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BRD6989

Catalog No. T14778   CAS 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.

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BRD6989 Chemical Structure
BRD6989, CAS 642008-81-9
Pack Size Availability Price/USD Quantity
1 mg In stock $ 30.00
5 mg In stock $ 67.00
10 mg In stock $ 98.00
25 mg In stock $ 207.00
50 mg In stock $ 369.00
100 mg In stock $ 549.00
1 mL * 10 mM (in DMSO) In stock $ 78.00
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Purity: 98.82%
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Biological Description
Chemical Properties
Storage & Solubility Information
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), recombinant CDK8:0.5 μM (IC50), recombinant CDK19:>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

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 11 mg/mL (41.61 mM)

TargetMolReferences and Literature

1. Johannessen L, et al. Small-molecule studies identify CDK8 as a regulator of IL-10 in myeloid cells. Nat Chem Biol. 2017 Oct;13(10):1102-1108

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Compound Library Bioactive Compounds Library Max Anti-Pancreatic Cancer Compound Library Immunology/Inflammation Compound Library Inhibitor Library Bioactive Compound Library Cytokine Inhibitor Library Anti-Cardiovascular Disease Compound Library NO PAINS Compound Library Cell Cycle Compound Library

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Keywords

BRD6989 642008-81-9 Cell Cycle/Checkpoint Immunology/Inflammation IL Receptor CDK Interleukin CDK8 Inhibitor inhibit CDK19 IL-10 inflammatory Cyclin dependent kinase BMDCs Interleukin Related BRD 6989 cortistatin-A BRD-6989 inhibitor

 

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