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Key Documents

559303

Sigma-Aldrich

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.

Sinónimos:

SANT-1, Shh Signaling Antagonist V

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About This Item

Fórmula empírica (notación de Hill):
C23H27N5
Número de CAS:
Peso molecular:
373.49
MDL number:
UNSPSC Code:
51111800
NACRES:
NA.77

Quality Level

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

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; KD = 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; Kd = 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

Storage Class

11 - Combustible Solids

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable


Certificados de análisis (COA)

Busque Certificados de análisis (COA) introduciendo el número de lote del producto. Los números de lote se encuentran en la etiqueta del producto después de las palabras «Lot» o «Batch»

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Kostadin Petrov et al.
Developmental cell, 55(3), 314-327 (2020-08-30)
Cholesterol plays two critical roles in Hedgehog signaling, a fundamental pathway in animal development and cancer: it covalently modifies the Sonic hedgehog (SHH) ligand, restricting its release from producing cells, and directly activates Smoothened in responding cells. In both contexts

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