HL001

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].

Product Specifications

CAS Number

[1186371-31-2]

UNSPSC

12352005

Target

Apoptosis; Cyclophilin; LPL Receptor; MDM-2/p53; Reactive Oxygen Species (ROS)

Related Pathways

Apoptosis; GPCR/G Protein; Immunology/Inflammation; Metabolic Enzyme/Protease; NF-κB

Field of Research

Cancer

Purity

98.90

Solubility

DMSO : 4.17 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

O=C(NC(C(C(O)=CC=C1)=C1O)=O)NC2C3=CC=CC=C3C4=CC=CC=C24

Molecular Formula

C21H16N2O4

Molecular Weight

360.36

References & Citations

[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.|[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.