UPCDC30245 | p97/VCP inhibitor | Probechem Biochemicals

Chemical Structure : UPCDC30245

CAS No.: 1883351-01-6

UPCDC30245 (UPCDC 30245)

Catalog No.: PC-63243Not For Human Use, Lab Use Only.

UPCDC-30245 is a potent, cell penetrant allosteric p97/VCP inhibitor with IC50 of 300 nM (WT p97), also potently inhibits CB-5083 resistant p97 D649A/T688A mutant.

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Biological Activity

UPCDC-30245 is a potent, cell penetrant allosteric p97/VCP inhibitor with IC50 of 300 nM (WT p97), also potently inhibits CB-5083 resistant p97 D649A/T688A mutant.

UPCDC-30245 inhibits proliferation of multiple cancer cell lines, with IC50s ranging from 0.5-4 uM.

UPCDC-30245 also retains more activity toward CB-5083 resistant HCT116 cell line CB-R-HCT116, harboring p97 double mutant D649A/T688A than does CB-5083, exhibits the same potency in inhibiting the proliferation of CB-R-HCT116 cells as parental HCT116 cells.

UPCDC-30245 blocks endo-lysosomal degradation by inhibiting the formation of early endosome and reducing the acidity of the lysosome, an effect not observed with the potent p97 inhibitor CB-5083.

Physicochemical Properties

M.Wt	463.63
Formula	C28H38FN5
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	1-(3-(5-Fluoro-1H-indol-2-yl)phenyl)-N-(2-(4-isopropylpiperazin-1-yl)ethyl)piperidin-4-amine

References

1. Segura-Cabrera A, et al. Sci Rep. 2017 Mar 21;7:44912.

2. Banerjee S, et al. Science. 2016 Feb 19;351(6275):871-5.

UPCDC30245 (UPCDC 30245)

Biological Activity

Physicochemical Properties

References

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