PF-5274857
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.
PF-5274857是hedgehog (Hh)信号通路的抑制剂，作为Smoothened (Smo)的高效选择性拮抗剂，其IC50值为5.8 nM。
作为G蛋白偶联受体，Smoothened是hedgehog信号通路的组分，从果蝇到人类皆保守。此蛋白是致畸环巴胺的分子靶点。SMO可以作为原癌基因，SMO激活突变导致hedgehog信号通路不受控制的活化和癌症。
通过检测Smo下游基因Gli的转录活性可知，PF-5274857处理MEF细胞能够完全抑制Shh诱导的Hh信号通路活性[1]。
体内试验中，PF-5274857在小鼠髓母细胞瘤模型中表现出抗肿瘤活性，其IC50值为8.9 nM。PF-5274857也能以剂量依赖的方式显著抑制肿瘤生长（TGI）并诱导肿瘤消退。皮肤组织中PF-5274857处理也观察到了类似时间进程的Gli1和Gli2的下调[1]。
参考文献：
Rohner A, Spilker ME, Lam JL, et al. Effective targeting of Hedgehog signaling in a medulloblastoma model with PF-5274857, a potent and selective Smoothened antagonist that penetrates the blood-brain barrier. Molecular cancer therapeutics.2012;11(1):57-65.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 436.96 |
| Cas No. | 1373615-35-0 |
| Formula | C20H25ClN4O3S |
| Solubility | insoluble in EtOH; ≥17.6 mg/mL in H2O with ultrasonic; ≥19.65 mg/mL in DMSO |
| Chemical Name | 1-[4-[5-chloro-4-(3,5-dimethylpyridin-2-yl)pyridin-2-yl]piperazin-1-yl]-3-methylsulfonylpropan-1-one |
| SDF | Download SDF |
| Canonical SMILES | CC1=CC(=C(N=C1)C2=CC(=NC=C2Cl)N3CCN(CC3)C(=O)CCS(=O)(=O)C)C |
| 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 | PF-5274857是Smoothened (Smo)的高效选择性拮抗剂，其IC50值分别为5.8 nM和4.6 nM。 | |||||
| 靶点 | Smoothened | |||||
| IC50 | 5.8 nM (Ki=4.6 nM) | |||||
化学结构
