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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.

Synonym(s):

SANT-1, Shh Signaling Antagonist V

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About This Item

Empirical Formula (Hill Notation):
C23H27N5
CAS Number:
Molecular Weight:
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 Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable


Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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Hsiao-Fan Lo et al.
Development (Cambridge, England), 148(19) (2021-10-06)
Many developmental disorders are thought to arise from an interaction between genetic and environmental risk factors. The Hedgehog (HH) signaling pathway regulates myriad developmental processes, and pathway inhibition is associated with birth defects, including holoprosencephaly (HPE). Cannabinoids are HH pathway
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
Isidora Paredes et al.
Nature neuroscience, 24(4), 478-488 (2021-01-30)
Neural-derived signals are crucial regulators of CNS vascularization. However, whether the vasculature responds to these signals by means of elongating and branching or in addition by building a feedback response to modulate neurodevelopmental processes remains unknown. In this study, we
Emily K Ho et al.
Current biology : CB, 30(14), 2829-2835 (2020-06-13)
The regulation of proliferation is a primary function of Hedgehog (Hh) signaling in development. Hh signal transduction requires the primary cilium for several steps in the pathway [1-5]. Many cells only build a primary cilium upon cell cycle exit, in
Gina La Sala et al.
Journal of neuroscience research (2020-12-23)
Mammalian cerebellar astrocytes critically regulate the differentiation and maturation of neuronal Purkinje cells and granule precursors. The G protein-coupled receptor 37-like 1 (Gpr37l1) is expressed by Bergmann astrocytes and interacts with patched 1 (Ptch1) at peri-ciliary membranes. Cerebellar primary astrocyte

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