| Name | SPI-112 |
| Description | SPI-112, the SPI-112 methyl ester analog, can inhibit cellular Shp2 PTP activity. SPI-112 bound to Shp2 by surface plasmon resonance (SPR) and displayed competitive inhibitor kinetics to Shp2. |
| Kinase Assay | The activity of c-KIT kinase is determined by following the production of ADP from the kinase reaction through coupling with the pyruvate kinase/lactate dehydrogenase system. In this assay, the oxidation of NADH (thus the decrease at A340 nM) is continuously monitored spectrophotometrically. The reaction mixture (100 μL) contained c-KIT (cKIT residues T544-V976, from ProQinase, 5.4 nM), polyE4Y (1 mg/mL), MgC12 (10 mM), pyruvate kinase (4 units), lactate dehydrogenase (0.7 units), phosphoenol pyruvate (1 mM), and NADH (0.28 mM) in 90 mM Tris buffer containing 0.2 % octyl-glucoside and 1% DMSO, pH 7.5. Test compounds (e.g., DCC-2618) are incubated with c-KIT and other reaction reagents at 22 °C for < 2 min before ATP (200 μM) is added to start the reaction. The absorption at 340 nm is monitored continuously for 0.5 hours at 30 °C on Polarstar Optima plate reader (BMG). The reaction rate is calculated using the 0 to 0.5 h time frame. Percent inhibition is obtained by comparison of reaction rate with that of a control (i.e. with no test compound). |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 50 mg/mL (106.73 mM), Sonication is recommended.
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| Keywords | SPR | SPI-112 | SPI112 | SPI 112 | SHP-2 | SHP2 | PTPN11 | PTP1B | PTP | Phosphatase | Inhibitor | inhibit | competitive | anticancer |
| Inhibitors Related | PTP1B-IN-22 | Disodium monofluorophosphate | β-Glycerophosphate disodium salt pentahydrate | Idoxuridine | Tartaric acid disodium dihydrate | Cyclosporine | Stearic acid | Cis-5-Norbornene-exo-2,3-dicarboxylic Anhydride | CaMKP Inhibitor | L-Ascorbic acid 2-phosphate magnesium | Cyclosporin A | Trimyristin |
| Related Compound Libraries | Glycometabolism Compound Library | Target-Focused Phenotypic Screening Library | Bioactive Compound Library | Inhibitor Library | Metabolism Compound Library | Lipid Metabolism Compound Library | Bioactive Compounds Library Max | Fluorochemical Library | Phosphatase Inhibitor Library |
United States
