Chelerythrine chloride

SKU: orb1304218

Description

Chelerythrine Chloride is a potent, cell-permeable protein kinase C (PKC) inhibitor that acts competitively with the substrate and non-competitively with ATP. It is widely used in vitro to study PKC-mediated signaling pathways in apoptosis, cancer research, and inflammation, and has been applied in various animal models for in vivo validation.

Research Area

Cell Biology, Epigenetics & Chromatin, Signal Transduction

Images & Validation

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Key Properties

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CAS Number	3895-92-9
MW	383.83
Purity	98.78%
Formula	C₂₁H₁₈ClNO₄
SMILES	[Cl-].COc1ccc2c(c[n+](C)c3c4cc5OCOc5cc4ccc23)c1OC
Target	Apoptosis,Autophagy,Bcl-2 Family,PKC
Solubility	DMSO:3.88 mg/mL (10.11 mM)

Bioactivity

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Target IC50	BTK:0.1 mM\|PKA:0.17 mM\|PKC:660 nM.
In Vivo	Chelerythrine exhibits substantial anti-inflammatory properties in vivo, notably in an experimentally induced endotoxic shock model in mice, by suppressing levels of LPS-induced tumor necrosis factor-alpha (TNF-α) and nitric oxide (NO) production in serum. Additionally, chelerythrine chloride (5 mg/kg/day, i.p.) effectively induces apoptosis in RCC cells while maintaining a minimal toxicity profile in mice. Moreover, treatment with Chelerythrine Chloride results in a dose-dependent accumulation of p53. Read more...
In Vitro	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. 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. 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. Read more...
Cell Research	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). Read more...

Storage & Handling

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Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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Bcl-2 Family, Autophagy, Apoptosis, Chelerythrine, Chelerythrine chloride, Chelerythrine Chloride, Inhibitor, inhibit, PKC, Protein kinase C

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Compound Identifiers

PubChem CID

72311 ↗

Key Properties

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No computed properties available.

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