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
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M.Wt
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835.46
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Formula
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C40H59ClN6O9S
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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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
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References
1. Yunkai Shi, et al. Chem Sci. 2024 Feb 28;15(13):5027-5035.
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