USP7-IN-4( R)-USP-IN-4 | USP7 inhibitor 4 )

Catalog No. M13500 CAS No. 2196243-57-7

COA

Datasheet

HNMR

HPLC

MSDS

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Product Name

USP7-IN-4
Note

Research use only, not for human use.
Brief Description

(R)-USP-IN-4 is a highly potent, selective, allosteric USP7 inhibitor with IC50 of 6 nM in FP assays.
Description

(R)-USP-IN-4 is a highly potent, selective, allosteric USP7 inhibitor with IC50 of 6 nM in FP assays; also shows high potency in an alternative assay using the Ub-Rh110 substrate (IC50=1.5 nM) and Kd of 2.0 nM; displays high selectivuty against other DUBs, proteases and kinases; demonstrates highly potent target engagement in cells (EC50=49 nM), with no off-target activity against USP47, causes nongenotoxic stabilization of p53 and decreased levels of MDM2 in HCT116 cells.
In Vitro

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In Vivo

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Synonyms

R)-USP-IN-4 | USP7 inhibitor 4
Pathway

Proteasome/Ubiquitin
Target

DUB
Recptor

DUB
Research Area

——
Indication

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CAS Number

2196243-57-7
Formula Weight

514.63
Molecular Formula

C29H34N6O3
Purity

>98% (HPLC)
Solubility

10 mM in DMSO
SMILES

O=C1C2=NN(C)C(C3=CC=C(CN)C=C3)=C2N=CN1CC4(O)CCN(C(C[C@H](C5=CC=CC=C5)C)=O)CC4
Chemical Name

(R)-3-(4-(aminomethyl)phenyl)-6-((4-hydroxy-1-(3-phenylbutanoyl)piperidin-4-yl)methyl)-2-methyl-2,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one

1. Gavory G, et al. Nat Chem Biol. 2018 Feb;14(2):118-125.

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