JH-RE-06是一种REV1-REV7互作抑制剂，IC50为0.78 μM，Kd为0.42 μM。它靶向与 POLζ 的 REV7 亚基相互作用的 REV1，可改善化疗效果。它通过阻止诱变 POLζ 的募集来破坏诱变性跨损伤合成。

JH-RE-06 disrupts mutagenic translesion synthesis (TLS) by preventing the recruitment of mutagenic POLζ. JH-RE-06 is an effective REV1-REV7 interface inhibitor (IC50=0.78 μM; Kd=0.42 μM), which targets REV1 that interacts with the REV7 subunit of POLζ. JH-RE-06 also improves chemotherapy.

JH-RE-06 unexpectedly causes dimerization of the REV1 CTD at its REV7-binding surface. It also blocks the REV1-REV7 interaction.

In mice, co-administration of JH-RE-06 with cisplatin inhibits the growth of xenograft human melanomas. JH-RE-06 suppresses mutagenic TLS and increases cisplatin-induced toxicity in cultured human and mouse cell lines [1].

1361227-90-8

C20H16Cl3N3O4

468.72

DMSO:5 mg/mL (10.67 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years