HL001 is an orally active small molecule inhibitor of Cyclophilin A (CypA) and a receptor antagonist of Lysophosphatidic acid 1 (LPA1). HL001 induces cell cycle arrest and apoptosis of tumor cells by p53. HL001 stabilizes p53 by down-regulating G3BP1, inducing reactive oxygen species and DNA damage. HL001 disrupts the interaction between MDM2 and p53-72R in a CypA dependent manner. HL001 has antitumor activity. HL001 can also be used to study pulmonary fibrosis[1][2].
IC 50
Cyclophilin A; LPA1 Receptor
References
[1] Lu W, et al. Selective targeting p53WT lung cancer cells harboring homozygous p53 Arg72 by an inhibitor of CypA. Oncogene. 2017 Aug 17;36(33):4719-4731. DOI:10.1038/onc.2017.41 [2] Yuki Y, et al. Preclinical evaluation of HL001, a novel lysophosphatidic acid 1 (LPA1) receptor antagonist, for idiopathic pulmonary fibrosis utilizing physiologically relevant stem cell-derived lung organoids. European Respiratory Journal 2023 62(suppl 67): OA898.
