SANT-1 - CAS 304909-07-7 - CALBIOCHEM

General description

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).

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).

Biochem/physiol Actions

Cell permeable: yes

Primary Target
Shh (Sonic Hedgehog) signaling pathway

Product does not compete with ATP.

Reversible: no

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

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.







From Catalog:

Desc. Field- added "cell-permeable"

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.

Legal Information

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

Molecular Weight: 373.49. Empirical Formula: C₂₃H₂₇N₅. Quality Level: 100. Assay: ≥. 95% (HPLC). form: solid. manufacturer/tradename: Calbiochem^®. . storage condition: OK to freeze, protect from light. color: white. solubility: DMSO: 5 . mg/mL. shipped in: ambient. storage temp.: −. 20°C. InChI: 1S/C23H27N5/c1-19-23(20(2)28(25-19)22-11-7-4-8-12-22)17-24-27-15-13-26(14-16-27)18-21-9-5-3-6-10-21/h3-12,17H,13-16,18H2,1-2H3/b24-17+. InChI key: FOORCIAZMIWALX-JJIBRWJFSA-N. Storage Class Code: 11 - Combustible Solids. WGK: WGK 3. Flash Point(F): Not applicable. Flash Point(C): Not applicable.