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Merck
CN

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.

别名:

SANT-1, Shh Signaling Antagonist V

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关于此项目

经验公式(希尔记法):
C23H27N5
化学文摘社编号:
分子量:
373.49
MDL编号:
UNSPSC代码:
51111800
NACRES:
NA.77
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质量水平

方案

≥95% (HPLC)

表单

solid

制造商/商品名称

Calbiochem®

储存条件

OK to freeze
protect from light

颜色

white

溶解性

DMSO: 5 mg/mL

运输

ambient

储存温度

−20°C

SMILES字符串

[n]2(nc(c(c2C)\C=N\N3CCN(CC3)Cc4ccccc4)C)c1ccccc1

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

一般描述

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).

生化/生理作用

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

包装

Packaged under inert gas

制备说明

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"

其他说明

Chen, J.K., et al. 2002. Proc. Natl. Acad. Sci. USA 99, 14071.
Frank-Kamenetsky, M., et al. 2002. J. Biol.1, 10.

法律信息

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

免责声明

Toxicity: Standard Handling (A)

储存分类代码

11 - Combustible Solids

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable


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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
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
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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