Chelerythrine chloride 是一种有效，可渗透细胞的蛋白酶 C (protein kinase C) 抑制剂，能够抑制 PKC 活性，IC50 值为 660 nM。Chelerythrine chloride 抑制 Bcl-XL-Bak BH3 肽结合，IC50 为 1.5 μM，并从 Bcl-XL 取代了 Bax。Chelerythrine chloride 诱导细胞凋亡 (apoptosis) 和自噬 (autophagy)。
| CAS No. | 3895-92-9 |
| 生物活性 | Chelerythrine chloride is a potent, cell-permeable inhibitor of protein kinase C, with an IC50 of 660 nM. Chelerythrine chloride inhibits the Bcl-XL-Bak BH3 peptide binding with IC50 of 1.5 μM and displaces Bax from Bcl-XL. Chelerythrine chloride induces apoptosis and autophagy. |
| 分子式 | C21H18ClNO4 |
| 分子量 | 383.82 |
| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存条件 | Powder -20°C 3 years |
| 溶解性数据 | DMSO : 4.35 mg/mL (11.33 mM; Need ultrasonic) |
| 体内研究 | Chelerythrine displays 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. Chelerythrine chloride (5 mg/kg/day, i.p.) induces apoptosis of RCC cells without significant toxicity to mice. Chelerythrine Chloride treatment leads to a dose-dependent accumulation of p53. |
| 体外研究 | Chelerythrine inhibits the BclXL-Bak BH3 peptide binding with IC50 of 1.5 μM and displaces Bax, a BH3-containing protein, from BclXL. Mammalian cells treated with Chelerythrine undergoes apoptosis with characteristic features that suggest involvement of the mitochondrial pathway. 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. Moreover, 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. 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. Chelerythrine chloride significantly enhances the phosphorylation of ERK1/2 in a dose-dependent manner. In addition, chelerythrine chloride inhibits the phosphorylation of p38. |
| 文献 | •Front Pharmacol. 13 May 2021. •Cell Commun Signal. 2021 Oct 11;19(1):103. •FASEB J. 2019 Dec;33(12):13644-13659. •Front Physiol. 2021 Oct 28;12:770430. •Sci Rep. 2017 Aug 23;7(1):9201. •Research Square Preprint. 2020 Oct. •Harvard Medical School LINCS LIBRARY |
| 纯度及产品资料 | 98% |
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