SANT-1
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
SANT-1是一种新型分子,通过结合smoothened蛋白发挥抗肿瘤效应[1].
Smoothened是两种类型整合膜蛋白之一,调节Hh信号通路的活化,Hh信号通路是靶向细胞分化和增殖的过程.此外,Smoothened功能异常与人类肿瘤的发生相关[1].
高通量实验表明SANT-1是四种Smoothened 拮抗剂之一,也是对Smoothened蛋白最具拮抗效应的分子[1].在两个健康细胞系 (Shh-LIGHT2和SmoA1-LIGHT2细胞系) 中,30小时处理后SANT-1能够抑制两种细胞,IC50值分别为20和30 nM.此外,在四种分子中SANT-1对Smoothened蛋白具有最高的亲和力,KDs为1.2 nM[1].在胰腺癌细胞系中,SANT-1能够抑制Panc-1细胞系,IC50值为100 μM.另外,SANT-1与SAHA(组蛋白去乙酰化酶)联合给药能通过协同抑制Hh通路活性而增强抗肿瘤效应[2].
SANT-1目前尚无体内试验.
参考文献:
[1]. Chen J K., Taipale J, Young K E,. Small molecule modulation of Smoothened activity. Proc Natl Acad Sci U S A, 2002, 99: 14071-6.
[2]. Chun SG, Zhou W & Yee N S. Combined targeting of histone deacetylases and hedgehog signaling enhances cytoxicity in pancreatic cancer. Cancer Biol Ther, 2009, 8: 1328-39.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 373.5 |
Cas No. | 304909-07-7 |
Formula | C23H27N5 |
Solubility | insoluble in H2O; insoluble in EtOH; ≥18.75 mg/mL in DMSO |
Chemical Name | (E)-N-(4-benzylpiperazin-1-yl)-1-(3,5-dimethyl-1-phenylpyrazol-4-yl)methanimine |
SDF | Download SDF |
Canonical SMILES | CC1=C(C(=NN1C2=CC=CC=C2)C)C=NN3CCN(CC3)CC4=CC=CC=C4 |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
Description | SANT-1是Smoothened (Smo)的抑制剂,Kd值为1.2 nM,IC50值为20 nM. | |||||
靶点 | Smoothened | |||||
IC50 | 20 nM (Kd=1.2 nM) |
质量控制和MSDS
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