Ro 26-4550 trifluoroacetate
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.
IC50:3 μM
Ro 26-4550 trifluoroacetate是一种白细胞介素-2(IL-2)与其受体结合的竞争性可逆抑制剂。[1]
白细胞介素-2(IL-2)(15.5 kDa的细胞因子)在活化T细胞的生长中起主导作用。IL-2诱导T细胞增殖,随后在T细胞表面结合,对异源三聚体受体复合物(由R、及链组成)具有皮摩尔亲和力。已证明其作为免疫抑制剂临床有效,抗体识别R受体亚基(IL-2RR)并破坏 IL-2的结合。小分子能够防止IL-2 / IL-2RR相互作用,可作为抗体药物潜在的口服活性接替药物[1]。
体外:与Ro 26-4550结合而被扰乱的IL-2区域证实参与与IL-2RR的结合。这表明,Ro 26-4550在IL-2上竞争结合IL-2RR的结合位点,以干扰IL-2 / IL-2RR结合。 [1]。
Ro 26-4550结合IL-2“热点”的X射线结构分析表明,该蛋白是可变的,然后进行显著的重排以创建小分子结合位点。这一观察驳斥了蛋白质-蛋白质相互作用是单调和无特征的观点,并且表明IL-2的表面可以存在其他不明显的结合位点(以高亲和力结合小分子)。但是,由于该位点的适应特性,基于结构的准确预测将更加困难。 [2]
体内:目前尚未进行体内研究。
临床试验:目前尚未进行临床研究。
参考文献:
[1]. Tilley JW, Chen L, Fry DC, Emerson SD, Powers GD, Biondi D, Varnell T, Trilles R, Guthrie R, Mennona F, Kaplan G, LeMahieu RA, Carson M, Han R-J, Liu C-M, Palermo R, Ju G. Identification of a small molecule inhibitor of the IL-2/IL-2Rr receptor interaction which binds to IL-2. J. Am. Chem. Soc. 1997, 119, 7589-7590
[2] Braisted AC, Oslob JD, Delano WL, Hyde J, McDowell RS, Waal N, Yu C, Arkin MR, Raimundo BC. Discovery of a potent small molecule IL-2 inhibitor through fragment assembly. J Am Chem Soc. 2003 Apr 2;125(13):3714-5.
Physical Appearance | White solid |
Storage | Store at -20°C |
M.Wt | 560.57 |
Cas No. | 1217448-66-2 |
Formula | C26H30N4O3·CF3CO2H |
Solubility | <28.03mg/ml in DMSO;insoluble in ethanol |
Chemical Name | (S)-methyl 2-(2-((R)-1-carbamimidoylpiperidin-3-yl)acetamido)-3-(4-(phenylethynyl)phenyl)propanoate 2,2,2-trifluoroacetate |
SDF | Download SDF |
Canonical SMILES | OC(C(F)(F)F)=O.NC(N1CCC[C@H](CC(N[C@H](C(OC)=O)CC2=CC=C(C#CC3=CC=CC=C3)C=C2)=O)C1)=N |
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。 |