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BRD6989

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Catalog No. T14778Cas No. 642008-81-9

BRD6989 is an analog of the natural product cortistatin A (dCA). Which inhibits CDK8 and upregulates IL-10. BRD6989 inhibits the kinase activity of recombinant CDK8 or CDK19 complexes. BRD6989 selectively binds a complex of CDK8 with an IC50 of ~200 nM.

BRD6989

BRD6989

😃Good
Purity: 99.43%
Catalog No. T14778Cas No. 642008-81-9
BRD6989 is an analog of the natural product cortistatin A (dCA). Which inhibits CDK8 and upregulates IL-10. BRD6989 inhibits the kinase activity of recombinant CDK8 or CDK19 complexes. BRD6989 selectively binds a complex of CDK8 with an IC50 of ~200 nM.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$30In StockIn Stock
5 mg$64In StockIn Stock
10 mg$98In StockIn Stock
25 mg$197In StockIn Stock
50 mg$297In StockIn Stock
100 mg$442In StockIn Stock
200 mg$638-In Stock
1 mL x 10 mM (in DMSO)$71In 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:99.43%
Appearance:Solid
Color:White
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Product Introduction

Bioactivity
Description
BRD6989 is an analog of the natural product cortistatin A (dCA). Which inhibits CDK8 and upregulates IL-10. BRD6989 inhibits the kinase activity of recombinant CDK8 or CDK19 complexes. BRD6989 selectively binds a complex of CDK8 with an IC50 of ~200 nM.
Targets&IC50
CDK8:200 nM (IC50), CDK8 (recombinant):0.5 μM (IC50), CDK19 (recombinant):>30 μM (IC50)
In vitro
Pretreatment of BMDCs with BRD6989 (0-100 μM; for 48 hours) increases IL-10 production (EC50: ~1 μM). BRD6989 (0.6, 1.7, 5, 15 μM) suppresses phosphorylation of the STAT1 transactivation domain at Ser727 in IFNγ-stimulated BMDCs. BRD6989 (5 μM; 24 hours) enhances IL-10 production in activated human and murine macrophages and dendritic cells. BRD6989 (5 μM; ~2 hours) suppresses induction of STAT1–STAT2 activity and NF-κB activation to a varying degree after stimulation of BMDMs.
Chemical Properties
Molecular Weight264.33
FormulaC16H16N4
Cas No.642008-81-9
SmilesCC1CCc2nc(N)c(C#N)c(-c3cccnc3)c2C1
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: 11 mg/mL (41.61 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+90% Corn Oil: 1 mg/mL (3.78 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 mM3.7831 mL18.9157 mL37.8315 mL189.1575 mL
5 mM0.7566 mL3.7831 mL7.5663 mL37.8315 mL
10 mM0.3783 mL1.8916 mL3.7831 mL18.9157 mL
20 mM0.1892 mL0.9458 mL1.8916 mL9.4579 mL

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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:
mg/kg
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μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

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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

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