Table 3Wee1 Degradation Inhibitor Probes and Prior Art

CompoundNote Book RefSource (S for Synth; P for Purch)CIDSIDMLS IDSR NumberStructureAID 434972 % INH Wee1 Degradation (relative to probe)AID 463080 Wee1 EC50 (μM)AID 463077 CK1d IC 50 (μM)AID 463076 FLT3 IC50 (μM)AID 463169 WEE1 Fold Stabilization at 100nMCyclin B Fold Stabilization at 100nM
New WEE1 Probe (ML177)2RJR 159S451004319.2E+07MLS 003128609SR- 03000001277
Image ml177fu2.jpg
1000.040.049 (Active)0.305 (Active)23.26 (Active)2.62 (Inactive)
Previous Wee1 Probe (ML118)NoneS323790487235992 (4243143 MLSMR)MLS 000089581SR- 01000621290
Image ml177fu3.jpg
79.19 (Active) AID 2088 (13.95% Activation, AID 1321, Active)7.87 (Active) AID 1412; 6.2 (Active AID 2088)3064.4% at 229 nM (Active) AID 2088−0.1% at 229 nM (Inactive) AID 2088 (6.78% max %ACT) Inactive
MG132 (Prior state of the art proteasome inhibitor)NoneP46238224892475 (powder SID 85261504)None (Sigma)SR- 01000864598
Image ml177fu4.jpg
ND4.5 (Active) AID 1412NDNDActiveEC50 = 4.7uM (Active) AID 1414 Non- Selective Compound

From: Identification of Small Molecule Inhibitors of Wee1 Degradation and Mitotic Entry

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Probe Reports from the NIH Molecular Libraries Program [Internet].

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