A potent cell-permeable benzothiophene compound that modulates the coupling of Smo with its downstream effector by interacting with the Smo heptahelical domain (KD = 59 nM). Shown to induce Hedgehog pathway activation (EC50= ~3 nM in NIH 3T3-derived Shh-LIGHT2 cells) and counteracts Cyclopamine (BML-GR334) inhibition of Smo. Reported to act as an activator at low concentrations and as an inhibitor at very high concentrations.
Product Specification
| Formula: | C28H28ClN3OS |
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| MW: | 490.1 |
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| CAS: | 364590-63-6 |
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| Purity: | ≥95% (HR-MS, 1H-NMR, 13C-NMR) |
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| Identity: | Determined by HR-MS, 1H- and 13C-NMR. |
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| Appearance: | White to off-white solid. |
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| Solubility: | Soluble in DMSO (10mg/ml), sparingly soluble in water (acidification with HCl increases water solubility). |
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| Shipping: | Ambient |
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| Long Term Storage: | -20°C |
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| Use/Stability: | Stable for at least 6 months when stored at -20°C. |
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Product Literature References
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7, Article number 10351 (2016),
Application(s): Cell culture,
Abstract;
Identification and Correction of Mechanisms Underlying Inherited Blindness in Human iPSC-Derived Optic Cups: D.A. Parfitt, et al.; Cell Stem Cell
18, 769 (2016),
Application(s): Cell culture,
Abstract;
Sequential Differentiation of Embryonic Stem Cells into Neural Epithelial-Like Stem Cells and Oligodendrocyte Progenitor Cells: J. Bian, et al.; PLoS One
11, e0155227 (2016),
Application(s): Cell culture,
Abstract;
Full Text
Modeling amyotrophic lateral sclerosis in pure human iPSc-derived motor neurons isolated by a novel FACS double selection technique: D. Toli, et al.; Neurobiol. Dis.
82, 269 (2015),
Application(s): Cell Culture,
Abstract;
Subregional specification of embryonic stem cell-derived ventral telencephalic tissues by timed and combinatory treatment with extrinsic signals: T. Danjo, et al.; J. Neurosci.
31, 1919 (2011),
Abstract;
Identification of a suppressive mechanism for Hedgehog signaling through a novel interaction of Gli with 14-3-3: Y. Asoaka, et al.; J. Biol. Chem.
285, 4185 (2010),
Abstract;
Full Text
Wnt signaling stimulates transcriptional outcome of the Hedgehog pathway by stabilizing GLI1 mRNA: F.K. Noubissi, et al.; Cancer Res.
69, 8572 (2009),
Abstract;
Full Text
Oxysterols stimulate Sonic hedgehog signal transduction and proliferation of medulloblastoma cells: R.B. Corcoran and M.P. Scott; PNAS
103, 8408 (2006),
Abstract;
Full Text
Smoothened Signal Transduction is Promoted by G-Protein Coupled Receptor Kinase 2: A.R. Meloni et al.; Mol Cell Biol.
26, 7550 (2006),
Abstract;
Activity-dependent internalization of smoothened mediated by beta-arrestin 2 and GRK2: W. Chen, et al.; Science
306, 2257 (2004),
Abstract;
Small molecule modulation of Smoothened activity: J.K. Chen, et al.; PNAS
99, 14071 (2002),
Abstract;
Full Text
Small-molecule modulators of Hedgehog signaling: identification and characterization of Smoothened agonists and antagonists: M. Frank-Kamenetsky, et al.; J. Biol.
1, 10 (2002),
Abstract;
Full Text
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