| Identification | Back Directory | [Name]
4(1H)-Quinolinone, 8-chloro-2-[(2,4-dichlorophenyl)amino]-3-(3-methyl-1-oxobutyl)-5-nitro- | [CAS]
1361227-90-8 | [Synonyms]
JH-RE-06
4(1H)-Quinolinone, 8-chloro-2-[(2,4-dichlorophenyl)amino]-3-(3-methyl-1-oxobutyl)-5-nitro- | [Molecular Formula]
C20H16Cl3N3O4 | [MOL File]
1361227-90-8.mol | [Molecular Weight]
468.72 |
| Chemical Properties | Back Directory | [Boiling point ]
586.9±50.0 °C(Predicted) | [density ]
1.503±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO: 5 mg/mL (10.67 mM) | [form ]
Solid | [pka]
-3.78±0.70(Predicted) | [color ]
White to yellow | [InChI]
1S/C20H16Cl3N3O4/c1-9(2)7-15(27)17-19(28)16-14(26(29)30)6-4-11(22)18(16)25-20(17)24-13-5-3-10(21)8-12(13)23/h3-6,8-9H,7H2,1-2H3,(H2,24,25,28) | [InChIKey]
LRTXIQCBQIKIOH-UHFFFAOYSA-N | [SMILES]
Clc1c(ccc(c1)Cl)Nc2[nH]c3c([c](c2C(=O)CC(C)C)=O)c(ccc3Cl)[N+](=O)[O-] |
| Hazard Information | Back Directory | [Uses]
JH-RE-06-d6 is deuterium labele JH-RE-06. JH-RE-06, a potent REV1-REV7 interface inhibitor (IC50=0.78 μM; Ki=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 improves chemotherapy[1]. | [Biological Activity]
JH-RE-06 is a potent and selective inhibitor of REV1-REV7 interaction th at induces REV1 dimerization blocking the REV1-REV7 interaction and POL ϲ recruitment. JH-RE-06 potently inhibits translesion synthesis (TLS) and augments cisplatin effectiveness in cultured human and mouse cell lines. It improves effectiveness of cisplatin in A375 tumor xenograft mouse model. | [References]
[1] Wojtaszek JL, et al. A Small Molecule Targeting Mutagenic Translesion Synthesis Improves Chemotherapy. Cell. 2019;178(1):152-159.e11. DOI:10.1016/j.cell.2019.05.028 |
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