HLI 373 (hydrochloride)

• CAT Number: R065737
• CAS Number: 1782531-99-0
• Molecular Formula: C18H23N5O2 • 2HCl
• Molecular Weight: 414.3
• Purity: ≥95%
• Storage: -20°C
• InChI: InChI=1S/C18H23N5O2.2ClH/c1-21(2)11-7-10-19-15-12-8-5-6-9-13(12)22(3)16-14(15)17(24)23(4)18(25)20-16;;/h5-6,8-9,19H,7,10-11H2,1-4H3;2*1H
• InChIKey: WUEMKAQTAIRDOA-UHFFFAOYSA-N
• SMILES: O=C(C1=C(NCCCN(C)C)C2=CC=CC=C2N(C)C1=N3)N(C)C3=O.Cl.Cl

Hdm-2 (human double minute-2; Mdm-2 in mouse) is a ubiquitin ligase and key negative regulator of p53, targeting it for proteasomal degradation. Overexpression of Hdm-2 in some tumors leads to inactivation of p53, thereby allowing tumor cells to escape p53-induced apoptosis. HLI 373 is an inhibitor of Hdm-2. At concentrations of 5-50 µM, it selectively inhibits autoubiquitylation of Hdm-2 as well as the ubiquitylation and degradation of p53. Through these actions, HLI 373 stabilizes p53 and increases p53-dependent transcription, inducing apoptosis of transformed cells, tumor cells, and mouse embryo fibroblasts harboring wild-type p53.

Reference

1.Chène, P. Inhibiting the p53-MDM2 interaction: An important target for cancer therapy. Nature Reviews.Cancer 3, 102-109 (2003).