2-Methoxyethyl 4-(3-hydroxyphenyl)-7-(2-methoxyphe nyl)-2-methyl-5-oxo-1,4,5,6,7,8-hexahydroquinolin

Uses

HPI-1 is a Hedgehog pathway inhibitor; Gli1/Gli2 inhibitor.

General Description

A cell-permeable oxo-tetrahydroquinolinecarboxylate compound that acts as a downstream Hh (Hedgehog) pathway blocker, effectively inhibiting Gli-dependent transcription activity in both Sufu^+/+ NIH 3T3 (shh-LIGHT2) and Sufu^-/- fibroblast cultures (IC₅₀ = 1.5 & 3 μM, respectively) in a manner similar to two other Hh downstream blockers, HPI-3 (Cat. No. 373276) and GANT-61 (Cat. No. 373401). However, only HPI-1, but not HPI-3 or GANT-61 (no effect at 30 μM), remains effective against Sufu^-/- fibroblasts overexpressing Gli1 or Gli2 (IC₅₀ = 6 & 4 μM, respectively). HPI-1 is also shown to inhibit the ligand-independent Hh pathway activation in SmoM2-expressing primary murine CGNPs (Cerebellar Granule Neuron Precursors) and NIH 3T3 (smoM2-LIGHT) cultures.

Biological Activity

hedgehog (hh) signaling inhibitor. inhibits sonic hedgehog (shh)-, sag- and gli-induced hh pathway activation in shh-light2 cells (ic50 values are 1.5, 1.5, 4 and 6 μm for shh-, sag-, gli2- and gli1-induced activation). also inhibits hh pathway activation

storage

Store at -20°C