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SPI-112

Catalog No. T4340   CAS 1051387-90-6

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.

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SPI-112 Chemical Structure
SPI-112, CAS 1051387-90-6
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
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Purity: 96.01%
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Biological Description
Chemical Properties
Storage & Solubility Information
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

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 50 mg/mL (106.73 mM)

TargetMolReferences and Literature

1. Chen L, et al. Biochem Pharmacol. Inhibition of cellular Shp2 activity by a methyl ester analog of SPI-112 . 2010 Sep 15;80(6):801-10 2. Wu R, Wang C, Li Z, et al. SOX2 promotes resistance of melanoma with PD-L1 high expression to T-cell-mediated cytotoxicity that can be reversed by SAHA[J]. Journal for immunotherapy of cancer. 2020, 8(2).

TargetMolCitations

1. Wu R, Wang C, Li Z, et al. SOX2 promotes resistance of melanoma with PD-L1 high expression to T-cell-mediated cytotoxicity that can be reversed by SAHA. Journal for immunotherapy of cancer. 2020 Nov;8(2):e001037. 2. Lu X, Yu R, Li Z, et al.JC-010a, a novel selective SHP2 allosteric inhibitor, overcomes RTK/non-RTK-mediated drug resistance in multiple oncogene-addicted cancers.Cancer Letters.2023: 216517.

Related compound libraries

This product is contained In the following compound libraries:
Fluorochemical Library Glycometabolism Compound Library Lipid Metabolism Compound Library Inhibitor Library Target-Focused Phenotypic Screening Library Bioactive Compounds Library Max Bioactive Compound Library Phosphatase Inhibitor Library Metabolism Compound Library

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Keywords

SPI-112 1051387-90-6 Metabolism Phosphatase SPI 112 SPR inhibit SHP2 Inhibitor SPI112 PTP1B anticancer PTP PTPN11 competitive inhibitor

 

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