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MedKoo Cat#: 561287 | Name: PHPS1
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

PHPS1 is an inhibitor of the protein tyrosine phosphatase Shp2. PHPS1 also efficiently inhibits activation of Erk1/2 by the leukemia-associated Shp2 mutant, Shp2-E76K, and blocks the anchorage-independent growth of a variety of human tumor cell lines.

Chemical Structure

PHPS1
PHPS1
CAS#314291-83-3 (free acid)

Theoretical Analysis

MedKoo Cat#: 561287

Name: PHPS1

CAS#: 314291-83-3 (free acid)

Chemical Formula: C21H15N5O6S

Exact Mass: 465.0743

Molecular Weight: 465.44

Elemental Analysis: C, 54.19; H, 3.25; N, 15.05; O, 20.62; S, 6.89

Price and Availability

Size Price Availability Quantity
100mg USD 1,250.00 2 Weeks
200mg USD 1,950.00 2 Weeks
500mg USD 2,950.00 2 Weeks
1g USD 3,950.00 2 Weeks
2g USD 6,950.00 2 Weeks
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Related CAS #
314291-83-3 (free acid) 1177131-02-0 (Na)
Synonym
PHPS1; PHPS 1; PHPS-1
IUPAC/Chemical Name
4-[2-[1,5-dihydro-3-(4-nitrophenyl)-5-oxo-1-phenyl-4H-pyrazol-4-ylidene]hydrazinyl]-benzenesulfonic Acid
InChi Key
VIQSBJOMLQLAKC-BSYVCWPDSA-N
InChi Code
InChI=1S/C21H15N5O6S/c27-21-20(23-22-15-8-12-18(13-9-15)33(30,31)32)19(14-6-10-17(11-7-14)26(28)29)24-25(21)16-4-2-1-3-5-16/h1-13,22H,(H,30,31,32)/b23-20+
SMILES Code
O=S(C1=CC=C(N/N=C2C(C3=CC=C([N+]([O-])=O)C=C3)=NN(C4=CC=CC=C4)C\2=O)C=C1)(O)=O
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Product Data
Product Data
Instruction
View handling instruction
Biological target:
PHPS1 is a potent and selective Shp2 inhibitor with Kis of 0.73, 5.8, 10.7, 5.8, and 0.47 μM for Shp2, Shp2-R362K, Shp1, PTP1B, and PTP1B-Q.
In vitro activity:
This study identified the phenylhydrazonopyrazolone sulfonate PHPS1 as a potent and cell-permeable inhibitor, which is specific for Shp2 over the closely related tyrosine phosphatases Shp1 and PTP1B. PHPS1 inhibits Shp2-dependent cellular events such as hepatocyte growth factor/scatter factor (HGF/SF)-induced epithelial cell scattering and branching morphogenesis. PHPS1 also blocks Shp2-dependent downstream signaling, namely HGF/SF-induced sustained phosphorylation of the Erk1/2 MAP kinases and dephosphorylation of paxillin. Furthermore, PHPS1 efficiently inhibits activation of Erk1/2 by the leukemia-associated Shp2 mutant, Shp2-E76K, and blocks the anchorage-independent growth of a variety of human tumor cell lines. Reference: Proc Natl Acad Sci U S A. 2008 May 20;105(20):7275-80. https://pubmed.ncbi.nlm.nih.gov/18480264/
In vivo activity:
PHPS1 decreased the number of atherosclerotic plaques without significantly affecting body weight, serum glucose levels or lipid metabolism. Plaque composition analysis showed a significant decrease in the number of VSMCs in atherosclerotic lesions of Ldlr-/- mice treated with PHPS1. Stimulation with oxLDL induced a dose-dependent increase in the number of VSMCs and in SHP2 and ERK phosphorylation levels, and these effects were blocked by PHPS1. Reference: BMC Cardiovasc Disord. 2018 Apr 27;18(1):72. https://pubmed.ncbi.nlm.nih.gov/29703160/
Solvent mg/mL mM comments
Solubility
Ethanol 93.0 199.81
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 465.44 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Jiang J, Hu B, Chung CS, Chen Y, Zhang Y, Tindal EW, Li J, Ayala A. SHP2 inhibitor PHPS1 ameliorates acute kidney injury by Erk1/2-STAT3 signaling in a combined murine hemorrhage followed by septic challenge model. Mol Med. 2020 Sep 21;26(1):89. doi: 10.1186/s10020-020-00210-1. PMID: 32957908; PMCID: PMC7504828. 2. Hellmuth K, Grosskopf S, Lum CT, Würtele M, Röder N, von Kries JP, Rosario M, Rademann J, Birchmeier W. Specific inhibitors of the protein tyrosine phosphatase Shp2 identified by high-throughput docking. Proc Natl Acad Sci U S A. 2008 May 20;105(20):7275-80. doi: 10.1073/pnas.0710468105. Epub 2008 May 14. PMID: 18480264; PMCID: PMC2438240. 3. Lu Y, Ma Q, Tan H, Li X, Zhang X, Tie Y. Specific inhibition of SHP2 suppressed abdominal aortic aneurysm formation in mice by augmenting the immunosuppressive function of MDSCs. Life Sci. 2021 Jan 15;265:118751. doi: 10.1016/j.lfs.2020.118751. Epub 2020 Nov 12. PMID: 33189823. 4. Chen J, Cao Z, Guan J. SHP2 inhibitor PHPS1 protects against atherosclerosis by inhibiting smooth muscle cell proliferation. BMC Cardiovasc Disord. 2018 Apr 27;18(1):72. doi: 10.1186/s12872-018-0816-2. PMID: 29703160; PMCID: PMC5923012.
In vitro protocol:
1. Jiang J, Hu B, Chung CS, Chen Y, Zhang Y, Tindal EW, Li J, Ayala A. SHP2 inhibitor PHPS1 ameliorates acute kidney injury by Erk1/2-STAT3 signaling in a combined murine hemorrhage followed by septic challenge model. Mol Med. 2020 Sep 21;26(1):89. doi: 10.1186/s10020-020-00210-1. PMID: 32957908; PMCID: PMC7504828. 2. Hellmuth K, Grosskopf S, Lum CT, Würtele M, Röder N, von Kries JP, Rosario M, Rademann J, Birchmeier W. Specific inhibitors of the protein tyrosine phosphatase Shp2 identified by high-throughput docking. Proc Natl Acad Sci U S A. 2008 May 20;105(20):7275-80. doi: 10.1073/pnas.0710468105. Epub 2008 May 14. PMID: 18480264; PMCID: PMC2438240.
In vivo protocol:
1. Lu Y, Ma Q, Tan H, Li X, Zhang X, Tie Y. Specific inhibition of SHP2 suppressed abdominal aortic aneurysm formation in mice by augmenting the immunosuppressive function of MDSCs. Life Sci. 2021 Jan 15;265:118751. doi: 10.1016/j.lfs.2020.118751. Epub 2020 Nov 12. PMID: 33189823. 2. Chen J, Cao Z, Guan J. SHP2 inhibitor PHPS1 protects against atherosclerosis by inhibiting smooth muscle cell proliferation. BMC Cardiovasc Disord. 2018 Apr 27;18(1):72. doi: 10.1186/s12872-018-0816-2. PMID: 29703160; PMCID: PMC5923012.
1: Yu C, Li Z, Nie C, Chang L, Jiang T. Targeting Src homology phosphatase 2 ameliorates mouse diabetic nephropathy by attenuating ERK/NF-κB pathway-mediated renal inflammation. Cell Commun Signal. 2023 Dec 18;21(1):362. doi: 10.1186/s12964-023-01394-9. PMID: 38110973; PMCID: PMC10729421. 2: Gao Q, Lu Y, Zhou W. Specific knockout of notch-1 attenuates non-alcoholic fatty liver disease by promoting SHP2 phosphorylation. Aging (Albany NY). 2023 Dec 13;15(23):14323-14332. doi: 10.18632/aging.205305. Epub 2023 Dec 13. PMID: 38095642; PMCID: PMC10756087. 3: Li Z, Xi J, Li B, Liu Y, Wang G, Yu B, Ma H, Li Z, Zhang Z. SHP-2-induced M2 polarization of tumor associated macrophages via IL-4 regulate colorectal cancer progression. Front Oncol. 2023 Jan 26;13:1027575. doi: 10.3389/fonc.2023.1027575. PMID: 36776333; PMCID: PMC9909964. 4: Lu YG, Tan H, Ma Q, Li XX, Cui J, Zhang X, Liang XL, Tie YQ. SH2 domain- containing protein tyrosine phosphatase-2 (SHP-2) prevents cardiac remodeling after myocardial infarction through ERK/SMAD signaling pathway. Hum Cell. 2021 Mar;34(2):325-334. doi: 10.1007/s13577-020-00430-x. Epub 2021 Jan 8. PMID: 33415691. 5: Chang CJ, Lin CF, Lee CH, Chuang HC, Shih FC, Wan SW, Tai C, Chen CL. Overcoming interferon (IFN)-γ resistance ameliorates transforming growth factor (TGF)-β-mediated lung fibroblast-to-myofibroblast transition and bleomycin- induced pulmonary fibrosis. Biochem Pharmacol. 2021 Jan;183:114356. doi: 10.1016/j.bcp.2020.114356. Epub 2020 Dec 4. PMID: 33285108. 6: Lu Y, Ma Q, Tan H, Li X, Zhang X, Tie Y. Specific inhibition of SHP2 suppressed abdominal aortic aneurysm formation in mice by augmenting the immunosuppressive function of MDSCs. Life Sci. 2021 Jan 15;265:118751. doi: 10.1016/j.lfs.2020.118751. Epub 2020 Nov 12. PMID: 33189823. 7: Jiang J, Hu B, Chung CS, Chen Y, Zhang Y, Tindal EW, Li J, Ayala A. SHP2 inhibitor PHPS1 ameliorates acute kidney injury by Erk1/2-STAT3 signaling in a combined murine hemorrhage followed by septic challenge model. Mol Med. 2020 Sep 21;26(1):89. doi: 10.1186/s10020-020-00210-1. PMID: 32957908; PMCID: PMC7504828. 8: Liu W, Yin Y, Wang M, Fan T, Zhu Y, Shen L, Peng S, Gao J, Deng G, Meng X, Kong L, Feng GS, Guo W, Xu Q, Sun Y. Disrupting phosphatase SHP2 in macrophages protects mice from high-fat diet-induced hepatic steatosis and insulin resistance by elevating IL-18 levels. J Biol Chem. 2020 Jul 31;295(31):10842-10856. doi: 10.1074/jbc.RA119.011840. Epub 2020 Jun 16. PMID: 32546483; PMCID: PMC7397102. 9: Idrees M, Xu L, Song SH, Joo MD, Lee KL, Muhammad T, El Sheikh M, Sidrat T, Kong IK. PTPN11 (SHP2) Is Indispensable for Growth Factors and Cytokine Signal Transduction During Bovine Oocyte Maturation and Blastocyst Development. Cells. 2019 Oct 18;8(10):1272. doi: 10.3390/cells8101272. PMID: 31635340; PMCID: PMC6830097. 10: Cheng Y, Yu M, Xu J, He M, Wang H, Kong H, Xie W. Inhibition of Shp2 ameliorates monocrotaline-induced pulmonary arterial hypertension in rats. BMC Pulm Med. 2018 Aug 7;18(1):130. doi: 10.1186/s12890-018-0700-y. PMID: 30086741; PMCID: PMC6081862. 11: Chen J, Cao Z, Guan J. SHP2 inhibitor PHPS1 protects against atherosclerosis by inhibiting smooth muscle cell proliferation. BMC Cardiovasc Disord. 2018 Apr 27;18(1):72. doi: 10.1186/s12872-018-0816-2. PMID: 29703160; PMCID: PMC5923012. 12: Sakurada S, Fujiwara S, Suzuki M, Kogure T, Uchida T, Umemura T, Tsuzuki M. Involvement of Acidic Polysaccharide Ph-PS-2 and Protein in Initiation of Coccolith Mineralization, as Demonstrated by In Vitro Calcification on the Base Plate. Mar Biotechnol (NY). 2018 Jun;20(3):304-312. doi: 10.1007/s10126-018-9818-4. Epub 2018 Apr 4. PMID: 29619589. 13: Salem IH, Plante S, Gounni AS, Rouabhia M, Chakir J. A shift in the IL-6/STAT3 signalling pathway imbalance towards the SHP2 pathway in severe asthma results in reduced proliferation process. Cell Signal. 2018 Mar;43:47-54. doi: 10.1016/j.cellsig.2017.12.001. Epub 2017 Dec 11. PMID: 29242170. 14: Zhou W, Yin Y, Weinheimer AS, Kaur N, Carpino N, French JB. Structural and Functional Characterization of the Histidine Phosphatase Domains of Human Sts-1 and Sts-2. Biochemistry. 2017 Sep 5;56(35):4637-4645. doi: 10.1021/acs.biochem.7b00638. Epub 2017 Aug 21. PMID: 28759203; PMCID: PMC5907918. 15: Qiu Z, Zhou J, Liu F, Qin X, Dai Y, Ke Y, Chen Z, Li W, Ying S, Shen H. Deletion of Shp2 in bronchial epithelial cells impairs IL-25 production in vitro, but has minor influence on asthmatic inflammation in vivo. PLoS One. 2017 May 8;12(5):e0177334. doi: 10.1371/journal.pone.0177334. PMID: 28481957; PMCID: PMC5421800. 16: Xia LX, Hua W, Jin Y, Tian BP, Qiu ZW, Zhang C, Che LQ, Zhou HB, Wu YF, Huang HQ, Lan F, Ke YH, Lee JJ, Li W, Ying SM, Chen ZH, Shen HH. Eosinophil differentiation in the bone marrow is promoted by protein tyrosine phosphatase SHP2. Cell Death Dis. 2016 Apr 7;7(4):e2175. doi: 10.1038/cddis.2016.74. Erratum in: Cell Death Differ. 2019 Sep;26(9):1859-1860. doi: 10.1038/s41418-018-0247-8. PMID: 27054330; PMCID: PMC4855658. 17: Li S, Wang L, Zhao Q, Liu Y, He L, Xu Q, Sun X, Teng L, Cheng H, Ke Y. SHP2 positively regulates TGFβ1-induced epithelial-mesenchymal transition modulated by its novel interacting protein Hook1. J Biol Chem. 2014 Dec 5;289(49):34152-60. doi: 10.1074/jbc.M113.546077. Epub 2014 Oct 20. PMID: 25331952; PMCID: PMC4256348. 18: Li J, Kang Y, Wei L, Liu W, Tian Y, Chen B, Lin X, Li Y, Feng GS, Lu Z. Tyrosine phosphatase Shp2 mediates the estrogen biological action in breast cancer via interaction with the estrogen extranuclear receptor. PLoS One. 2014 Jul 21;9(7):e102847. doi: 10.1371/journal.pone.0102847. PMID: 25048202; PMCID: PMC4105620. 19: Wang X, Zhang A, Gao J, Chen W, Wang S, Wu X, Shen Y, Ke Y, Hua Z, Tan R, Sun Y, Xu Q. Trichomide A, a natural cyclodepsipeptide, exerts immunosuppressive activity against activated T lymphocytes by upregulating SHP2 activation to overcome contact dermatitis. J Invest Dermatol. 2014 Nov;134(11):2737-2746. doi: 10.1038/jid.2014.252. Epub 2014 Jun 16. PMID: 24933319. 20: Schramm C, Edwards MA, Krenz M. New approaches to prevent LEOPARD syndrome- associated cardiac hypertrophy by specifically targeting Shp2-dependent signaling. J Biol Chem. 2013 Jun 21;288(25):18335-44. doi: 10.1074/jbc.M113.483800. Epub 2013 May 14. PMID: 23673659; PMCID: PMC3689975.

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PNU 142300

PNU 142300