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Chelerythrine Chloride (NSC 646662) PKC inhibitor

Name: Chelerythrine Chloride (NSC 646662)
Brand: Selleck Chemicals
SKU: S1292
Availability: InStock
Rating: 5 (4 reviews)

Cat.No.S1292

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

Chemical Structure

Molecular Weight: 384.83

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.53%

99.53

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Chemical Information, Storage & Stability

Molecular Weight	384.83	Formula	C₂₁H₁₈NO₄.HCl	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	3895-92-9	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	Broussonpapyrine chloride			Smiles	C[N+]1=C2C(=C3C=CC(=C(C3=C1)OC)OC)C=CC4=CC5=C(C=C42)OCO5.[Cl-]

Solubility

In vitro
Batch:

DMSO : 3 mg/mL (7.79 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.15mg/ml (0.39mM)	Taking the 1 mL working solution as an example, add 50 μL of 3 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Features	Chelerythrine is at least 100-fold more selective for PKCs than for other kinases.
Targets/IC₅₀/Ki	PKC ^[5] (Cell-free assay) 0.66 μM
In vitro	Chelerythrine Chloride (NSC 646662) 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. It shows potent cytotoxic effects against L-1210 cells with IC50 of 0.53 μM. This compound does not alter any activity of PKA, TPK and Ca/CM-PK, and its inhibitory effect on PKC activity does not vary among the various substrates including GS, MLC, MBP and Fibrinogen. ^[1] It 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] At 5 μM, it suppresses VEGF-induced expression of ICAM-1, VCAM-1, and E-selectin in HUVECs. It also suppresses VEGF-induced NF-κB activity in HUVECs at the same concentration and all suppresses basal and VEGF-induced leukocyte adhesiveness in HUVECs. ^[3] At concentrations of 6 mM-30 mM, it 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. At 10 μM, it causes cytochrome c release from mitochondria, suggesting that ROS mediates chelerythrine-induced cytochrome c release in cardiac myocytes. ^[4] It displaces the fluorescently labeled BH3 domain peptide from a recombinant GST-BcLXL fusion protein with IC50 of 1.5 μM. At 2.5 μM and 5 μM for 16 hours, it induces a substantial decrease in mitochondrial potential as indicated by an increase in JC-1 green fluorescence in human neuroblastoma SH-SY5Y cells. At 5 μM, it also induces the appearance of sub-G1 DNA that is indicative of apoptosis in SH-SY5Y cells. At 10 μM, it induces mitochondrial potential change, CytC release from the mitochondria in SH-SY5Y cells. ^[5]
Kinase Assay	assay for protein kinase C
Kinase Assay	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 Chloride (NSC 646662) 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.
In vivo	Chelerythrine Chloride (NSC 646662) (5 mg/kg i.p.) results in tumor growth delay in mice bearing SQ-20B xenografts. ^[2] This compound (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]
References	[1] https://pubmed.ncbi.nlm.nih.gov/2244923/ [2] https://pubmed.ncbi.nlm.nih.gov/10690561/ [3] https://pubmed.ncbi.nlm.nih.gov/11108718/ [4] https://pubmed.ncbi.nlm.nih.gov/11603925/ [5] https://pubmed.ncbi.nlm.nih.gov/12702731/

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