盐酸白屈菜红碱 T3419

Product Introduction
Bioactivity


英文名: Chelerythrine chloride

描述: Chelerythrine chloride 是一种可渗透细胞的蛋白激酶 C 抑制剂，对磷酸盐受体具有竞争性，而对 ATP 是非竞争性的。它诱导细胞凋亡和自噬。

细胞实验: Chelerythrine is dissolved in DMSO. Cell viability is evaluated via MTT assay. Cells (2×103?HEK-293 cells/well and 3×103?SW-839 cells/well) in 100 μL medium are seeded into 96-well plates, and incubated for 12 h. Next, the medium in each well is replaced with medium containing various concentrations of Chelerythrine Chloride, and the cells are incubated at 37°C for an additional 24 and 48 h. Subsequently, 20 μL MTT (5 mg/mL) is added to each well. Following an additional incubation at 37°C for 4 h, the supernatant is removed, and 100 μL DMSO is added to each well. The absorbance values (read at 540 nm) are determined using the iMark? Microplate Absorbance Reader. The data are analyzed using Microplate Manager software (ver. 6.3; 1689520).

体外活性: Chelerythrine inhibits the BclXL-Bak BH3 peptide binding with IC50 of 1.5 μM. It displaced Bax, a BH3-containing protein, from BclXL. Mammalian cells treated with Chelerythrine undergoes apoptosis with characteristic features that suggest involvement of the mitochondrial pathway[1]. Chelerythrine treatment inhibits LPS-induced TNF-α level and NO production in LPS-induced murine peritoneal macrophages through selective inhibition of p38 mitogen-activated protein kinase (MAPK) and extracellular signal-regulated protein kinases 1 and 2 (ERK1/2) activation. In addition, the effects of chelerythrine on NO and cytokine TNF-α production can possibly be explained by the role of p38 MAPK and ERK1/2 in the regulation of inflammatory mediators expression[2]. Chelerythrine shows cytotoxic effect on the human monocytic leukaemia cells with LD50 value of 3.46 μM. Two hours after LPS stimulation, cells influenced by sanguinarine and Chelerythrine significantly decline the CCL-2 expression by a factors of 3.5 and 1.9[3]. Chelerythrine chloride significantly enhances the phosphorylation of ERK1/2 in a dose-dependent manner. In addition, chelerythrine chloride inhibits the phosphorylation of p38[4].

体内活性: Chelerythrine shows significant anti-inflammatory effects in experimentally induced mice, endotoxic shock model, in vivo through inhibition of LPS-induced tumor necrosis factor-alpha (TNF-α) level and nitric oxide (NO) production in serum[2]. Chelerythrine chloride (5 mg/kg/day, i.p.) induces apoptosis of RCC cells without significant toxicity to mice. Chelerythrine Chloride treatment leads to the accumulation of p53 in a dose-dependent manner[4].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 3.8 mg/mL(10 mM)


关键字: Protein kinase C | Chelerythrine chloride | inhibit | Bcl-2 Family | Chelerythrine Chloride | PKC | Chelerythrine | Apoptosis | Autophagy | Inhibitor

相关产品: Oxcarbazepine | Taurochenodeoxycholic Acid | Novobiocin | MY-1076 | Pyrogallol | ICG-001 | NSC 15364 | Nortrachelogenin | CDKI-73 | Aloperine

相关库: Oxidation-Reduction Compound Library | Anti-Cancer Compound Library | Inhibitor Library | Kinase Inhibitor Library | Alkaloid Natural Product Library | Traditional Chinese Medicine Monomer Library | Anti-Cancer Active Compound Library | Natural Product Library for HTS | TGF-beta/Smad Compound Library | Anti-Cardiovascular Disease Compound Library

盐酸白屈菜红碱 T3419信息由TargetMol中国为您提供，如您想了解更多关于盐酸白屈菜红碱 T3419报价、型号、参数等信息，欢迎来电或留言咨询。

注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途