2-Cyano-3-(1-phenyl-1H-indol-3-yl)-2-propenoicacid
2-cyano-3-(1-phenylindol-3-yl)acrylate
CAS: 56396-35-1
Molecular Formula: C18H12N2O2
2-Cyano-3-(1-phenyl-1H-indol-3-yl)-2-propenoicacid - Names and Identifiers
2-Cyano-3-(1-phenyl-1H-indol-3-yl)-2-propenoicacid - Physico-chemical Properties
| Molecular Formula | C18H12N2O2 |
| Molar Mass | 288.3 |
| Density | 1.20 |
| Melting Point | 235-238°C |
| Boling Point | 448.6±45.0 °C(Predicted) |
| Solubility | DMSO: >20mg/mL |
| Appearance | Morphological powder |
| Color | yellow to tan |
| pKa | 1.49±0.19(Predicted) |
| Storage Condition | 2-8°C |
| Stability | Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 1 month. |
| MDL | MFCD19443867 |
| Physical and Chemical Properties | Bioactive UK-5099 (PF-1005023) is a potent inhibitor of the mitochondrial pyruvate transporter (MPC) with an IC50 value of 50 nM for inhibiting pyruvate-dependent O2 consumption. |
| Use | UK-5099 |
| In vitro study | The trypanosomal pyruvate carrier is found to be rather insensitive to inhibition by alpha-cyano-4-hydroxycinnamate (K i =17 mM) but can be completely blocked by UK-5099 (K i =49 microM). UK-5099 also inhibits the monocarboxylate transporter (MCT) . UK5099 significantly inhibits the glucose-stimulated rise in oxygen consumption in a dose-dependent manner and at 150 μM reduced oxygen consumption below basal levels. UK5099 reduces ATP levels and increases ADP and AMP levels in 832/13 cells. The UK5099 treated cells show significantly higher proportion of side population fraction and express higher levels of stemness markers Oct3/4 and Nanog. UK5099 application may be an ideal model for Warburg effect studies. |
| In vivo study | The MPC inhibitor UK5099 increases the glucose excursion seen during an intraperitoneal glucose tolerance test in C57BLK mice. |
2-Cyano-3-(1-phenyl-1H-indol-3-yl)-2-propenoicacid - Risk and Safety
| WGK Germany | 3 |
2-Cyano-3-(1-phenyl-1H-indol-3-yl)-2-propenoicacid - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 3.469 ml | 17.343 ml | 34.686 ml |
| 5 mM | 0.694 ml | 3.469 ml | 6.937 ml |
| 10 mM | 0.347 ml | 1.734 ml | 3.469 ml |
| 5 mM | 0.069 ml | 0.347 ml | 0.694 ml |
Last Update：2024-01-02 23:10:35
2-Cyano-3-(1-phenyl-1H-indol-3-yl)-2-propenoicacid - Reference Information
| biological activity | UK-5099 (PF-1005023) is an effective inhibitor of mitochondrial pyruvate transporter (MPC), and the IC50 value for inhibiting pyruvate-dependent O2 consumption is 50 nM. |
| target | TargetValue mitochondrial pyruvate carrier () 49 μM(Ki) |
| Target | Value |
| mitochondrial pyruvate carrier () | 49 μM(Ki) |
| in vitro study | the trypanosomal pyruvate carrier is found to be rather insensitive to inhibition by alpha-cyano-4-hydroxycinnamate (K I = 17 mM) but can be completely blocked by UK-5099 (K I = 49 microM). UK-5099 also inhibits the monocarboxylate transporter (MCT) . UK5099 significantly inhibits the glucose-stimulated rise in oxygen consumption in a dose-dependent manner and at 150 μM reduced oxygen consumption below basic levels. UK5099 reduces ATP levels and increases ADP and AMP levels in 832/13 cells. The UK5099 treated cells show significantly higher proportion of side population fraction and express higher levels of stemness markers Oct 3/4 and Nanog. UK5099 application may be an open model for Warburg effect studies. |
| in vivo study | The MPC inhibitor UK5099 increases the glucose excursion seen during an intraperitoneal glucose tolerance test in C57BLK mice. |
Last Update：2024-04-10 22:29:15
2-Cyano-3-(1-phenyl-1H-indol-3-yl)-2-propenoicacid - Uses and synthesis methods
Target
Target Value
mitochondrial pyruvate carrier
49 μM(Ki)
in vitro studies
The trypanosomal pyruvate carrier is found to be rather insensitive to inhibition by alpha-cyano-4-hydroxycinnamate (K I =17 mM) but can be completely blocked by UK-5099 (K I =49 microM). UK-5099 also inhibits the monocarboxylate transporter (MCT) . UK5099 significantly inhibits the glucose-stimulated rise in oxygen consumption in a dose-dependent manner and at 150 μM reduced oxygen consumption below basal levels. UK5099 reduces ATP levels and increases ADP and AMP levels in 832/13 cells. The UK5099 treated cells show significantly higher proportion of side population fraction and express higher levels of stemness markers Oct3/4 and Nanog. UK5099 application may be an ideal model for Warburg effect studies.
In vivo studies
The MPC inhibitor UK5099 increases the glucose excursion seen during an intraperitoneal glucose tolerance test in C57BLK mice.
Last Update：2024-04-09 19:04:56
Supplier List
Spot supply
Product Name: UK-5099 Visit Supplier Webpage Request for quotationCAS: 56396-35-1
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
Spot supply
Product Name: UK-5099 Visit Supplier Webpage Request for quotationCAS: 56396-35-1
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
View History