559303

SANT-1

A potent, cell-permeable antagonist of the Shh signaling pathway by binding directly to Smoothened, a distant relative of G protein-coupled receptors.

• Synonym(s): SANT-1, Shh Signaling Antagonist V
• Empirical Formula (Hill Notation): C₂₃H₂₇N₅
• CAS Number: 304909-07-7
• Molecular Weight: 373.49
• MDL number: MFCD01827306
• UNSPSC Code: 51111800
• NACRES: NA.77

Properties

• 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

Description

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

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable