USP7-IN-4

Research use only, not for human use.

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

(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.

R)-USP-IN-4;USP7 inhibitor 4

Proteasome/Ubiquitin

DUB

DUB

——

——

2196243-57-7

514.63

C29H34N6O3

>98% (HPLC)

10 mM in DMSO

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

(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

(-20℃)

With Ice Pack

≥ 2 years