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Bisindolylmaleimide VIII acetate

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Catalog No. T10549Cas No. 138516-31-1
Alias Ro 31-7549 acetate, Bis VIII acetate

Bisindolylmaleimide VIII acetate (Ro 31-7549 acetate) is a potent and selective PKC inhibitor (IC50: 158 nM for rat brain PKC) with IC50 values of 53, 195, 163, 213, and 175 nM for PKC-α, PKC-βI, PKC-βII, PKC-γ, and PKC-ε, respectively.

Bisindolylmaleimide VIII acetate

Bisindolylmaleimide VIII acetate

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Purity: 99.27%
Catalog No. T10549Alias Ro 31-7549 acetate, Bis VIII acetateCas No. 138516-31-1
Bisindolylmaleimide VIII acetate (Ro 31-7549 acetate) is a potent and selective PKC inhibitor (IC50: 158 nM for rat brain PKC) with IC50 values of 53, 195, 163, 213, and 175 nM for PKC-α, PKC-βI, PKC-βII, PKC-γ, and PKC-ε, respectively.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$39In StockIn Stock
5 mg$94In StockIn Stock
10 mg$149In StockIn Stock
25 mg$313In StockIn Stock
50 mg$455In StockIn Stock
100 mg$636In StockIn Stock
1 mL x 10 mM (in DMSO)$136In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:99.27%
Appearance:Solid
Color:Red
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Product Introduction

Bioactivity
Description
Bisindolylmaleimide VIII acetate (Ro 31-7549 acetate) is a potent and selective PKC inhibitor (IC50: 158 nM for rat brain PKC) with IC50 values of 53, 195, 163, 213, and 175 nM for PKC-α, PKC-βI, PKC-βII, PKC-γ, and PKC-ε, respectively.
Targets&IC50
PKC:158 nM(Rat Brain), PKCβ1:195 nM, PKCε:175 nM, PKCβ2:163 nM, PKCγ:213 nM, PKCα:53 nM
In vitro
Bisindolylmaleimide VIII acetate facilitates Fas-mediated apoptosis and inhibits T cell-mediated autoimmune diseases. Bisindolylmaleimide VIII acetate (5 μM; 8, 12 hours) dramatically increases TRA-8-induced cell death in time-dependent and TRA-8 dose-dependent manners. Bisindolylmaleimide VIII acetate (5 μM; 6 hours) significantly decreases procaspase-8 at 4 h and completely disappears at 6 h after the combined treatment with TRA-8 [2].
In vivo
Bisindolylmaleimide VIII acetate (100 μg; i.p.; every other day for three doses) results in nearly complete tumor regression combined toTRA-8. The alone treatment with Bisindolylmaleimide VIII acetate does not induce significant tumor regression [2].
SynonymsRo 31-7549 acetate, Bis VIII acetate
Chemical Properties
Molecular Weight458.51
FormulaC26H26N4O4
Cas No.138516-31-1
SmilesCC(O)=O.Cn1cc(C2=C(C(=O)NC2=O)c2cn(CCCN)c3ccccc23)c2ccccc12
Relative Density.no data available
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 150 mg/mL (327.15 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.36 mM), Sonication is recommended.
Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.1810 mL10.9049 mL21.8098 mL109.0489 mL
5 mM0.4362 mL2.1810 mL4.3620 mL21.8098 mL
10 mM0.2181 mL1.0905 mL2.1810 mL10.9049 mL
20 mM0.1090 mL0.5452 mL1.0905 mL5.4524 mL
50 mM0.0436 mL0.2181 mL0.4362 mL2.1810 mL
100 mM0.0218 mL0.1090 mL0.2181 mL1.0905 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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g
μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

Dose Conversion

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

Keywords

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