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Chemical Structure| 314291-83-3 Chemical Structure| 314291-83-3

Structure of PHPS1
CAS No.: 314291-83-3

Chemical Structure| 314291-83-3

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PHPS1 is a potent and selective SHP2 inhibitor with Ki value of 0.73μM.

Synonyms: Phenylhydrazonopyrazolone sulfonate 1; PTP Inhibitor V; Protein Tyrosine Phosphatase Inhibitor V

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Product Details of PHPS1

CAS No. :314291-83-3
Formula : C21H15N5O6S
M.W : 465.44
SMILES Code : O=S(C1=CC=C(NN=C2C(C3=CC=C([N+]([O-])=O)C=C3)=NN(C4=CC=CC=C4)C2=O)C=C1)(O)=O
Synonyms :
Phenylhydrazonopyrazolone sulfonate 1; PTP Inhibitor V; Protein Tyrosine Phosphatase Inhibitor V
MDL No. :MFCD01079012
InChI Key :IYPHPQODKSHEHV-UHFFFAOYSA-N
Pubchem ID :3109390

Safety of PHPS1

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H315-H319-H335
Precautionary Statements:P261-P264-P271-P280-P302+P352-P304+P340-P305+P351+P338-P312-P332+P313-P337+P313-P362-P403+P233-P405-P501

Isoform Comparison

Biological Activity

In Vitro:

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
Bovine oocytes 5 µM 22 hours PHPS1 inhibits SHP2 phosphatase activity, reducing oocyte maturation and embryo development. Cells. 2019 Oct 18;8(10):1272
THP-1 macrophages 10 mm 24 hours 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

In Vivo:

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. Cell Commun Signal. 2023 Dec 18;21(1):362

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.15mL

0.43mL

0.21mL

10.74mL

2.15mL

1.07mL

21.49mL

4.30mL

2.15mL

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