| Cas No.: | 2009273-67-8 |
| Chemical 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 |
| SMILES: | O([H])C1C([H])=C([H])C(=C([H])C=1[H])C1C(N([H])[H])=NC([H])=C(C2C([H])=C([H])C3=C(C([H])=NN3[H])C=2[H])C=1C([H])([H])C([H])([H])[H] |
| Formula: | C20H18N4O |
| M.Wt: | 330.3831 |
| Purity: | >98% |
| Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Description: | GNE-6640 is a selective and non-covalent inhibitor of ubiquitin epecific peptidase 7 (USP7), with IC50 values of 0.75 μM, 0.43 μM, 20.3 μM and 0.23 μM for full length USP7, USP7 catalytic domain, full length USP43 and Ub-MDM2, respectively. |
| 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 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]. |
| 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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| LOT NO. | DOWNLOAD |
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| 2018-0101 |
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| 2018-0101 |
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