Chelerythrine-Chloride - PKC 抑制劑 - 生命科學(xué)試劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEChelerythrine ChlorideCat. No.: HY-12048CAS No.: 3895-92-9分式: CHClNO分量: 383.82作靶點: PKC; Autophagy作通路: Epigenetics; TGF-beta/Smad; Autophagy儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 4.

2、35 mg/mL (11.33 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 2.6054 mL 13.0269 mL 26.0539 mL5 mM 0.5211 mL 2.6054 mL 5.2108 mL10 mM 0.2605 mL 1.3027 mL 2.6054 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。體內(nèi)實驗 請根據(jù)您的實驗動物和給藥式選擇適當(dāng)?shù)娜芙獍?，配制前請先配制澄清的儲備液，再依次添加助溶?為保證實驗結(jié)果的可靠性，體內(nèi)實驗的作液

3、，建議您現(xiàn)現(xiàn)配，當(dāng)天使；澄清的儲備液可以根據(jù)儲存條件，適當(dāng)保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 0.43 mg/mL (1.12 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 0.44 mg/mL (1.15 mM); Clear solution3. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolub

4、ility: 0.44 mg/mL (1.15 mM); Clear solution1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEBIOLOGICAL ACTIVITY物活性 Chelerythrine Chloride種有效，可滲透細胞的蛋酶 C (protein kinase C) 抑制劑，能夠抑制 PKC 活性，IC50 值為 660 nM。IC50 & Target PKC PKA TPK660 nM (IC50) 0.17 mM (IC50) 0.1 mM (IC50)體外研究 Chelerythrine inhibits the

5、 BclXL-Bak BH3 peptide binding with IC50 of 1.5 M and displaces Bax, a BH3-containing protein, from BclXL. Mammalian cells treated with Chelerythrine undergoes apoptosis withcharacteristic features that suggest involvement of the mitochondrial pathway 1. Chelerythrine treatmentinhibits LPS-induced T

6、NF- level and NO production in LPS-induced murine peritoneal macrophages throughselective inhibition of p38 mitogen-activated protein kinase (MAPK) and extracellular signal-regulated proteinkinases 1 and 2 (ERK1/2) activation. Moreover, the effects of chelerythrine on NO and cytokine TNF-production

7、can possibly be explained by the role of p38 MAPK and ERK1/2 in the regulation of inflammatorymediators expression 2. Chelerythrine shows cytotoxic effect on the human monocytic leukaemia cells withLD50 value of 3.46 M. Two hours after LPS stimulation, cells influenced by sanguinarine and Chelerythr

8、inesignificantly decline the CCL-2 expression by a factors of 3.5 and 1.9 3. Chelerythrine chloride significantlyenhances the phosphorylation of ERK1/2 in a dose-dependent manner. In addition, chelerythrine chlorideinhibits the phosphorylation of p38 4.體內(nèi)研究 Chelerythrine displays significant anti-in

9、flammatory effects in experimentallyinduced mice endotoxic shock model in vivo through inhibition of LPS-induced tumor necrosis factor-alpha(TNF-) level and nitric oxide (NO) production in serum 2. Chelerythrine chloride (5 mg/kg/day, i.p.) inducesapoptosis of RCC cells without significant toxicity

10、to mice. Chelerythrine Chloride treatment leads to a dose-dependent accumulation of p53 4.PROTOCOLCell Assay 1 Cell viability is evaluated via MTT assay. Cells (2103 HEK-293 cells/well and 3103 SW-839 cells/well) in100 L medium are seeded into 96-well plates, and incubated for 12 h. Next, the medium

11、 in each well isreplaced with medium containing various concentrations of Chelerythrine Chloride, and the cells areincubated at 37C for an additional 24 and 48 h. Subsequently, 20 L MTT (5 mg/mL) is added to each well.Following an additional incubation at 37C for 4 h, the supernatant is removed, and

12、 100 L DMSO is addedto each well. The absorbance values (read at 540 nm) are determined using the iMark MicroplateAbsorbance Reader. The data are analyzed using Microplate Manager software (ver. 6.3; 1689520).MCE has not independently confirmed the accuracy of these methods. They are for reference o

13、nly.Animal A total of 5106 SW-839 cells are mixed with Matrigel, and injected subcutaneously into the flanks of 14 5-Administration 1 week-old male BALB/c nude mice. The mice are maintained in 1830-cm cages containing three mice each,at a temperature of 22C using a 12 h light/dark cycle. Food and wa

14、ter is available ad libitum. The mice arerandomLy divided into two groups (n=7). As previously described, the mice are administrated with2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEchelerythrine chloride at a dose of 5 mg/kg/day via intraperitoneal injection for 5 weeks, with the first injectio

15、nof chelerythrine chlorideurring 24 h after injection with the SW-839 cells. The control mice are administeredwith the same volume of PBS containing 1% DMSO. The volume and weight of the mouse tumors aremeasured once a week. All the mice are sacrificed 36 days subsequent to inoculation of the cancer

16、 cells,when the tumors are resected.MCE has not independently confirmed the accuracy of these methods. They are for reference only.戶使本產(chǎn)品發(fā)表的科研獻 Sci Rep. 2017 Aug 23;7(1):9201. Harvard Medical School LINCS LIBRARYSee more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Chan, et al. Identi

17、fication of chelerythrine as an inhibitor of BclXL function. J Biol Chem. 2003 Jun 6;278(23):20453-6.2. Li W, et al. Effect of Chelerythrine Against Endotoxic Shock in Mice and Its Modulation of Inflammatory Mediators in PeritonealMacrophages Through the Modulation of Mitogen-Activated Protein Kinas

18、e (MAPK) Pathway. Inflammation. 2012 Jul 24.3. Pencikova K, et al. Investigation of sanguinarine and chelerythrine effects on LPS-induced inflammatory gene expression in THP-1 cellline. Phytomedicine. 2012 Jul 15;19(10):890-5. Epub 2012 May 14.4. Chen XM, et al. Chelerythrine chloride induces apoptosis in renal cancer HEK-293 and SW-839 cell lines. Oncol Lett. 2016Jun;11(6):3917-39245. Herbert JM, et al. Chelerythrine is a potent and specific inh