Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
10 mg | In stock | $ 43.00 | |
25 mg | In stock | $ 85.00 | |
50 mg | In stock | $ 150.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 48.00 |
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. |
Targets&IC50 | PTP:18.3 μM (IC50), PTP1B:14.5 μM (IC50), SHP2:1 μM (IC50) |
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). |
Molecular Weight | 468.46 |
Formula | C22H17FN4O5S |
CAS No. | 1051387-90-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 50 mg/mL (106.73 mM)
You can also refer to dose conversion for different animals. More
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SPI-112 1051387-90-6 Metabolism Phosphatase SPI 112 SPR inhibit SHP2 Inhibitor SPI112 PTP1B anticancer PTP PTPN11 competitive inhibitor