P005091

Catalog #

27767-1

$145 *

Size: 10 mg

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Description

P005091 is a selective, potent inhibitor of USP7 deubiquitylating activity.

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Synonyms

P005091; P5091, USP-7

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Product Info

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Target(s)

USP7

Formula

C₁₂H₇Cl₂NO₃S₂

348.2 Da

Solubility

Soluble in DMSO

Biological Activity

Selective inhibitor of ubiquitin-specific protease (USP) 7 (IC50 = 4.2 µM). Displays little-to-no inhibition of other USP variants or proteases such as caspase, cathepsins and serine proteases; exhibits some activity on USP47. Induces elevated p53 and apoptosis in cancer cell lines; displays antiangiogenic activity in vivo.

CAS Registry #

882257-11-6

Background

USP7, known as herpes-associated-ubiquitin-specificprotease (HAUSP), is a deubiquitylating enzyme that regulates the levels of the oncoprotein HDM2 and its substrate, the tumor suppressor p53. P005091 accelerated the degradation of HDM2, while analogs of the compound induced dose- and time-dependent increases in the protein levels of p53 and p21. P005091 induced apoptosis in numerous cancer cell lines, including both p53+/+ and p53-mutant cancer cell lines. P005091 also downregulated claspin and phosphorylation of the DNA checkpoint kinase Chk1.

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P005091

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