JH-RE-06 is a potent REV1-REV7 interface inhibitor with an IC50 value of 0.78 μM and Kd value of 0.42 μM, which disrupted the mutagenic transmembrane synthesis (TLS) mediated by REV1-POLζ.

 

Brand: BCM

 

Target: DNA/RNA Synthesis

 

Signaling Pathways: Cell Cycle/Checkpoint; DNA Damage/DNA Repair

 

In Vitro: JH-RE-06 unexpectedly causes dimerization of the REV1 CTD at its REV7-binding surface. It also blocks the REV1-REV7 interaction.

 

In Vivo: In mice, co-administration of JH-RE-06 with cisplatin inhibits the growth of xenograft human melanomas. JH-RE-06 suppresses mutagenic TLS and increases cisplatin-induced toxicity in cultured human and mouse cell lines.

 

Boiling Point: 586.9±50.0 °C(Predicted)

 

pKa: -3.78±0.70(Predicted)

 

Solubility: Soluble in DMSO. Insoluble in Water; insoluble in Ethanol.

 

Isomeric SMILES: CC(C)CC(=O)C1=C(NC2=C(C=CC(=C2C1=O)[N+](=O)[O-])Cl)NC3=C(C=C(C=C3)Cl)Cl  

 

InChIKey: LRTXIQCBQIKIOH-UHFFFAOYSA-N  

 

InChI: 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) 

 

Attribute
[Chem Name]	8-chloro-2-(2,4-dichloroanilino)-3-(3-methylbutanoyl)-5-nitro-1H-quinolin-4-one
[Synonym]	JH-RE-06
[CAS No.]	1361227-90-8
[Formula]	C20H16Cl3N3O4
[Molecular]	468.72
[Form]	Solid powder
[Storage]	Store at -20°C

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