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JH-RE-06

Cat. No. M20728
JH-RE-06 Structure
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Biological Activity

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).

Chemical Information
Molecular Weight 468.72
Formula C20H16Cl3N3O4
CAS Number 1361227-90-8
Solubility (25°C) DMSO 12 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Joshua Victor, et al. Res Sq. SARS-CoV-2 hijacks host cell genome instability pathways

[2] Yunshang Chen, et al. Cell Death Dis. REV1 promotes lung tumorigenesis by activating the Rad18/SERTAD2 axis

[3] Angelo Taglialatela, et al. Mol Cell. REV1-Polζ maintains the viability of homologous recombination-deficient cancer cells through mutagenic repair of PRIMPOL-dependent ssDNA gaps

[4] Nimrat Chatterjee, et al. Proc Natl Acad Sci U S A. REV1 inhibitor JH-RE-06 enhances tumor cell response to chemotherapy by triggering senescence hallmarks

[5] Jessica L Wojtaszek, et al. Cell. A Small Molecule Targeting Mutagenic Translesion Synthesis Improves Chemotherapy

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