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SML2208

Sigma-Aldrich

BRD6989

≥98% (HPLC)

Synonym(s):

2-Amino-3-cyano-6-methyl-4-(3-pyridinyl)-5,6,7,8-tetrahydroquinoline, 2-Amino-5,6,7,8-tetrahydro-6-methyl-4-(3-pyridinyl)-3-quinolinecarbonitrile

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5 MG
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25 MG
€241.00

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5 MG
€74.20
25 MG
€241.00

About This Item

Empirical Formula (Hill Notation):
C16H16N4
CAS Number:
642008-81-9
Molecular Weight:
264.33
UNSPSC Code:
12352200
NACRES:
NA.77

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Assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

2-8°C

SMILES string

NC1=NC(CCC(C)C2)=C2C(C3=CN=CC=C3)=C1C#N

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)

InChI key

QSYBDNXNOJIKML-UHFFFAOYSA-N

Biochem/physiol Actions

BRD6989 is an inhibitor of cyclin-dependent kinase 8 (CDK8) that upregulates production of interleukin-10 (IL-10). BRD6989 was shown to bind cyclin C–CDK8 complex selectively with an IC50 value ∼200 nM and to inhibit the kinase activity of recombinant cyclin C–CDK8 or cyclin C–CDK19 complexes with IC50 values ∼500 nM and >30 μM, respectively. It enhanced the production interleukin-10 (IL-10) enhances IL-10 production in activated human and murine macrophages and dendritic cells with an EC50 value ∼1 μM.
Inhibitor of cyclin-dependent kinase 8 (CDK8) that upregulates production of interleukin-10 (IL-10)

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

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Certificates of Analysis (COA)

Lot/Batch Number
0000043674
0000043675
0000037246

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Liv Johannessen et al.
Nature chemical biology, 13(10), 1102-1108 (2017-08-15)
Enhancing production of the anti-inflammatory cytokine interleukin-10 (IL-10) is a promising strategy to suppress pathogenic inflammation. To identify new mechanisms regulating IL-10 production, we conducted a phenotypic screen for small molecules that enhance IL-10 secretion from activated dendritic cells. Mechanism-of-action

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