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Merck

SML2208

Sigma-Aldrich

BRD6989

≥98% (HPLC)

别名:

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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About This Item

经验公式(希尔记法):
C16H16N4
分子量:
264.33
分類程式碼代碼:
12352200
NACRES:
NA.77

化驗

≥98% (HPLC)

形狀

powder

顏色

white to beige

溶解度

DMSO: 2 mg/mL, clear

儲存溫度

2-8°C

SMILES 字串

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

生化/生理作用

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.

儲存類別代碼

11 - Combustible Solids

水污染物質分類(WGK)

WGK 3

閃點(°F)

Not applicable

閃點(°C)

Not applicable


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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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