PHPS1 is a potent and selective SHP2 inhibitor with Ki value of 0.73μM[1]. PHPS1 at dose of 3mg/kg (i.p.) decreased the number of atherosclerotic plaques without significantly affecting body weight, serum glucose levels or lipid metabolism in high-cholesterol diet fed Ldlr−/− mice[2].
PHPS1 细胞实验
Cell Line
Concentration
Treated Time
Description
References
MOLM-13 cells
10 µg/mL
12 hours
Inhibit SHP2 protein expression and reverse the promoting effect of Siglec6 overexpression on the proliferation, invasion, and migration abilities of AML cells
Sci Rep. 2025 May 28;15(1):18611
Madin-Darby canine kidney (MDCK) cells
5 µM
20 hours
PHPS1 completely inhibited HGF/SF-induced scattering of MDCK cells
Proc Natl Acad Sci U S A. 2008 May 20;105(20):7275-80
Low expression of SHP-2 promoted the protein levels of Arginase-1 and IL-10, while inhibited those of IL-1β and TNF-α in M2 macrophages.
Front Oncol. 2023 Jan 26;13:1027575
HK-2 cells
5 µM
24 hours
Pre-treatment with PHPS1 prevented elevated production of proinflammatory cytokines (TNF-α, IL-6, and CCL-2) induced by high glucose (HG, 30 mM) stimulation, indicating that PHPS1 treatment repressed HG-induced inflammatory responses.
Cell Commun Signal. 2023 Dec 18;21(1):362
A549 cells
20 µM
48 hours
PHPS1 inhibited TGFβ1-induced EMT phenotype, manifested by reduced expression of Snail1, COL1A1 and weakened activation of ERK and Smad pathways
J Biol Chem. 2014 Dec 5;289(49):34152-60
Bone-marrow-derived eosinophils
20 µM
6 days
PHPS-1 significantly reduced the production of eosinophils without affecting their apoptosis.
Cell Death Dis. 2016 Apr 7;7(4):e2175
PHPS1 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Mice
HFD-induced obesity and insulin resistance model
Intraperitoneal injection
2 mg/kg
Every 16 days for 16 days
To study the ameliorative effect of PHPS1 on HFD-induced insulin resistance and hepatic steatosis
J Biol Chem. 2020 Jul 31;295(31):10842-10856
Male C57BL/6 mice
Hemorrhagic shock followed by cecal ligation and puncture model
Subcutaneous injection
3 mg/kg
Two injections, immediately after hemorrhagic shock and immediately after CLP
PHPS1 significantly attenuated Hem/CLP-induced kidney injury, including reduced serum BUN, Cre, and NGAL levels, decreased kidney histopathological changes, and inhibited the activation of Erk1/2 and STAT3 signaling pathways.
Mol Med. 2020 Sep 21;26(1):89
Mice
Allergic asthma model
Intraperitoneal injection
5 mg/kg
Injected 1 hour before each OVA challenge, for 3 days
PHPS-1 significantly alleviated eosinophilic airway inflammation and airway hyper-responsiveness, accompanied by significantly reduced levels of systemic eosinophils and eosinophil lineage-committed progenitors in allergic mice.
Cell Death Dis. 2016 Apr 7;7(4):e2175
Mice
Db/db mice
Intraperitoneal injection
8 mg/kg
Once daily for 12 weeks
PHPS1 treatment significantly reduced serum creatinine levels and urine albumin-to-creatinine ratio (UACR) in db/db mice, alleviated glomerulosclerosis and tubulointerstitial injury, and decreased the production of proinflammatory cytokines (TNF-α, IL-6, and CCL-2) and macrophage infiltration.
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