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p97 inhibitor PPA

Chemical Structure : p97 inhibitor PPA

CAS No.: 1135195-64-0

p97 inhibitor PPA (VCP inhibitor PPA, ACJI-99C)

Catalog No.: PC-26297Not For Human Use, Lab Use Only.

p97 inhibitor PPA (ACJI-99C) is a selective, covalent p97/VCP ATPase inhibitor with IC50 of 0.6 uM in in vitro ATPase activity assay, with no activity against yeast Cdc48, and N-ethylmaleimide sensitive factor (NSF).

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

p97 inhibitor PPA (ACJI-99C) is a selective, covalent p97/VCP ATPase inhibitor with IC50 of 0.6 uM in in vitro ATPase activity assay, with no activity against yeast Cdc48, and N-ethylmaleimide sensitive factor (NSF).
PPA inhibits proliferation of HCT116, HeLa, and RPMI8226 with IC50 of 2.7 μM, 6.1 μM, and 3.4 μM, respectively.
PPA inhibits proliferation of two HCT116 cell lines that are resistant to CB-5083 and NMS-873, respectively.
PPA covalently modifies VCP on the active site Cys522.

Physicochemical Properties

M.Wt 321.38
Formula C18H19N5O
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
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Solubility

10 mM in DMSO

Chemical Name/SMILES

2-Propenamide, N-[1-(1,1-dimethylethyl)-3-phenyl-1H-pyrazolo[3,4-d]pyrimidin-4-yl]-

References

1. Gang Zhang, et al. Eur J Med Chem. 2021 Mar 5:213:113148.

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