1-(2-吡啶基)乙基]-2H-咪唑并[4,5-C]喹啉-2-酮
I-BET151
CAS: 1300031-49-5
Molecular Formula: C23H21N5O3
1-(2-吡啶基)乙基]-2H-咪唑并[4,5-C]喹啉-2-酮 - Names and Identifiers
1-(2-吡啶基)乙基]-2H-咪唑并[4,5-C]喹啉-2-酮 - Physico-chemical Properties
| Molecular Formula | C23H21N5O3 |
| Molar Mass | 415.44 |
| Density | 1.314 |
| Solubility | DMSO: soluble20mg/mL, clear |
| Appearance | powder |
| Color | white to beige |
| pKa | 11.14±0.20(Predicted) |
| Storage Condition | 2-8°C |
| In vitro study | I-BET151 efficient, selective action on a variety of different protein types, such as COX-2, P450, Aurora B, GSK3β, PI3K-γ, GPCR, ion channels, transporters. Similar to I-BET762 (GSK525762A), I-BET151 had a high binding affinity for BRD2, BRD3 and BRD4 with a Kd of 0.02-0.1 μm, acting on human peripheral blood mononuclear cells (PBMC) and whole blood (WB). As well as rat WB, significantly inhibited lipopolysaccharide-stimulated IL-6 cytokine production with IC50 of 0.16 μm, 1.26 μm, and 1.26 μm, respectively. I-BET151(0.5 or 5 μm) acted on the HL60 nuclear extract, inhibiting the binding of BETs(BRD2, BRD3, BRD4, and BRD9) to acetylated histone peptides but not the 23 other bromodomain proteins. I-BET151 efficiently acts on cell lines containing different MLL fusions, such as MV4;11, RS4;11, MOLM13, and NOMO1 cells, with an IC50 of 15-192 nM. Consistently, I-BET151 completely abolished the colony forming potential of MLL fusion-driven leukemia (MOLM13) but not tyrosine kinase activation (K562)-driven leukemia. I-BET151 was also effective in liquid culture and clonogenic experiments with MLL-ENL or MLL-AF9 transformed primary mouse progenitor cells. I-BET151 acts on MLL fusion cell lines driven by different MLL fusions (containing MLL-AF9 and MLL-AF4 of MOLM13 and MV4;11, respectively) rather than K562 cells, significantly induced apoptosis and G0/G1 arrest, likely due to BCL-2 inhibition by the recruitment of BRD3/4,PAFc and SEC components to the transcription start site (TSS), c-MYC and CDK6 transcription. |
| In vivo study | I-BET151 Daily 30 mg/kg dose treatment of mice, significantly inhibited the growth of murine MLL-AF9 and human MLL-AF4 leukemia tumor, significantly prolonged life. |
1-(2-吡啶基)乙基]-2H-咪唑并[4,5-C]喹啉-2-酮 - Risk and Safety
| Hazard Symbols | T - Toxic |
| Risk Codes | 25 - Toxic if swallowed |
| Safety Description | 45 - In case of accident or if you feel unwell, seek medical advice immediately (show the label whenever possible.) |
| UN IDs | UN 2811 6.1 / PGIII |
| WGK Germany | 3 |
1-(2-吡啶基)乙基]-2H-咪唑并[4,5-C]喹啉-2-酮 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.407 ml | 12.035 ml | 24.071 ml |
| 5 mM | 0.481 ml | 2.407 ml | 4.814 ml |
| 10 mM | 0.241 ml | 1.204 ml | 2.407 ml |
| 5 mM | 0.048 ml | 0.241 ml | 0.481 ml |
Last Update：2024-01-02 23:10:35
1-(2-吡啶基)乙基]-2H-咪唑并[4,5-C]喹啉-2-酮 - Reference Information
| biological activity | I-BET151 (GSK1210151A) is a new and selective BET inhibitor that acts on BRD2, BRD3 and BRD4 with IC50 of 0.5 μM, 0.25 μM and 0.79 μM respectively. |
| in vitro research | I-BET151 is effective and selectively acts on a variety of different protein types, such as COX-2, P450, Aurora B, GSK3β, PI3K-γ, GPCR, ion channels, transporters. Similar to I-BET762 (GSK525762A), I-BET151 has high binding affinity for BRD2, BRD3 and BRD4, Kd is 0.02-0.1 μM, acting on human peripheral blood mononuclear cells (PBMC) and whole blood (WB) and rat WB, significantly inhibiting lipopolysaccharide-stimulated IL-6 cytokine production, IC50 is 0.16 μM, 1.26 μM, and 1.26 μM, respectively. I-BET151(0.5 or 5 μM) acts on HL60 nuclear extract to inhibit BETs(BRD2, BRD3, BRD4, and BRD9) instead of 23 other bromine region proteins binding to acetylated hibmin peptides. I-BET151 effectively acts on cell lines containing different MLL fuses, such as MV4;11, RS4;11, MOLM13, and NOMO1 cells, IC50 is 15-192 nM. Consistent, the colony-forming potential of MLL fusion-driven leukemias (MOLM13) but not tyrosine kinase-activated (K562)-driven leukemias I-BET151 be completely eliminated. I-BET151 also effectively acts on the cloning and formation experiments of primary mouse progenitor cells in liquid culture and transformation MLL-ENL or MLL-AF9. I-BET151 acts on different MLL fuses (MOLM13 and MV4 containing MLL-AF9 and MLL-AF4 respectively; 11) MLL fusion cell lines driven by K562 cells significantly induced apoptosis and G0/G1 phase arrest, probably due to inhibition of BCL-2,C-MYC and CDK6 transcription by recruiting transcription initiation sites (TSS) through inhibition of BRD3/4,PAFc and SEC components. |
| in vivo study | I-BET151 treated mice at a dose of 30 mg/kg per day significantly inhibited the growth of murine MLL-AF9 and human MLL-AF4 leukemia tumors and significantly prolonged life span. |
| features | optimize the I-BET151 to effectively and selectively target BET, while enhancing in vivo pharmacokinetics and terminal half-life to prolong in vivo research. |
| target | pIC50: 6.1 (BRD4), 6.3 (BRD2), 6.6 (BRD3) |
Last Update：2024-04-09 20:49:11
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View History
1-(2-吡啶基)乙基]-2H-咪唑并[4,5-C]喹啉-2-酮
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Pyriproxyfen
1-(氨基甲基)-3-丙基环丁烷-1-羧酸乙酯
4,4'-DIPYRIDYL DISULFIDE
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(S)-2-(4-硝基苯基)吗啉-4-羧酸叔丁酯
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4-CHLORO-2-PHENYL-6-[(PHENYLSULFONYL)METHYL]PYRIMIDINE