SANT1 是Smo拮抗剂，能够抑制Hedgehog通路，在 Shh-LIGHT2 和 SmoA1-LIGHT2 实验中，得到的IC50值分别为 20 nM 和 30 nM。

SANT-1 directly binds to Smoothened (Smo) receptor (Kd: 1.2 nM) and inhibits Smo agonist effects (IC50: 20 nM).

SANT-1对Smo（PKA刺激）运输到近端纤毛的过程有抑制作用。SANT-1对野生型和致癌的Smo的抑制效果相同。在SmoA1-LIGHT2细胞中,SANT-1抑制通路激活,在Shh-LIGHT2实验中显示的作用效力相似。在Shh-LIGHT2和BODIPY-Cyclopamine实验中,SANT-1表现放出不同的抑制活性,且对SAG调节的通路激活有异常有效的抑制作用。SANT-1与SAHA联用,可抑制细胞增殖,并对抗吉西他滨的胰腺癌细胞系Panc-1和BxPC-3的集落形成有抑制作用。

CK1 kinase assay: All protein kinase assays (25 μL) are carried out at room temperature (21℃). Assays are performed for 40 min using a Biomek 2000 Laboratory Automation Workstation in a 96-well format. The concentrations of magnesium acetate and [γ-33P]ATP (800 cpm/pmol) in the assays are 10 mM and 0.1 mM, respectively. Assays are initiated with MgATP and stopped by the addition of 5 μL of 0.5 M orthophosphoric acid. Aliquots are then spotted on to P30 ?ltermats, washed four times in 75 mM phosphoric acid to remove ATP, once in methanol, then dried and counted for radioactivity. CK1 δ (5-20 m-units), diluted in 20 mM Hepes, pH 7.5, 0.15 M NaCl, 0.1 mM EGTA, 0.1% (v/v) Triton X-100, 5 mM dithiothreitol, 50% (v/v) glycerol, is assayed against the peptide RRKDLHDDEEDEAMSITA in an incubation containing 20 mM Hepes, pH 7.5, 0.15 M NaCl, 0.1 mM EDTA, 5 mM DTT, 0.1% (v/v) Triton X-100 and 0.5 mM substrate peptide.

304909-07-7

C23H27N5

373.504

SANT 1

DMSO:18.7 mg/mL (50 mM)
Ethanol:9.3 mg/mL (25 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years