Hh Signaling Antagonist XIII, HPI-3

A cell-permeable piperazinyl-quinazoline 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 = 3 & 9 µM, respectively) in a manner similar to two other Hh downstream blockers, HPI-1 (Cat. No. 373275) and GANT-61 (Cat. No. 373401). However, unlike HPI-1, HPI-3′s inhibitory activity against Su(fu)^-/- fibroblasts is completely abolished by Gli1 or Gli2 overexpression. While both HPI-1 and HPI-3 are shown to inhibit the ligand-independent Hh pathway activation in SmoM2-expressing NIH 3T3 cultures (IC₅₀ = 2.5 & 1 µM, respectively), only HPI-1, but not HPI-3, is able to effectively suppress the SmoM2-induced Hh pathway activation in primary murine CGNPs (Cerebellar Granule Neuron Precursors) cultures.

Packaged under inert gas

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Hyman, J.M., et al. 2009. Proc. Natl. Acad. Sci. USA106, 14132.

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Toxicity: Standard Handling (A)