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JH-RE-06

Chemical Structure : JH-RE-06

CAS No.: 1361227-90-8

JH-RE-06

Catalog No.: PC-72501Not For Human Use, Lab Use Only.

JH-RE-06 is a potent REV1-REV7 interface inhibitor (IC50=0.78 uM, Kd=0.42 uM) that disrupts mutagenic translesion synthesis (TLS) by preventing recruitment of mutagenic POLζ, induces REV1 dimerization and blocks POLζ recruitment.

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Biological Activity

JH-RE-06 is a potent REV1-REV7 interface inhibitor (IC50=0.78 uM, Kd=0.42 uM) that disrupts mutagenic translesion synthesis (TLS) by preventing recruitment of mutagenic POLζ, induces REV1 dimerization and blocks POLζ recruitment.
JH-RE-06 enhances cisplatin cytotoxicity and suppresses cisplatin-induced mutagenesis by interfering with REV1-dependent mutagenic TLS.
JH-RE-06 sensitizes cells to cisplatin and reduces HPRT mutations in a REV1-dependent manner.
JH-RE-06 (1.6 mg/kg, i.p.) improves tumor cell response to cisplatin in a xenograft mouse model.
JH-RE-06 is a novel TLS inhibitor as a class of chemotherapy adjuvants.

Physicochemical Properties

M.Wt 468.72
Formula C20H16Cl3N3O4
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

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

References

1. Wojtaszek JL, et al. Cell. 2019 Jun 27;178(1):152-159.e11.

2. Chatterjee N, et al. Proc Natl Acad Sci U S A. 2020 Nov 17;117(46):28918-28921.

3. Taglialatela A, et al. Mol Cell. 2021 Oct 7;81(19):4008-4025.e7.

4. Chen Y, et al. Cell Death Dis. 2022 Feb 3;13(2):110.

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