BRD6989

• 常用名: BRD6989
• 英文名: BRD 6989
• CAS号: 642008-81-9
• 分子量: 264.325
• 密度: 1.2±0.1 g/cm3
• 沸点: 496.6±45.0 °C at 760 mmHg
• 分子式: C₁₆H₁₆N₄
• 熔点: N/A
• 闪点: 254.2±28.7 °C

BRD6989用途

一种新型有效的选择性CDK8抑制剂,对重组细胞周期蛋白C/CDK8复合物的IC50为0.5 uM；对包括CDK19在内的几种参与细胞周期的CDK没有活性(IC50>30 uM)；抑制IFNγ诱导的STAT1磷酸化在BMDCs的Ser 727位点,选择性上调IL-10,EC50为1 uM。

BRD6989名称

• 中文名: 2-氨基-6-甲基-4-(吡啶-3-基)-5,6,7,8-四氢喹啉-3-甲腈
• 英文名: 2-Amino-6-methyl-4-(3-pyridinyl)-5,6,7,8-tetrahydro-3-quinolinecarbonitrile

BRD6989生物活性

• 描述: 一种新型有效的选择性CDK8抑制剂,对重组细胞周期蛋白C/CDK8复合物的IC50为0.5 uM；对包括CDK19在内的几种参与细胞周期的CDK没有活性(IC50>30 uM)；抑制IFNγ诱导的STAT1磷酸化在BMDCs的Ser 727位点,选择性上调IL-10,EC50为1 uM。
• 参考文献: References 1. Johannessen L, et al. Nat Chem Biol. 2017 Oct;13(10):1102-1108. View Related Products by Target Cyclin-dependent Kinase (CDK)

BRD6989物理化学性质

• 密度: 1.2±0.1 g/cm3
• 沸点: 496.6±45.0 °C at 760 mmHg
• 分子式: C₁₆H₁₆N₄
• 分子量: 264.325
• 闪点: 254.2±28.7 °C
• 精确质量: 264.137512
• LogP: 3.69
• InChIKey: QSYBDNXNOJIKML-UHFFFAOYSA-N
• SMILES: CC1CCc2nc(N)c(C#N)c(-c3cccnc3)c2C1
• 蒸汽压: 0.0±1.3 mmHg at 25°C
• 折射率: 1.640
• 储存条件: 2-8°C， 避光， 惰性气体

BRD6989靶点实验

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实验名称：Primary cell-based high-throughput screening assay for identification of compounds th... 来源：Johns Hopkins Ion Channel Center 靶标：regulator of G-protein signaling 4 isoform 2 [Homo sapiens] External Id：JHICC_RGS_Act_HTS

实验名称：Luminescence-based cell-based primary high throughput screening assay to identify ago... 来源：The Scripps Research Institute Molecular Screening Center 靶标：mu-type opioid receptor isoform MOR-1 [Homo sapiens] External Id：OPRM1-OPRD1_AG_LUMI_1536_1X%ACT PRUN

实验名称：QFRET-based biochemical primary high throughput screening assay to identify exosite i... 来源：The Scripps Research Institute Molecular Screening Center 靶标：disintegrin and metalloproteinase domain-containing protein 17 preproprotein [Homo sapiens] External Id：ADAM17_INH_QFRET_1536_1X%INH PRUN

实验名称：Fluorescence-based cell-based primary high throughput screening assay to identify ago... 来源：The Scripps Research Institute Molecular Screening Center 靶标：muscarinic acetylcholine receptor M1 [Homo sapiens] External Id：CHRM1_AG_FLUO8_1536_1X%ACT PRUN

实验名称：uHTS identification of small molecule activators of the adaptive arm of the Unfolded ... 来源：Burnham Center for Chemical Genomics 靶标：N/A External Id：BCCG-A405-UPR-XBP1-PrimaryAgonist-Assay

实验名称：High throughput fluorescence intensity-based biochemical assay to screen for small mo... 来源：University of Pittsburgh Molecular Library Screening Center 靶标：furin (paired basic amino acid cleaving enzyme), isoform CRA_a [Homo sapiens] External Id：MH080376 Biochemical HTS for Inhibitors of the Proprotein Convertase Furin.

实验名称：Fluorescence polarization to screen for inhibitor that competite the binding of FadD2... 来源：Broad Institute 靶标：FATTY-ACID-CoA LIGASE FADD28 (FATTY-ACID-CoA SYNTHETASE) External Id：2147-01_Inhibitor_SinglePoint_HTS_Activity

实验名称：Bursicon-induced LGR2 mediated cAMP production in LGR-2/CRE6x-Luciferase co-transfect... 来源：Broad Institute 靶标：N/A External Id：Bursicon-induced LGR2 mediated cAMP production in LGR-2/CRE6x-Luciferase co-transfected HEK293 cells Inhibition - 7011-01_Antagonist_SinglePoint_HTS_Activity

实验名称：Counterscreen for inhibitors of the Steroid Receptor Coactivator 1 (SRC1; NCOA1): Lum... 来源：The Scripps Research Institute Molecular Screening Center 靶标：transactivating tegument protein VP16 [Human herpesvirus 1] External Id：VP16_INH_LUMI_1536_3X%INH CSRUN for SRC1

实验名称：HSF-1 induced GFP reporter and Doxycycline induced RFP reporter Measured in Cell-Base... 来源：Broad Institute 靶标：Hsf1 protein External Id：2038-03_Inhibitor_Dose_CherryPick_Activity_Set4

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BRD6989英文别名

• 2-Amino-6-methyl-4-(3-pyridinyl)-5,6,7,8-tetrahydro-3-quinolinecarbonitrile
• MFCD04013193