JLK 6
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.
JLK 6是异香豆素,是γ分泌酶的选择性抑制剂,IC50值在10 μM-1 mM之间[1,2]。
γ分泌酶催化β淀粉样前体蛋白(βAPP)裂解生成淀粉样蛋白β肽(Aβ)。 Aβ是阿尔茨海默病患者脑中斑块的一部分。γ分泌酶还针对其它一些底物,例如Notch。Notch是一种跨膜蛋白,在胚胎和成年发育的不同阶段发挥重要功能 [1]。
野生型βAPP在HEK293细胞中过表达(在35毫米孔中浓度为962 fmol/mL)。JLK6显著降低Aβ在这些细胞中的分泌。有趣的是,JLK6增强了两个片段的恢复。免疫学特性表明,单一片段标记了针对Aβ的Asp1残基的特定抗体。同样地,JLK6也可抑制过表达Swedish突变体βAPP的细胞中Aβ的恢复[2]。
在斑马鱼胚胎中,JLK异香豆素抑制剂并没有改变负责体节发生的Notch通路。不同于其他的γ分泌酶抑制剂,这些药物并不影响E-cadherin过程。JLKs并不抑制α分泌酶、β位APP裂解酶(BACE)1和BACE2、GSK3β激酶和蛋白酶体。JLK抑制剂抑制Aβ生成,但不引起其他蛋白质不必要的分解[1]。
参考文献:
[1]. Petit A, Pasini A, Alves Da Costa C, et al. JLK isocoumarin inhibitors: Selective γ-secretase inhibitors that do not interfere with notch pathway in vitro or in vivo. Journal of neuroscience research, 2003, 74(3): 370-377.
[2]. Petit A, Bihel F, da Costa CA, et al. New protease inhibitors prevent γ-secretase-mediated production of Aβ40/42 without affecting Notch cleavage. Nature cell biology, 2001, 3(5): 507-511.
Physical Appearance | Yellow solid |
Storage | Store at RT |
M.Wt | 225.63 |
Cas No. | 62252-26-0 |
Formula | C10H8ClNO3 |
Synonyms | 7-Amino-4-chloro-3-methoxy-1H-2-benzopyran |
Solubility | <22.56mg/ml in DMSO; <5.64mg/ml in ethanol |
Chemical Name | 7-amino-4-chloro-3-methoxy-1H-isochromen-1-one |
SDF | Download SDF |
Canonical SMILES | COC1=C(Cl)C2=CC=C(N)C=C2C(O1)=O |
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。 |