GSK 525768A
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.
GSK 525768A是I-BET-762的无活性立体异构体,而I-BET-762是一种选择性的BET家族抑制剂,IC50值为35 nM[1]。
BET(溴区和额外的末端结构域) 蛋白有4个成员,分别为BRD2、BDR3、BRD4和BRDT,在调节转录中起重要作用。BET参与巨噬细胞对促炎细胞因子产生的抑制过程,对肿瘤细胞具有有效的抗增殖效应[2]。
I-BET-762是一种有效的BET抑制剂,抑制巨噬细胞源性促炎细胞因子的产生[1]。在幼稚CD4+ T细胞中,I-BET-762处理2天后上调抗炎细胞因子的产生(IL-10、Lag 3和Egr2),并下调促炎细胞因子的产生(GM-CSF和IL-17)[3]。
在LPS处理的C57BL/6小鼠中,与对照GSK 525768A处理组相比,I-BET-762(5mg/kg,i.p.)给药后显著抑制LPS诱导的急性炎症反应[1]。在产生IL-17的2D2 T细胞受体继转移EAE小鼠模型中,与GSK 525768A 处理相比,T细胞用I-BET-762预处理可抑制T细胞介导的炎症,并减少巨噬细胞的募集[3]。
参考文献:
[1]. Nicodeme, E., et al., Suppression of inflammation by a synthetic histone mimic. Nature, 2010. 468(7327): p. 1119-23.
[2]. Bartholomeeusen, K., et al., Bromodomain and extra-terminal (BET) bromodomain inhibition activate transcription via transient release of positive transcription elongation factor b (P-TEFb) from 7SK small nuclear ribonucleoprotein. J Biol Chem, 2012. 287(43): p. 36609-16.
[3]. Bandukwala, H.S., et al., Selective inhibition of CD4+ T-cell cytokine production and autoimmunity by BET protein and c-Myc inhibitors. Proc Natl Acad Sci U S A, 2012. 109(36): p. 14532-7.
Storage | Store at -20°C |
M.Wt | 423.9 |
Cas No. | 1260530-25-3 |
Formula | C22H22ClN5O2 |
Synonyms | GSK525768A;GSK-525768A |
Solubility | Soluble in DMSO |
Chemical Name | 2-[(4R)-6-(4-chlorophenyl)-8-methoxy-1-methyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepin-4-yl]-N-ethylacetamide |
SDF | Download SDF |
Canonical SMILES | CCNC(=O)CC1C2=NN=C(N2C3=C(C=C(C=C3)OC)C(=N1)C4=CC=C(C=C4)Cl)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。 |