| CAS NO: | 1361227-90-8 |
| Cas No. | 1361227-90-8 |
| Canonical SMILES | O=C1C(C(CC(C)C)=O)=C(NC2=CC=C(Cl)C=C2Cl)NC3=C1C([N+]([O-])=O)=CC=C3Cl |
| 分子式 | C20H16Cl3N3O4 |
| 分子量 | 468.72 |
| 溶解度 | DMSO: 5 mg/mL (10.67 mM) |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
| 产品描述 | JH-RE-06, a potent REV1-REV7 interface inhibitor (IC50=0.78 μM; Kd=0.42 μM), targets REV1 that interacts with the REV7 subunit of POLζ. JH-RE-06 disrupts mutagenic translesion synthesis (TLS) by preventing recruitment of mutagenic POLζ. JH-RE-06 enhances Cisplatin-induced cytotoxicity and improves chemotherapy[1][2]. IC50: 0.78 μM (REV1-REV7)[1]Kd: 0.42 μM (REV1-REV7)[1] JH-RE-06 unexpectedly induces dimerization of the REV1 CTD at its REV7-binding surface and blocks the REV1-REV7 interaction[1]. JH-RE-06 inhibits mutagenic TLS and enhances cisplatin-induced toxicity in cultured human and mouse cell lines[1]. Co-administration of JH-RE-06 with cisplatin suppresses the growth of xenograft human melanomas in mice[1]. [1]. Wojtaszek JL, et al. A Small Molecule Targeting Mutagenic Translesion Synthesis Improves Chemotherapy. Cell. 2019 Jun 27;178(1):152-159.e11. [2]. REV1-POLς Inhibition Enhances Cisplatin-Induced Cytotoxicity. Cancer Discov. 2019 Aug;9(8):OF17. |
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