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NE26394

Chemical Structure : NE26394

CAS No.:

NE26394

Catalog No.: PC-27389Not For Human Use, Lab Use Only.

NE26394 is a first-in-class, selective molecular glue degrader (MGD) of cyclin-dependent kinase 4 (CDK4) with DC50 of 163 nM and Dmax=93%, induces CDK4 recognition by CRBN depending on the co recruitment of endogenous INK4 family proteins.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

NE26394 is a first-in-class, selective molecular glue degrader (MGD) of cyclin-dependent kinase 4 (CDK4) with DC50 of 163 nM and Dmax=93%, induces CDK4 recognition by CRBN depending on the co recruitment of endogenous INK4 family proteins.
NE26394 has much weaker downregulation of the close homologue CDK6 with DC50 of >10 uM, shows no activity for kinases CDK1, CDK2, CDK5, CDK7, CDK9, GSK3α and GSK3β.
NE26394 is a selective CRBN-based molecular glue recruiting CDK4-INK4 complexes.
NE26394 inhibits RB-E2F pathway activity in CDK4-dependent cancer cells, broadly suppresses E2F target protein expression across CDK4-dependent and RB-proficient prostate cancer cell lines.

Physicochemical Properties

M.Wt
Formula
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

References

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