SAG

Smoothened ligand



ALX-270-426-M001	1 mg	207.00 USD

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

Identity:	Identity determined by HR-MS, ¹H- and ¹³C-NMR.

Formula:	C₂₈H₂₈ClN₃OS

MW:	490.1

Purity:	≥95% (HR-MS, ¹H-NMR, ¹³C-NMR)

Appearance:	White to off-white solid.

CAS:	364590-63-6

Solubility:	Soluble in water (5mg/ml) or DMSO (10mg/ml).

Long Term Storage:	-20°C

Use/Stability:	Stable for at least 6 moths when stored at -20°C.

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Product Literature References

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