Home TGF-beta/Smad PKC inhibitor Chelerythrine Chloride (NSC 646662) For research use only.

Chelerythrine Chloride (NSC 646662)

Synonyms: Broussonpapyrine chloride

Chelerythrine Chloride (NSC 646662, Broussonpapyrine) is a potent, selective antagonist of PKC with IC50 of 0.66 μM.

Chelerythrine Chloride (NSC 646662) Chemical Structure

Chelerythrine Chloride (NSC 646662) Chemical Structure

CAS No. 3895-92-9

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Chelerythrine Chloride (NSC 646662) Related Products

Signaling Pathway

PKC Signaling Pathways

PKC Signaling Pathway

Biological Activity

Description Chelerythrine Chloride (NSC 646662, Broussonpapyrine) is a potent, selective antagonist of PKC with IC50 of 0.66 μM.
Features Chelerythrine is at least 100-fold more selective for PKCs than for other kinases.
Targets
PKC [5]
(Cell-free assay)
0.66 μM
In vitro
In vitro

Chelerythrine interacts with the catalytic domain of PKC, is a competitive inhibitor with respect to the phosphate acceptor (histone IIIS) with Ki value of 0.7 μM and a non-competitive inhibitor with respect to ATP. Chelerythrine shows potent cytotoxic effects against L-1210 cells with IC50 of 0.53 μM. Chelerythrine does not alter any activity of PKA, TPK and Ca/CM-PK, and the Chelerythrine inhibitory effect on PKC activity does not vary among the various substrates including GS, MLC, MBP and Fibrinogen. [1] Chelerythrine inhibits PKC activity in crude cell extracts from SQ-20B cells in a dose dependent manner. Chelerythrine decreases cell viability as determined by the MTT assay in a dose-dependent manner in SCC35, JSQ3, SQ20B and SCC61 cells. [2] Chelerythrine chloride (5 μM) suppresses VEGF-induced expression of ICAM-1, VCAM-1, and E-selectin in HUVECs. Chelerythrine chloride (5 μM) suppresses VEGF-induced NF-κB activity in HUVECs. Chelerythrine chloride (5 μM) all suppresses basal and VEGF-induced leukocyte adhesiveness in HUVECs. [3] Chelerythrine (6 mM-30 mM) rapidly induces pyknosis, shrinkage and subsequent cell death in cardiac myocytes. Chelerythrine(30 μM)-induced myocyte death is accompanied by nuclear fragmentation and activation of caspase-3 and -9 in primary culture of neonatal rat ventricular myocytes. Chelerythrine (10 μM) causes cytochrome c release from mitochondria, suggesting that ROS mediates chelerythrine-induced cytochrome c release in cardiac myocytes. [4] Chelerythrine displaces the fluorescently labeled BH3 domain peptide from a recombinant GST-BcLXL fusion protein with IC50 of 1.5 μM. Chelerythrine at 2.5 μM and 5 μM for 16 hours induces a substantial decrease in mitochondrial potential as indicated by an increase in JC-1 green fluorescence in human neuroblastoma SH-SY5Y cells. Chelerythrine (5 μM) also induces the appearance of sub-G1 DNA that is indicative of apoptosis in SH-SY5Y cells. Chelerythrine (10 μM) induces mitochondrial potential change, CytC release from the mitochondria in SH-SY5Y cells. [5]
Kinase Assay assay for protein kinase C
The purified protein kinase C is prepared from rat brain. Briefly, the incubation mixture (200 μL) contains 20 mM Tris/HCl buffer (pH 7.5), 10 mM MgCl2, 200 μg/mL histones, micelles makes with 700 μM phosphatidyl serine and 180 μM 1,2-dioleine in 0.3% triton X100, 0.2 mM CaCl2, 100 μM ATP, [γ-32P ]-ATP (105 dpm), Chelerythrine to be tested (solubilized in dimethylsulphoxyde) and the enzyme (0.5 μg protein). After incubation at 30℃ for 3 minutes, the reaction is terminated by the addition of 3 mL of 20% trichloroacetic acid. Acid-precipitable materials are collected on Whatman GFE filters and extensively washed with ice-cold 20% trichloroacetic acid. The radioactivity on the filters is measured using a liquid scintillation counter. Protein kinase C activity is corrected for non-specific activity by assaying in the absence of micelles and CaCl2.
Cell Research Cell lines L-1210 cells
Concentrations ~10 μM
Incubation Time 2 days
Method

The lymphocytic mouse leukemia L1210 cells are plated sparsely at 1×104 cells per well in 24-well cluster plates in RPMI 1640 medium containing 10% foetal calf serum, 4 mM glutamine, 100 U/mL penicillin, 100 pg/mL streptomycin sulphate and Chelerythrine to be tested (solubilized in dimethylsulphoxyde ). After a 2 day incubation period at 37 ℃ in a humidified atmosphere (5% CO2 in air), growth is monitored by counting cell numbers in a coulter-counter. IC50 values are calculated on the basis of the linear regression lines established for Chelerythrine tested.
In Vivo
In vivo

Chelerythrine (5 mg/kg i.p.) results in tumor growth delay in mice bearing SQ-20B xenografts. [2] Chelerythrine (5 mg/kg) treatment significantly increases TUNEL-positive nuclei in the myocardium as well as cleaved forms of caspase-3 and -9 in adult rat. [4]
Animal Research Animal Models mice bearing SQ-20B xenografts
Dosages 5 mg/kg
Administration Intraperitoneal injection

Chemical Information & Solubility

Molecular Weight 384.83 Formula

C21H18NO4.HCl
CAS No. 3895-92-9 SDF Download Chelerythrine Chloride (NSC 646662) SDF
Smiles C[N+]1=C2C(=C3C=CC(=C(C3=C1)OC)OC)C=CC4=CC5=C(C=C42)OCO5.[Cl-]
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 3 mg/mL ( (7.79 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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