An antagonist of Smoothened
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SANT 1

Item No. 14933

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[(3,5-dimethyl-1-phenyl-1H-pyrazol-4-yl)methylene]-4-(phenylmethyl)-1-piperazinamine
CAS Number
304909-07-7
Molecular Formula
C23H27N5
Formula Weight
373.5
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 10 mg/mlDMSO: 3 mg/mlEthanol: 5 mg/ml
λmax
284 nm
SMILES
CC(N(C1=CC=CC=C1)N=C2C)=C2/C=N/N(CC3)CCN3CC4=CC=CC=C4
InChi Code
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
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $69

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    5 mg

    $118

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    10 mg

    $185

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    Product Description

    Smoothened (SMO) is a GPCR-like receptor which, with Patched, mediates hedgehog signaling to regulate gene expression through the Gli transcription factors.1 SANT 1 is a potent inhibitor of hedgehog signaling that acts by directly antagonizing SMO (IC50 = 20 nM).2 It counteracts SMO activation by the SMO agonist SAG but only partially competes with SAG binding to SMO.2,3 SANT 1 targets inactive SMO while it is in the cytoplasm, before it relocates to the primary cilium and is activated.4 Through antagonism of SMO, SANT 1 represses Gli-mediated transcription in a variety of cell types.4,5

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description 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).