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CP134

Chemical Structure : CP134

CAS No.:

CP134 (CP 134)

Catalog No.: PC-22688Not For Human Use, Lab Use Only.

CP134 is a potent, selective PROTAC degrader of dual-specificity tyrosine phosphorylation-regulated kinase 2 (DYRK2) with DC50 of 1.6 uM in MM231 and 3.3 uM in HeLa, respectively.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

CP134 is a potent, selective PROTAC degrader of dual-specificity tyrosine phosphorylation-regulated kinase 2 (DYRK2) with DC50 of 1.6 uM in MM231 and 3.3 uM in HeLa, respectively.
CP134 reduced the intracellular DYRK2 level in a concentration- and time-dependent manner.
CP134 (5 uM) significantly downregulated the levels of phosphorylated p53 (Ser46) and c-Myc (Ser62) in MM231 cells.
CP134 effectively inhibited cell proliferation with IC50 values of 9.1 uM in MM231 cell line.

Physicochemical Properties

M.Wt 921.64
Formula C42H43Br2N5O9
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

2-(3,5-bis((E)-2-bromobenzylidene)-4-oxopiperidin-1-yl)-N-(2-(2-(2-(2-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)ethoxy)ethoxy)ethoxy)ethyl)acetamide

References

1. Chen J, et al. ACS Med Chem Lett. 2024 Apr 30;15(5):659-666.

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