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Chelerythrine

MCE China：Chelerythrine

Brand：MedChemExpress (MCE)

Cat. No.HY-N2359

CAS：34316-15-9

Storage：Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping：Room temperature in continental US; may vary elsewhere.

Description：Chelerythrine is a natural alkaloid, acts as a potent and selective Ca2+/phospholopid-dependent PKC antagonist, with an IC50 of 0.7 μM. Chelerythrine has antitumor, antidiabetic and anti-inflammatory activity. Chelerythrine inhibits the BclXL-Bak BH3 peptide binding with IC50 of 1.5 μM and displaces Bax from BclXL. Chelerythrine triggers apoptosis and autophagy.

In Vitro：Chelerythrine (48 h) inhibits the growth of L-1210 cells (IC50: 0.53 uM )[1]. Chelerythrine (0-20 μM, 24 h) inhibits cell viability, induces apoptosis and autophagy in A549 and NCI-H1299 cells[4]. Chelerythrine (0-5 μM, 24 or 48 h) induces apoptosis in BclXL-overexpressing SH-SY5Y cells[3]. Chelerythrine (2.5-10 μM, 16 h) induces mitochondrial depolarization (decrease in mitochondrial potential) in SH-SY5Y cells, and stimulates release of CytC from isolated mitochondria[4]. Chelerythrine (0-100 ng/mL, 24 h) reduces the LPS induced production of NO and TNF-α in primary macrophages[5]. Chelerythrine (MIC: 0.156 mg/mL) shows antibacterial activities against Gram-positive bacteria, Staphylococcus aureus (SA), MRSA, and extended spectrum β-lactamase S. aureus (ESBLs-SA)[6].

In Vivo：Chelerythrine (5 mg/kg, i.p., daily) attenuates partial unilateral ureteral obstruction (UUO) induced kidney injury, and restores renal function in neonatal rats[2]. Chelerythrine (1-10 mg/kg, i.p., at 24 and 1 h before injection of 100 μg/kg LPS) shows anti-inflammatory effects (increased survival rate, decreased serum nitrite and TNF-α level) in LPS induced mice endotoxic shock model[5].

IC50 & Target：PKC 0.7 μM (IC50)

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References：

[1]. Herbert JM, et al. Chelerythrine is a potent and specific inhibitor of protein kinase C. Biochem Biophys Res Commun. 1990 Nov 15;172(3):993-9.  [Content Brief]

[2]. Shi B, et al. Protein kinase C inhibitor chelerythrine attenuates partial unilateral ureteral obstruction induced kidney injury in neonatal rats. Life Sci. 2019 Jan 1;216:85-91.  [Content Brief]

[3]. Chan SL, et al.Identification of chelerythrine as an inhibitor of BclXL function.J Biol Chem. 2003 Jun 6;278(23):20453-6.  [Content Brief]

[4]. Tang ZH, et al.Induction of reactive oxygen species-stimulated distinctive autophagy by chelerythrine in non-small cell lung cancer cells.Redox Biol. 2017 Aug;12:367-376.  [Content Brief]

[5]. Li W, et al. Effect of chelerythrine against endotoxic shock in mice and its modulation of inflammatory mediators in peritoneal macrophages through the modulation of mitogen-activated protein kinase (MAPK) pathway. Inflammation. 2012 Dec;35(6):1814-24.  [Content Brief]

[6]. He N, et al. Antibacterial mechanism of chelerythrine isolated from root of Toddalia asiatica (Linn) Lam. BMC Complement Altern Med. 2018 Sep 26;18(1):261.  [Content Brief]