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BJE6-106

Cat No.:V32597 Purity: ≥98%
BJE6-106 (B106) is a potent and specific PKCδ inhibitor (antagonist) with IC50 of 0.05 μM.
BJE6-106
BJE6-106 Chemical Structure CAS No.: 1564249-38-2
Product category: New2
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
1mg
5mg
10mg
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Product Description
BJE6-106 (B106) is a potent and specific PKCδ inhibitor (antagonist) with IC50 of 0.05 μM. BJE6-106 (B106) is 1000 times more selective for targeting PKCδ than the PKC isoenzyme PKCα (IC50=50 μM). . BJE6-106 (B106) can induce caspase-dependent apoptosis (apoptosis). BJE6-106 (B106) has tumor-specific effects.
Biological Activity I Assay Protocols (From Reference)
ln Vitro
BJE6-106 (B106) (0.2 μM, 0.5 μM; 24-72 hours) reduces cell survival in melanoma cell lines carrying NRAS mutations [1]. BJE6-106 (B106) (0.2 μM, 0.5 μM; 6-24 hours) causes caspase-dependent apoptosis and enhances caspase 3/7 activity. The effect of B106 is stronger than that of Rottlerin (10-fold) in SBcl2 cells [1]. BJE6-106 (B106) (0.5 μM; 2-10 hours) triggers the MKK4-JNK-H2AX pathway by triggering MKK4, JNK and H2AX activation at separate periods in SBcl2 cells [1].
Cell Assay
Cell Viability Assay[1]
Cell Types: Melanoma cell lines with NRAS mutations: SBcl2, FM6, SKMEL2, WM1366, WM1361A, and WM852 Cell
Tested Concentrations: 0.2 μM, 0.5 μM
Incubation Duration: 24 hrs (hours), 48 hrs (hours), or 72 hrs (hours)
Experimental Results: Inhibition of cell survival in melanoma cell lines.

Apoptosis analysis[1]
Cell Types: SBcl2 Cell
Tested Concentrations: 0.2 μM, 0.5 μM
Incubation Duration: 6 hrs (hours), 12 hrs (hours) or 24 hrs (hours)
Experimental Results: Induction of caspase 3/7 activation.

Western Blot Analysis[1]
Cell Types: SBcl2 Cell
Tested Concentrations: 0.2 μM, 0.5 μM
Incubation Duration: 2 hrs (hours), 5 hrs (hours), 10 hrs (hours)
Experimental Results: Increased phosphorylation of MKK4, JNK and H2AX.
References

[1]. Protein kinase Cδ is a therapeutic target in malignant melanoma with NRAS mutation. ACS Chem Biol. 2014 Apr 18;9(4):1003-14.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C26H23NO2
Molecular Weight
381.4663
Exact Mass
381.172
CAS #
1564249-38-2
PubChem CID
85471521
Appearance
White to off-white solid powder
LogP
5.6
Hydrogen Bond Donor Count
0
Hydrogen Bond Acceptor Count
2
Rotatable Bond Count
4
Heavy Atom Count
29
Complexity
606
Defined Atom Stereocenter Count
0
SMILES
O1C2C(C([H])=O)=C([H])C(=C([H])C=2C([H])=C([H])C1(C([H])([H])[H])C([H])([H])[H])C([H])([H])C([H])([H])N1C2=C([H])C([H])=C([H])C([H])=C2C2=C([H])C([H])=C([H])C([H])=C12
InChi Key
QLDDENZBVHBRKN-UHFFFAOYSA-N
InChi Code
InChI=1S/C26H23NO2/c1-26(2)13-11-19-15-18(16-20(17-28)25(19)29-26)12-14-27-23-9-5-3-7-21(23)22-8-4-6-10-24(22)27/h3-11,13,15-17H,12,14H2,1-2H3
Chemical Name
6-(2-carbazol-9-ylethyl)-2,2-dimethylchromene-8-carbaldehyde
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO : ~50 mg/mL (~131.07 mM)
Solubility (In Vivo)
Solubility in Formulation 1: 2.5 mg/mL (6.55 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

Solubility in Formulation 2: ≥ 2.5 mg/mL (6.55 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.6214 mL 13.1072 mL 26.2144 mL
5 mM 0.5243 mL 2.6214 mL 5.2429 mL
10 mM 0.2621 mL 1.3107 mL 2.6214 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

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An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

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