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(e):
SANT-1, Shh Signaling Antagonist V
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Alle Fotos(1)
About This Item
Empirische Formel (Hill-System):
C23H27N5
CAS-Nummer:
Molekulargewicht:
373.49
MDL-Nummer:
UNSPSC-Code:
51111800
NACRES:
NA.77
Empfohlene Produkte
Qualitätsniveau
Assay
≥95% (HPLC)
Form
solid
Hersteller/Markenname
Calbiochem®
Lagerbedingungen
OK to freeze
protect from light
Farbe
white
Löslichkeit
DMSO: 5 mg/mL
Versandbedingung
ambient
Lagertemp.
−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+
InChIKey
FOORCIAZMIWALX-JJIBRWJFSA-N
Allgemeine Beschreibung
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. Wirkung
Cell permeable: yes
Primary Target
Shh (Sonic Hedgehog) signaling pathway
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
Verpackung
Packaged under inert gas
Warnhinweis
Toxicity: Standard Handling (A)
Rekonstituierung
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"
From Catalog:
Desc. Field- added "cell-permeable"
Sonstige Hinweise
Chen, J.K., et al. 2002. Proc. Natl. Acad. Sci. USA 99, 14071.
Frank-Kamenetsky, M., et al. 2002. J. Biol.1, 10.
Frank-Kamenetsky, M., et al. 2002. J. Biol.1, 10.
Rechtliche Hinweise
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Lagerklassenschlüssel
11 - Combustible Solids
WGK
WGK 3
Flammpunkt (°F)
Not applicable
Flammpunkt (°C)
Not applicable
Analysenzertifikate (COA)
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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
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
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
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
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