MedKoo Biosciences

PHPS1
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 561287

CAS#: 314291-83-3

Description: 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

CAS# 314291-83-3

Product data Instruction

Theoretical Analysis

MedKoo Cat#: 561287
Name: PHPS1
CAS#: 314291-83-3
Chemical Formula: C21H15N5O6S
Exact Mass: 465.07
Molecular Weight: 465.440
Elemental Analysis: C, 54.19; H, 3.25; N, 15.05; O, 20.62; S, 6.89

Price and Availability

Size	Price	Availability
100mg	USD 1250	2 Weeks
200mg	USD 1950	2 Weeks
500mg	USD 2950	2 Weeks
1g	USD 3950	2 Weeks
2g	USD 6950	2 Weeks
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

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

Product Data:

Product Data

Instruction:

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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/

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	Ethanol	93.0	199.81

Preparing Stock Solutions

The following data is based on the product molecular weight 465.440000000000000000000000000000 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.

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.

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1: 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 Jul 31. doi: 10.1021/acs.biochem.7b00638. [Epub ahead of print] PubMed PMID: 28759203. 2: 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. eCollection 2017. PubMed PMID: 28481957; PubMed Central PMCID: PMC5421800. 3: 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. PubMed PMID: 25331952; PubMed Central PMCID: PMC4256348. 4: 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. eCollection 2014. PubMed PMID: 25048202; PubMed Central PMCID: PMC4105620. 5: 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):2737-46. doi: 10.1038/jid.2014.252. Epub 2014 Jun 16. PubMed PMID: 24933319. 6: 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. PubMed PMID: 23673659; PubMed Central PMCID: PMC3689975. 7: 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. PubMed PMID: 18480264; PubMed Central PMCID: PMC2438240. 8: Hosaka Y, Okamoto R, Irinoda K, Kaieda S, Koizumi W, Saigenji K, Inoue M. Characterization of pKU701, a 2.5-kb plasmid, in a Japanese Helicobacter pylori isolate. Plasmid. 2002 May;47(3):193-200. PubMed PMID: 12151234. 9: De Ungria MC, Kolesnikow T, Cox PT, Lee A. Molecular characterization and interstrain variability of pHPS1, a plasmid isolated from the Sydney strain (SS1) of Helicobacter pylori. Plasmid. 1999 Mar;41(2):97-109. PubMed PMID: 10087213.

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