SANT-1

Names

[ Name ]:
SANT-1

[Synonym ]:
(E)-N-(4-Benzylpiperazin-1-yl)-1-(3,5-dimethyl-1-phenyl-1H-pyrazol-4-yl)methanimine
SANT-1
(4-Benzyl-piperazin-1-yl)-(3,5-dimethyl-1-phenyl-1H-pyrazol-4-ylmethylene)-amine
Shh Signaling Antagonist V
(E)-N-(4-Benzyl-1-piperazinyl)-1-(3,5-dimethyl-1-phenyl-1H-pyrazol-4-yl)methanimine
1-Piperazinamine (N-[(3,5-dimethyl-1-phenyl-1H-pyrazol-4-yl)methylene]-4-(phenylmethyl)
1-Piperazinamine, N-[(1E)-(3,5-dimethyl-1-phenyl-1H-pyrazol-4-yl)methylene]-4-(phenylmethyl)-

Biological Activity

[Description]:

SANT-1 is a potent Smo antagonist, inhibits Hedgehog signaling, with IC50s of 20 nM and 30 nM in Shh-LIGHT2 and SmoA1-LIGHT2 assay, respectively[1].

[Related Catalog]:

Signaling Pathways >> Stem Cell/Wnt >> Smo

Research Areas >> Cancer

Signaling Pathways >> Stem Cell/Wnt >> Hedgehog

[Target]

IC50: 20 nM (Shh signaling), 30 nM (SmoA1)[1]

[References]

[1]. Chen JK, et al. Small molecule modulation of Smoothened activity. Proc Natl Acad Sci U S A. 2002 Oct 29;99(22):14071-6.

Chemical & Physical Properties

[ Density]:
1.13g/cm3

[ Boiling Point ]:
547.4ºC at 760mmHg

[ Melting Point ]:
104-106ºC

[ Molecular Formula ]:
C₂₃H₂₇N₅

[ Molecular Weight ]:
373.49

[ Flash Point ]:
284.8ºC

[ Exact Mass ]:
373.22700

[ PSA ]:
36.66000

[ LogP ]:
3.51660

[ Index of Refraction ]:
1.623

[ Storage condition ]:
−20°C

[ Water Solubility ]:
Soluble in DMSO with warming

Safety Information

[ Personal Protective Equipment ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ RIDADR ]:
NONH for all modes of transport

Precursor & DownStream

Precursor

DownStream

Articles

Smoothened adopts multiple active and inactive conformations capable of trafficking to the primary cilium.

PLoS ONE 4(4) , e5182, (2009)

Activation of Hedgehog (Hh) signaling requires the transmembrane protein Smoothened (Smo), a member of the G-protein coupled receptor superfamily. In mammals, Smo translocates to the primary cilium up...

MicroRNA-602 and microRNA-608 regulate sonic hedgehog expression via target sites in the coding region in human chondrocytes.

Arthritis Rheumatology 67(2) , 423-34, (2015)

Hedgehog (HH) signaling has recently been associated with cartilage degradation in osteoarthritis (OA). Because interleukin-1β (IL-1β) has been implicated as a principal instigator of OA, we sought to...

MRT-92 inhibits Hedgehog signaling by blocking overlapping binding sites in the transmembrane domain of the Smoothened receptor.

FASEB J. 29 , 1817-29, (2015)

The Smoothened (Smo) receptor, a member of class F G protein-coupled receptors, is the main transducer of the Hedgehog (Hh) signaling pathway implicated in a wide range of developmental and adult proc...