LY2940680
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.
LY2940680是Smo受体的选择性抑制剂，可抑制Hh信号通路[1]。
Smoothened（SMO）受体是F型G蛋白偶联受体的成员，参与Hedgehog（Hh）信号通路的传导，在发育和成长过程中发挥重要的作用[2]。
LY2940680是一种强效的Smo受体抑制剂，主要结合在胞外环，与已报道的结合在7TM位点的Smo受体抑制剂SANT-1具有不同的作用位点[2]。在基因编码的Smoothened突变细胞系和对vismodegib具有抗性的癌症患者中，LY2940680抑制细胞增殖[3]。
研究表明，Hh信号通路在CSCs中起关键作用，Hh抑制引起的多方面的转变都归因于CSCs。作为单一疗法，LY2940680对基底细胞癌和髓母细胞瘤患者显示出良好的药效[1]。
参考文献：
[1]. Justilien, V. and A.P. Fields, Molecular pathways: novel approaches for improved therapeutic targeting of Hedgehog signaling in cancer stem cells. Clin Cancer Res, 2015. 21(3): p. 505-13.
[2].Hoch, L., et al., MRT-92 inhibits Hedgehog signaling by blocking overlapping binding sites in the transmembrane domain of the Smoothened receptor. Faseb j, 2015. 29(5): p. 1817-29.
[3].Redmond, E.M., et al., Investigational Notch and Hedgehog inhibitors--therapies for cardiovascular disease. Expert Opin Investig Drugs, 2011. 20(12): p. 1649-64.
| Physical Appearance | A crystalline solid |
| Storage | Store at -20°C |
| M.Wt | 512.5 |
| Cas No. | 1258861-20-9 |
| Formula | C26H24F4N6O |
| Solubility | insoluble in H2O; ≥5.2 mg/mL in EtOH with ultrasonic; ≥51.3 mg/mL in DMSO with gentle warming and ultrasonic |
| Chemical Name | 4-fluoro-N-methyl-N-[1-[4-(2-methylpyrazol-3-yl)phthalazin-1-yl]piperidin-4-yl]-2-(trifluoromethyl)benzamide |
| SDF | Download SDF |
| Canonical SMILES | CN1C(=CC=N1)C2=NN=C(C3=CC=CC=C32)N4CCC(CC4)N(C)C(=O)C5=C(C=C(C=C5)F)C(F)(F)F |
| 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。 |
| 描述 | LY2940680是Smoothened（SMO）受体和Hedgehog（Hh）信号的有效抑制剂。 | |||||
| 靶点 | Smoothened | |||||
| IC50 | ||||||
质量控制和MSDS
- 批次:
化学结构
