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SANT 1 (CAS 304909-07-7) LS-H107

SAG agonist
LS-H107-1 / 1 mg / $195
LS-H107-5 / 5 mg / $225
LS-H107-10 / 10 mg / $255
USA Shipment Only
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Description: Smoothened (SMO) is a GPCR-like receptor which, with Patched, mediates hedgehog signaling to regulate gene expression through the Gli transcription factors. SANT 1 is a potent inhibitor of hedgehog signaling that acts by directly antagonizing SMO (IC50 = 20 nM). It counteracts SMO activation by the SMO agonist SAG but only partially competes with SAG binding to SMO. SANT 1 targets inactive SMO while it is in the cytoplasm, before it relocates to the primary cilium and is activated. Through antagonism of SMO, SANT 1 represses Gli-mediated transcription in a variety of cell types. H107_ChemicalStructureImage.png
N-[(3,5-dimethyl-1-phenyl-1H-pyrazol-4-yl)methylene]-4-(phenylmethyl)-1-piperazinamine
 
biochemical, chemical, agonist
LS-H107
304909-07-7
C23H27N5
≥98%
A crystalline solid
 
CC(N(C1=CC=CC=C1)N=C2C)=C2/C=N/N(CC3)CCN3CC4=CC=CC=C4
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+
FOORCIAZMIWALX-JJIBRWJFSA-N
Shipped Ambient, store at -20°C, ≥ 2 years shelf life.
This product is for research use only. Not for administration to humans, or for human or veterinary diagnostic or therapeutic use.
Data Sheet DataSheet    SDS SDS
Related Products: smo-smoothened related products

Usage Information

SANT 1 is supplied as a crystalline solid. A stock solution may be made by dissolving the SANT 1 in the solvent of choice. SANT 1 is soluble in organic solvents such as ethanol, DMSO, and dimethyl formamide, which should be purged with an inert gas. The solubility of SANT 1 in these solvents is approximately 5, 3, and 10 mg/ml, respectively. SANT 1 is sparingly soluble in aqueous solutions. To enhance aqueous solubility, dilute the organic solvent solution into aqueous buffers or isotonic saline. If performing biological experiments, ensure the residual amount of organic solvent is insignificant, since organic solvents may have physiological effects at low concentrations. We do not recommend storing the aqueous solution for more than one day.

References:
  1. Ruiz-Gómez, A., Molnar, C., Holguín, H., et al. The cell biology of Smo signalling and its relationships with GPCRs. Biochim. Biophys. Acta 1768(4), 901-912 (2007).
  2. Chen, J.K., Taipale, J., Young, K.E., et al. Small molecule modulation of smoothened activity. Proc. Natl. Acad. Sci. USA 99(22), 14071-14076 (2002).
  3. Rominger, C.M., Bee, W.-L.T., Copeland, R.A. , et al. Evidence for allosteric interactions of antagonist binding to the smoothened receptor. J. Pharmacol. Exp. Ther. 329(3), 995-1005 (2009).
  4. Stanton, B.Z. and Peng, L.F. Small-molecule modulators of the Sonic Hedgehog signaling pathway. Mol. BioSyst. 6(1), 44-54 (2010).
  5. Scales, S.J. and de Sauvage, F.J. Mechanisms of hedgehog pathway activation in cancer and implications for therapy. Trends Pharmacol. Sci. 30(6), 303-312 (2009).

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