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P1D-34

Chemical Structure : P1D-34

CAS No.: 2957895-04-2

P1D-34 (Pin1 PROTAC degrader)

Catalog No.: PC-22075Not For Human Use, Lab Use Only.

P1D-34 is a first-in-class, potent and covalent PROTAC degrader of Pin1 with DC50 value of 177 nM in MV-4-11 cells, Dmax of 95%.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

P1D-34 is a first-in-class, potent and covalent PROTAC degrader of Pin1 with DC50 value of 177 nM in MV-4-11 cells, Dmax of 95%.
P1D-34 coupled the covalent Pin1 inhibitor Sulfopin to a cereblon ligand.
P1D-34 induces cell cycle arrest and apoptosis in AML cells, exhibits cell growth inhibitory activities with IC50 of 2-8 uM in a panel of AML cell lines: MV-4-11, MOLM-13, HL-60, THP-1, Kasumi-1, BDCM and OCI-AML3.
P1D-34 sensitizes ABT-199 against ABT-199-resistant AML cell lines, induces DNA damage and apoptosis by releasing ROS generation, and sensitizes 2-DG by down-regulating UPR pathways.

Physicochemical Properties

M.Wt 835.46
Formula C40H59ClN6O9S
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

N1-(3-(2-chloro-N-((R)-1,1-dioxidotetrahydrothiophen-3-yl)acetamido)-2,2-dimethylpropyl)-N4-(12-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-5-yl)amino)dodecyl)succinamide

References

1. Yunkai Shi, et al. Chem Sci. 2024 Feb 28;15(13):5027-5035.

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