GRADE & PURITY ≥98%

Synonyms

4(1H)​-​Quinolinone,8-​chloro-​2-​[(2,​4-​dichlorophenyl)​amino]​-​3-​(3-​methyl-​1-​oxobutyl)​-​5-​nitro- | 8-Chloro-2-[(2,4-dichlorophenyl)amino]-3-(3-methyl-1-oxobutyl)-5-nitro-4(1H)-quinolinone

Storage

Store at -20°C

Shipped In

Ice chest + Ice pads

Descripción general

Information

JH-RE-06 JH-RE-06 is a potent REV1-REV7 interface inhibitor with an IC50 of 0.78 μM and Kd value of 0.42 μM, disrupting REV1-POL ζ-mediated mutagenic translesion synthesis (TLS).

Targets

REV1-REV7 (Cell-free assay); REV1-REV7 (Cell-free assay) 0.42 μM(Kd); 0.78 μM

In vitro

JH-RE-06 disrupts mutagenic TLS by preventing recruitment of mutagenic POL ζ. Remarkably, JH-RE-06 targets a nearly featureless surface of REV1 that interacts with the REV7 subunit of POL ζ. Binding of JH-RE-06 induces REV1 dimerization, which blocks the REV1-REV7 interaction and POL ζ recruitment. JH-RE-06 inhibits mutagenic TLS and enhances cisplatin-induced-toxicity in cultured human and mouse cell lines.

In vivo

JH-RE-06 improves tumor cell response to cisplatin in vivo. Co-administration of JH-RE-06 with cisplatin suppresses the growth of xenograft human melanomas in mice, establishing a framework for developing TLS inhibitors as a novel class of chemotherapy adjuvants.

Cell Research(from reference)

Cell lines：HT1080 cells, A375 cells, KP cells, MEF, LNCap cells, AG01522 cells. 

Concentrations：1.5 μM 

Incubation Time：24 h 

Specifications

Sinónimos

4(1H)​-​Quinolinone, 8-​chloro-​2-​[(2, ​4-​dichlorophenyl)​amino]​-​3-​(3-​methyl-​1-​oxobutyl)​-​5-​nitro- | 8-Chloro-2-[(2, 4-dichlorophenyl)amino]-3-(3-methyl-1-oxobutyl)-5-nitro-4(1H)-quinolinone

Especificaciones y pureza

≥98%

Mecanismos bioquímicos y fisiológicos

JH-RE-06 is a potent REV1-REV7 interface inhibitor with an IC50 of 0.78 μM and Kd value of 0.42 μM, disrupting REV1-POL ζ-mediated mutagenic translesion synthesis (TLS).

Condiciones de almacenamiento de almacenamiento

Store at -20°C

Enviado en

Ice chest + Ice pads

Este producto requiere envío en cadena de frío. Los servicios terrestres y otros servicios económicos no están disponibles.

Pureza

≥98%

Propiedades del producto

• ALogP: 6.232
• hba_count: 2
• Recuento HBD: 2
• Enlace rotable: 6

Nombres e identificadores

• Sonrisas canónicas: CC(C)CC(=O)C1=C(NC2=CC=C(Cl)C=C2Cl)NC3=C(Cl)C=CC(=C3C1=O)[N+]([O-])=O
• Peso molecular: 468.72
• Reaxy-Rn: 22334922
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=22334922&ln=

Propiedades químicas y físicas

• Solubilidad: Solubility (25°C) In vitro DMSO: 12 mg/mL (25.6 mM); Water: Insoluble; Ethanol: Insoluble
• DMSO (mg/ml) Solubilidad máxima: 12
• DMSO (mM) Solubilidad máxima: 25.6016385048643
• Agua (mg/ml) Solubilidad máxima: ＜1