UCI-LC0019 

UCI-LC0019 is a mutant p53 reactivator. UCI-LC0019 binds to mutant p53, induces wild-type-like conformational change, restores sequence-specific DNA binding activity, activates p53-dependent transcription programs, and does not act via thiol reactivity or glutathione depletion. UCI-LC0019 inhibits proliferation and induces apoptosis in cancer cells harboring mutant p53, with no significant effect on p53^null or wild-type p53 tumors cells. UCI-LC0019 exhibits anti-tumor activity in xenograft mouse models carrying p53^R175H mutant tumors. UCI-LC0019 can be used for the research of cancer, such as ovarian cancer^[1].

UCI-LC0019 potently inhibits proliferation of p53^G245S-expressing Saos-2 cells (IC₅₀ = 16.5 μM) and p53^R175H-expressing TOV112D cells (IC₅₀ = 15.2 μM) with reduced activity against p53^null Saos-2 cells (IC₅₀ = 24.1 μM)^[1].
UCI-LC0019 (0-30 μM; 3-72 h) rapidly reduces proliferation and induces apoptosis in p53^R175H-expressing TOV112D cells^[1].
UCI-LC0019 (25-30 μM; 3 days) inhibits proliferation of p53^R175H-expressing TOV112D cells via a mechanism independent of thiol reactivity, as co-treatment with 5 mM NAC (HY-B0215) does not reverse its antiproliferative effects^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

UCI-LC0019 (10 mg/kg; i.p.; daily for 10 days) inhibits tumor growth in mice with p53^R175H-expressing TOV112D Xenografts^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

278.31

C₁₇H₁₄N₂O₂

1372406-51-3

Solid

Light yellow to yellow

COC1=CC=CC(/C=C/C(C2=NC3=CC=CC=C3N2)=O)=C1

Room temperature in continental US; may vary elsewhere.

• [1]. Durairaj G, et al. Discovery of compounds that reactivate p53 mutants in vitro and in vivo. Cell Chem Biol. 2022;29(9):1381-1395.e13.