Biochem/physiol Actions

Reversible: no

Product does not compete with ATP.

Cell permeable: yes

Target IC₅₀: 20 nM as antagonist of the Shh (Sonic Hedgehog) signaling pathway in the Shh-LIGHT2 assay and in Ptch1-l- cells

Primary TargetShh (Sonic Hedgehog) signaling pathway

General description

A potent, cell-permeable antagonist of the Shh (Sonic Hedgehog) signaling pathway (IC₅₀ = 20 nM in the Shh-LIGHT2 assay and in Ptch1^-l- cells) by binding directly to Smoothened (Smo; K_d = 1.2 nM), a distant relative of G protein-coupled receptors. Unlike cyclopamine (Cat. No. 239803), SANT-1 equipotently inhibits the activities of both wild-type and oncogenic Smo (IC₅₀ = 30 nM in SmoA1-LIGHT2 assay).

A potent antagonist of the Sonic Hedgehog (Shh) signaling pathway (IC₅₀ = 20 nM in Shh-LIGHT2 assay and in Ptch1^-l-< cells) that acts by binding to Smoothened (Smo; K_D = 1.2 nM), a distant relative of G protein-coupled receptors. In contrast to cyclopamine, SANT-1 inhibits the activities of both wild type and oncogenic Smo with equal potency (IC₅₀ = 30 nM in SmoA1-LIGHT2 assay).

Legal Information

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

Other Notes

Chen, J.K., et al. 2002. Proc. Natl. Acad. Sci. USA 99, 14071.Frank-Kamenetsky, M., et al. 2002. J. Biol.1, 10.

Packaging

Packaged under inert gas

5 mg in Plastic ampoule

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.r>r>r>r>From Catalog:r>Desc. Field- added "cell-permeable"

Warning

Toxicity: Standard Handling (A)