SPI-112 是一种有效的，选择性和竞争性的 SHP2 (PTPN11) 抑制剂，对 SHP2，蛋白酪氨酸磷酸酶 (PTP) 和 PTP1B 的 IC₅₀ 分别为 1 μM，18.3 μM 和 14.5 μM。

SPI-112 is a potent, selective and competitive SHP2 (PTPN11) inhibitor with IC 50 s of 1 μM, 18.3 μM and 14.5 μM for SHP2, protein tyrosine phosphatase (PTP) and PTP1B, respectively.

Solid

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

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.
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. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

4°C, protect from light In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

[1]. Chen L, et al. Inhibition of cellular Shp2 activity by a methyl ester analog of SPI-112. Biochem Pharmacol. 2010 Sep 15;80(6):801-10.
[2]. Lawrence HR, et al. Inhibitors of Src homology-2 domain containing protein tyrosine phosphatase-2 (Shp2) based on oxindole scaffolds. J Med Chem. 2008 Aug 28;51(16):4948-56.

In Vitro: DMSO : 50 mg/mL (106.73 mM; Need ultrasonic)配制储备液