1. Metabolic Enzyme/Protease
  2. Phosphatase
  3. SPI-112

SPI-112 

Cat. No.: HY-101964
Handling Instructions

SPI-112 is a potent, selective and competitive SHP2 (PTPN11) inhibitor with IC50s of 1 μM, 18.3 μM and 14.5 μM for SHP2, protein tyrosine phosphatase (PTP) and PTP1B, respectively.

For research use only. We do not sell to patients.

SPI-112 Chemical Structure

SPI-112 Chemical Structure

CAS No. : 1051387-90-6

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Description

SPI-112 is a potent, selective and competitive SHP2 (PTPN11) inhibitor with IC50s of 1 μM, 18.3 μM and 14.5 μM for SHP2, protein tyrosine phosphatase (PTP) and PTP1B, respectively[1][2].

IC50 & Target

IC50: 1 μM (SHP2), 18.3 μM (PTP) and 14.5 μM (PTP1B)[2]

In Vitro

SPI-112 has a polar -NO2 or a negatively charged -COOH group and has no detectable cellular activity, suggesting that SPI-112 is not cell permeable[1].
In surface plasmon resonance (SPR) binding assay, SPI-112 displays a 1:1 stoichiometric binding kinetics to SHP2 with a kinetic constant KD of 1.30 µM. Enzyme kinetic data obtained with SPI-112 are best fitted with the competitive inhibition model (Ki of 0.8 µM), suggesting that SPI-112 interacts with the catalytic site of SHP2[1].

Molecular Weight

468.46

Formula

C₂₂H₁₇FN₄O₅S

CAS No.

1051387-90-6

SMILES

O=C(O)C1=CC=CC(N/N=C2C(NC3=C\2C=C(S(=O)(NCC4=CC=C(F)C=C4)=O)C=C3)=O)=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

SPI-112SPI112SPI 112PhosphatasePTPSHP2PTPN11anticancerPTP1BSPRcompetitiveInhibitorinhibitorinhibit

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