GNE-6640 Datasheet DC Chemicals
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Cat.No DC12495
Name GNE-6640

Chemical Properties

CAS 2009273-67-8
Formula C20H18N4O
MW 330.3831
Storage 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Biological activity

Description CAS NO.：2009273-67-8
Product Name：4-[2-Amino-4-ethyl-5-(1H-indazol-5-yl)-3-pyridyl]phenol
Synonyms：4-[2-amino-4-ethyl-5-(1H-indazol-5-yl)-3-pyridyl]phenol;4-(2-amino-4-ethyl-5-(1H-indazol-5-yl)pyridin-3-yl)phenol;4-[2-Amino-4-Ethyl-5-(1h-Indazol-5-Yl)pyridin-3-Yl]phenol;BCP31358;BDBM50250963;ZB1503;GNE 6640; GNE6640;AK00799504;A16883;NC1=NC=C(C(=C1C1=CC=C(C=C1)O)CC)C=1C=C2C=NNC2=CC=1;8JM;GNE-6640
EINEC:
Molecular Formula：C20H18N4O
Molecular Weight：330.3831
Target: IC50: 0.75 μM(full length USP7), 0.43 μM(USP7 catalytic domain), 20.3 μM(full length USP43), 0.23 μM(Ub-MDM2)[1].
In Vivo
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[1].
Kinase Assay
Cell Assay
Animal Administration

References

[1]. Kategaya L, et al. USP7 small-molecule inhibitors interfere with ubiquitin binding. Nature. 2017 Oct 26;550(7677):534-538.
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