GNE-6640

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

GNE-6640 (GNE6640) 是一种有效的选择性 USP7 抑制剂，IC50 为 0.75 uM。

GNE-6640 (GNE6640) is a potent, selective USP7 inhibitor with IC50 of 0.75 uM; dislpalys selectivity over USP47 and USP5 (IC50>200 uM); promotes endogenous MDM2 ubiquitination, stabilized p53 and upregulated p21, induces tumour cell death and enhances cytotoxicity with chemotherapeutic agents and targeted compounds, including PIM kinase inhibitors; decreased viability of 108 cell lines with IC50 <10 uM.(In Vitro):GNE-6640 promotes endogenous MDM2 ubiquitination with Lys48 (K48)-linked polyubiquitin chains, which directs proteasomal degradation13. GNE-6640 targets cellular USP7, MDM2, and p53 signalling pathways. GNE-6640 decreases viability of 108 cell lines with IC50 ≤ 10 μM. Combining GNE-6640 with doxorubicin or cisplatin (DNA-damaging agents), which could activate the p53 response and enhance USP7 inhibitor efficacy. GNE-6640 could induce tumor cell death. GNE-6640 enhances cytotoxicity with chemotherapeutic agents and targeted compounds, including PIM kinase inhibitors.

GNE-6640 promotes endogenous MDM2 ubiquitination with Lys48 (K48)-linked polyubiquitin chains, which directs proteasomal degradation13. GNE-6640 targets cellular USP7, MDM2, and p53 signalling pathways. GNE-6640 decreases viability of 108 cell lines with IC50 ≤ 10 μM. Combining GNE-6640 with doxorubicin or cisplatin (DNA-damaging agents), which could activate the p53 response and enhance USP7 inhibitor efficacy. GNE-6640 could induce tumor cell death. GNE-6640 enhances cytotoxicity with chemotherapeutic agents and targeted compounds, including PIM kinase inhibitors.

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GNE 6640 | GNE6640

Proteasome/Ubiquitin

DUB

DUB

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2009273-67-8

330.391

C20H18N4O

>98% (HPLC)

10 mM in DMSO

OC1=CC=C(C2=C(CC)C(C3=CC4=C(NN=C4)C=C3)=CN=C2N)C=C1

4-[2-Amino-4-ethyl-5-(1H-indazol-5-yl)-3-pyridyl]phenol

(-20℃)

With Ice Pack

≥ 2 years