HL001 is a Cyclophilin A (CypA) inhibitor that has demonstrated significant bioactivity in non-small cell lung cancer (NSCLC) cells possessing wild-type p53 with a homozygous Arg72 variant. By inhibiting CypA, HL001 effectively suppresses MDM2-mediated ubiquitination of p53, leading to the restoration of p53 expression. This restoration results in cell cycle arrest and apoptosis in the targeted NSCLC cells. Notably, HL001 exhibits selective cytotoxicity towards NSCLC cells with the homozygous p53 Arg72 variant, while sparing cells with the Pro72 variant. In vivo studies further support its efficacy, showing that HL001 treatment significantly inhibits tumor growth in mouse xenograft models of NSCLC. These findings suggest that HL001 holds promise as a targeted therapeutic agent for NSCLC patients with specific p53 genetic profiles.
MedKoo Cat#: 126321
Name: HL001
CAS#: 1186371-31-2
Chemical Formula: C21H16N2O4
Exact Mass: 360.1110
Molecular Weight: 360.37
Elemental Analysis: C, 69.99; H, 4.48; N, 7.77; O, 17.76
The following data is based on the product molecular weight 360.37 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
