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Submit ReviewBRD 6989
Description: Cdk8 inhibitor; enhances IL-10 production
Chemical Name: 2-Amino-5,6,7,8-tetrahydro-6-methyl-4-(3-pyridinyl)-3-quinolinecarbonitrile
Purity: ≥98% (HPLC)
Biological Activity
Binds and inhibits Cdk8 in complex with cyclin C (IC50 ~ 200 nM). Enhances IL-10 production in activated human and murine macrophages and dendritic cells (EC50 is approximately 1 μM for IL-10 production in bone marrow-derived dendritic cells). Also inhibits CDK19 in complex with cyclin C.
Technical Data
| M. Wt | 264.33 |
| Formula | C16H16N4 |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 642008-81-9 |
| PubChem ID | 3835861 |
| InChI Key | QSYBDNXNOJIKML-UHFFFAOYSA-N |
| Smiles | CC1CCC2=NC(N)=C(C(C3=CN=CC=C3)=C2C1)C#N |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 5.29 | 20 |
Preparing Stock Solutions
The following data is based on the product molecular weight 264.33. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.2 mM | 18.92 mL | 94.58 mL | 189.16 mL |
| 1 mM | 3.78 mL | 18.92 mL | 37.83 mL |
| 2 mM | 1.89 mL | 9.46 mL | 18.92 mL |
| 10 mM | 0.38 mL | 1.89 mL | 3.78 mL |
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References
References are publications that support the biological activity of the product.
Johannessen et al (2017) Small-molecule studies identify CDK8 as a regulator of IL-10 in myeloid cells. Nat.Chem.Biol. 13 1102 PMID: 28805801
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Keywords: BRD 6989, BRD 6989 supplier, BRD6989, IL-10, production, enhancers, CDK8, inhibitors, enhances, inhibits, Cytokines, Cyclin-dependent, Kinase, 6438, Tocris Bioscience
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