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| | HL001
(HL 001) Basic information |
| | HL001
(HL 001) Chemical Properties |
| Melting point | 225-227 °C | | density | 1.48±0.1 g/cm3(Predicted) | | pka | 7.40±0.35(Predicted) |
| | HL001
(HL 001) Usage And Synthesis |
| Uses | 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. |
| | HL001
(HL 001) Preparation Products And Raw materials |
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