₅₀ of 0.185 μM^[1].
WEE1/PKMYT1-IN-4 (2 h) potently inhibits CDK1^T14 phosphorylation in HCC1569 cells, with an IC₅₀ of 4.9 nM^[1].
WEE1/PKMYT1-IN-4 (2 h) inhibits CDK1 Y15 phosphorylation in HCC1569 cells, with an IC₅₀ of 0.186 μM^[1].
WEE1/PKMYT1-IN-4 (7 d) inhibits proliferation of HCC1569 cells with an IC₅₀ of 0.032 μM and KYSE30 cells with an IC₅₀ of 0.252 μM, yielding a selectivity ratio of 7.9^[1].
WEE1/PKMYT1-IN-4 (0.1-1 μM) exhibits favorable kinome selectivity at 1 μM, with off-target activity against ABL1, ABL2, WEE2, SRC, and PLK3 at 0.1 μM, having IC₅₀ values ranging from 12.8 nM to 284.0 nM^[1].
WEE1/PKMYT1-IN-4 demonstrates potent antiproliferative activity across most patient-derived colorectal cancer organoids, outperforming single-target PKMYT1 and WEE1 inhibitors, with TP53 mutation status correlating significantly with drug sensitivity^[1].
WEE1/PKMYT1-IN-4 (0.1-10 μM; 4 h) dose-dependently reduces CDK1 T14 and Y15 phosphorylation in PDM190 colorectal cancer organoids after 4 hours of treatment^[1].
WEE1/PKMYT1-IN-4 (10 μM) exhibits favorable in vitro ADME properties including improved permeability, low human hepatic clearance, and favorable plasma protein binding, with moderate inhibition of CYP3A4^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.