RWJ-56110 dihydrochloride is a potent, selective, peptide-mimetic inhibitor of PAR-1 activation and internalization (binding IC50=0.44 uM) and shows no effect on PAR-2, PAR-3, or PAR-4. RWJ-56110 dihydrochloride inhibits the aggregation of human platelets induced by both SFLLRN-NH2 (IC50=0.16 μM) and thrombin (IC50=0.34 μM), quite selective relative to U46619 . RWJ-56110 dihydrochloride blocks angiogenesis and blocks the formation of new vessels in vivo. RWJ-56110 dihydrochloride induces cell apoptosis[1][2].
Proteinase-activated receptors (PARs) are a family of G protein-coupled receptors activated by the proteolytic cleavage of their N-terminal extracellular domain, exposing a new amino terminal sequence that functions as a tethered ligand to activate the receptors.RWJ56110 inhibits the aggregation of human platelets induced by both SFLLRN-NH2 (IC50=0.16 μM) and thrombin (IC50=0.34 μM) while being quite selective relative to collagen and the thromboxane mimetic U46619 [1].RWJ-56110 dihydrochloride is fully inhibits thrombin-induced RASMC proliferation with an IC50 value of 3.5 μM. RWJ-56110 dihydrochloride shows blockade of thrombin's action with RASMC calcium mobilization (IC50=0.12 μM), as well as with HMVEC (IC50=0.13 μM) and HASMC calcium mobilization (IC50=0.17 μM)[1].RWJ56110 (0.1-10 μM; 24-96 hours) inhibits endothelial cell growth dose-dependently, with half-maximal inhibitory concentration of RWJ56110 is approximately 10 μM[2].RWJ56110 (0.1-10 μM; 6 hours) inhibits DNA synthesis of endothelial cells in a thymidine incorporation assays. Endothelial cells are in fast-growing state (50-60% confluence), RWJ56110 inhibits cell DNA synthesis in a dose-dependent manner, but when cells that are in the quiescent state (100% confluent), the inhibitory effect of PAR-1 antagonists is much less pronounced[2].RWJ56110 (0.1-10 μM; pretreatment for 15 min) inhibits thrombin-induced Erk1/2 activation in a concentration-dependent manner. However, when endothelial cells are stimulated by FBS (final concentration 4%), it reduces partially the activated levels of Erk1/2[2].RWJ56110 (30 μM; 24 hours) has an inhibitory effect on endothelial cell cycle progression. It reduces the percentage of cells in the S phase, while alterations in the percentages of G1 and G2/M cells are less pronounced[2]. Western Blot Analysis[2] Cell Line: Endothelial cells
[1]. Andrade-Gordon, et al.Design, synthesis, and biological characterization of a peptide-mimetic antagonist for a tethered-ligand receptor. oc Natl Acad Sci U S A. 1999 Oct 26;96(22):12257-62. [2]. Panagiota Zania, et al. Blockade of angiogenesis by small molecule antagonists to protease-activated receptor-1: association with endothelial cell growth suppression and induction of apoptosis. J Pharmacol Exp Ther. 2006 Jul;318(1):246-54.
MHY219 is a novel HDAC inhibitor. MHY219 induces apoptosis via up-regulation of androgen receptor expression in human prostate cancer cells. MHY219 was shown to enhance the cytotoxicity on DU145 cells (IC50, 0.36 μM) when compared with LNCaP (IC50, 0.97 μM) and PC3 cells (IC50, 5.12 μM). MHY219 showed a potent inhibition of total HDAC activity when compared with SAHA. MHY219 increased histone H3 hyperacetylation and reduced the expression of class I HDACs (1, 2 and 3) in prostate cancer cells. MHY219 effectively increased the sub-G1 fraction of cells through p21 and p27 dependent pathways in DU145 cells. MHY219 significantly induced a G2/M phase arrest in DU145 and PC3 cells and arrested the cell cycle at G0/G1 phase in LNCaP cells. Furthermore, MHY219 effectively increased apoptosis in DU145 and LNCaP cells, but not PC3 cells, according to Annexin V/PI staining and Western blot analysis. These results indicate that MHY219 is a potent HDAC inhibitor that targets regulating mu......
3X HA Tag(Triple-HA Tag)是一种生物活性肽,由三个重复的 HA 标签(YPYDVPDYA)通过肽键连接而成,主要用于蛋白质和肽的检测以及促进目标蛋白质的功能分析。3X HA Tag 可以被抗 HA 标签的抗体特异性识别和结合,广泛应用于 Western blot、免疫荧光、免疫沉淀等实验技术。
10× TBSTw(TBS with Tween-20)为10倍浓缩的Tris缓冲盐溶液(含Tween-20),即在TBS基础上加入非离子型表面活性剂Tween-20。主要组分包括Tris、Tris-HCl、NaCl和Tween-20,其中Tris/Tris-HCl提供稳定的pH缓冲体系,NaCl维持离子强度,Tween-20作为去污剂降低表面张力、增强洗涤能力并减少非特异性结合。10× TBSTw(TBS with Tween-20)是免疫学实验中最常用的洗涤缓冲液之一,主要用于免疫印迹(Western Blot)、抗体孵育与洗涤、封闭液配置和其他免疫学实验。本产品为10×浓缩液,使用前须用蒸馏水或去离子水稀释至1×工作浓度。
1× TBSTw(TBS with Tween-20)为Tris缓冲盐溶液(含Tween-20),即在TBS基础上加入非离子型表面活性剂Tween-20。主要组分包括Tris、Tris-HCl、NaCl和Tween-20,其中Tris/Tris-HCl提供稳定的pH缓冲体系,NaCl维持离子强度,Tween-20作为去污剂降低表面张力、增强洗涤能力并减少非特异性结合。1× TBSTw(TBS with Tween-20)是免疫学实验中最常用的洗涤缓冲液之一,主要用于免疫印迹(Western Blot)、抗体孵育与洗涤、封闭液配置和其他免疫学实验。