WAY 316606 HCl
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.
WAY316606是分泌型卷曲相关蛋白1(sFRP1)的选择性小分子抑制剂,其EC50值为0.65 μM[1]。
Wnt信号通路已被证明是一个治疗代谢性骨病(如骨质疏松症)的药物靶点。研究发现,在老龄小鼠中,Wnt拮抗剂的功能丧失性突变促进骨形成,另外,去除Wnt拮抗剂sFRP-1也可以促进骨小梁形成。因此,Wn拮抗剂(sFRP-1)的小分子抑制剂已被研发出。WAY 316606是通过基于细胞的试验以测定Wnt信号通路的激活,从超过440,000个化合物的数据库中筛选出的。WAY316606选择性地结合sFRP-1(Kd = 0.08 μM),抑制sFRP-1引起的Wnt通路负调控。器官培养试验表明,WAY316606促进骨形成[1]。
WAY316606是sFRP-1的选择性抑制剂,其对sFRP-2具有10倍更弱的亲和力(Kd = 1 μM)。在荧光偏振结合试验中,WAY316606抑制sFRP-1,其IC50值为0.5 μM。虽然sFRP-1、sFRP-2和sFRP-3的序列高度相似,相对于其它两种蛋白质,WAY316606选择性地抑制sFRP-1。在基于细胞的瞬时转染和荧光素酶报告试验中,使用骨肉瘤细胞U2-OS, WAY316606呈剂量依赖性地激活Wnt信号通路,其EC50值为0.65 μM。在离体试验中,使用新生鼠颅盖,WAY316606呈剂量依赖性地增强成骨细胞活性,促进高达60%的骨形成,其EC50值为1 nM[1,2]。
虽然WAY316606具有良好的水溶性和稳定性,大鼠对WAY316606的血浆清除率高(77 mL/min/kg)。作为一种口服给药的代谢性骨疾病药物,高血浆清除率抑制该药物持续暴露,限制该化合物发展[1]。
参考文献:
[1] Bodine P V N, Stauffer B, Ponce-de-Leon H, et al. A small molecule inhibitor of the Wnt antagonist secreted frizzled-related protein-1 stimulates bone formation. Bone, 2009, 44(6): 1063-1068.
[2] Moore W J, Kern J C, Bhat R, et al. Modulation of Wnt Signaling Through Inhibition of Secreted Frizzled-Related Protein I (sFRP-1) with N-Substituted Piperidinyl Diphenylsulfonyl Sulfonamides. Journal of medicinal chemistry, 2008, 52(1): 105-116.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 484.94 |
Cas No. | 915759-45-4 (free base) |
Formula | C18H19F3N2O4S2·HCI |
Synonyms | WAY-316606 HCl;WAY316606 HCl |
Solubility | ≥24.25 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH |
Chemical Name | 5-(phenylsulfonyl)-N-(piperidin-4-yl)-2-(trifluoromethyl)benzenesulfonamide hydrochloride |
SDF | Download SDF |
Canonical SMILES | O=S(NC1CCNCC1)(C2=C(C(F)(F)F)C=CC(S(=O)(C3=CC=CC=C3)=O)=C2)=O.Cl |
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。 |
质量控制和MSDS
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