JH-RE-06 - 10mM in DMSO , CAS No.1361227-90-8

CAS: 1361227-90-8 Cat. No.: J421371 Formula: C₂₀H₁₆Cl₃N₃O₄ Molecular Weight: 468.72

GRADE & PURITY 10mM in DMSO

Synonyms

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

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

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

Synonyms

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

Specifications & Purity

10mM in DMSO

Biochemical and Physiological Mechanisms

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).

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Action Type

INHIBITOR

Product Properties

ALogP

6.232

hba_count

2

HBD Count

2

Rotatable Bond

6

Names and Identifiers

Molecular Weight

468.72

Reaxy-Rn

22334922

Reaxys-RN_link_address

https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=22334922&ln=

Chemical and Physical Properties

• DMSO(mg / mL) Max Solubility: 12
• DMSO(mM) Max Solubility: 25.6016385048643
• Water(mg / mL) Max Solubility: ＜1

Frequently Asked Questions

How should this product be stored?

Store at ?80 °C. Ultra-low temperature storage is required to maintain the specified shelf life.

How is this product shipped?

This product ships frozen with dry ice and cold packs. Unpack on arrival and transfer it to the storage condition stated above; handle dry ice with insulated gloves in a ventilated area.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 1361227-90-8, the molecular formula is C20H16Cl3N3O4, and the molecular weight is 468.72 g/mol.

What documentation is provided?

Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.