CZC-25146
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.
CZC-25146是一种选择性的和细胞渗透性的富亮氨酸重复激酶-2 (LRRK2)抑制剂,IC50值为4.76 nM [1].
CZC-25146是LRRK2的二代抑制剂,具有极高的效力和选择性.时间分辨荧光共振能量转移实验中,CZC-25146对重组人野生型LRRK2和G2019S突变型LRRK2都具有高效的抑制活性,IC50值分别为4.76 nM和6.87 nM.CZC-25146选择性抑制LRRK2.在184种蛋白激酶和一种脂类激酶中,CZC-25146只对五种激酶具有高效的抑制作用,包括PLK4\GAK\TNK1\CAMKK2和PIP4K2C.此外,在原代啮齿动物皮层神经元中,CZC-25146能够减缓G2019S LRRK2诱导的细胞损伤和死亡,EC50值为100 nM.CZC-25146也能减轻G2019S LRRK2诱导的人神经元损伤,EC50值为4 nM.但是,在啮齿类动物PD模型中,CZC-25146缺乏足够的脑部暴露[1, 2].
参考文献：
[1] Ramsden N, Perrin J, Ren Z, et al. Chemoproteomics-based design of potent LRRK2-selective lead compounds that attenuate Parkinson’s disease-related toxicity in human neurons. ACS chemical biology, 2011, 6(10): 1021-1028.
[2] Troxler T, Greenidge P, Zimmermann K, et al. Discovery of novel indolinone-based, potent, selective and brain penetrant inhibitors of LRRK2. Bioorganic & medicinal chemistry letters, 2013, 23(14): 4085-4090.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 488.54 |
| Cas No. | 1191911-26-8 |
| Formula | C22H25FN6O4S |
| Solubility | ≥24.45 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O |
| Chemical Name | (E)-N-(2-((5-fluoro-2-((2-methoxy-4-morpholinophenyl)amino)pyrimidin-4(3H)-ylidene)amino)phenyl)methanesulfonamide |
| SDF | Download SDF |
| Canonical SMILES | COC1=C(NC2=NC=C(F)/C(N2)=N\C3=CC=CC=C3NS(C)(=O)=O)C=CC(N4CCOCC4)=C1 |
| 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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化学结构
