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Formula | C20H16Cl3N3O4 |
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Molecular Weight | 468.72 | CAS No. | 1361227-90-8 | |
Solubility (25°C)* | In vitro | DMSO | 40 mg/mL (85.33 mM) | |
Water | Insoluble | |||
Ethanol | Insoluble | |||
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
Description | 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). | ||||
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Targets |
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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 induced-toxicity in cultured human and mouse cell lines.[1] |
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In vivo | JH-RE-06 improves tumor cell response in vivo. JH-RE-06 suppresses the growth of xenograft human melanomas in mice, establishing a framework for developing TLS inhibitors as a novel class of chemotherapy adjuvants.[1] |
Cell Assay: |
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Animal Study: |
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EXO1 and DNA2-mediated ssDNA gap expansion is essential for ATR activation and to maintain viability in BRCA1-deficient cells [ Nucleic Acids Res, 2024, gkae317] | PubMed: 38721777 |
Polyubiquitinated PCNA triggers SLX4-mediated break-induced replication in alternative lengthening of telomeres (ALT) cancer cells [ Nucleic Acids Res, 2024, gkae785] | PubMed: 39291733 |
Loss of POLE3-POLE4 unleashes replicative gap accumulation upon treatment with PARP inhibitors [ Cell Rep, 2024, 43(5):114205] | PubMed: 38753485 |
POLQ seals post-replicative ssDNA gaps to maintain genome stability in BRCA-deficient cancer cells [ Mol Cell, 2022, S1097-2765(22)01070-X] | PubMed: 36455556 |
Translesion DNA synthesis mediates acquired resistance to olaparib plus temozolomide in small cell lung cancer [ Sci Adv, 2022, 8(19):eabn1229] | PubMed: 35559669 |
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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.