BRD6989 是天然产物皮质抑素 A 的类似物，可抑制CDK8并上调IL-10，抑制重组 CDK8 或 CDK19 复合物的激酶活性。它选择性结合 CDK8 复合物，IC50约为 200 nM。

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.

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.

642008-81-9

C16H16N4

264.33

DMSO:10 mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years