Description
BRD6989, an analog of the natural product cortistatin A (dCA), inhibits CDK8 and upregulates IL-10. BRD6989 selectively binds a complex of CDK8 with an IC50 of ~200 nM. BRD6989 inhibits the kinase activity of recombinant CDK8 or CDK19 complexes.
Product information
CAS Number: 642008-81-9
Molecular Weight: 264.33
Formula: C16H16N4
Chemical Name: 2-amino-6-methyl-4-(pyridin-3-yl)-5,6,7,8-tetrahydroquinoline-3-carbonitrile
Smiles: CC1CC2=C(C(C#N)=C(N)N=C2CC1)C1=CN=CC=C1
InChiKey: QSYBDNXNOJIKML-UHFFFAOYSA-N
InChi: InChI=1S/C16H16N4/c1-10-4-5-14-12(7-10)15(11-3-2-6-19-9-11)13(8-17)16(18)20-14/h2-3,6,9-10H,4-5,7H2,1H3,(H2,18,20)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 25 mg/mL (94.58 mM; Need ultrasonic).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
Pretreatment of BMDCs with BRD6989 (0-100 μM; for 48 hours) increases IL-10 production with an EC50 of ~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; ~2 hours) suppresses induction of STAT1–STAT2 activity and NF-κB activation to a varying degree after stimulation of BMDMs. BRD6989 (5 µM; 24 hours) enhances IL-10 production in activated human and murine macrophages and dendritic cells.
Products are for research use only. Not for human use.
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