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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 Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $30 | In Stock | |
5 mg | $67 | In Stock | |
10 mg | $98 | In Stock | |
25 mg | $207 | In Stock | |
50 mg | $369 | In Stock | |
100 mg | $549 | In Stock | |
1 mL x 10 mM (in DMSO) | $78 | In Stock |
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 (recombinant):0.5 μM (IC50), CDK8:200 nM (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. |
Molecular Weight | 264.33 |
Formula | C16H16N4 |
Cas No. | 642008-81-9 |
Smiles | CC1CCc2nc(N)c(C#N)c(-c3cccnc3)c2C1 |
Relative Density. | no data available |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||
Solubility Information | DMSO: 11 mg/mL (41.61 mM) | |||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||
DMSO
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