JMS-053

JMS-053 is an efficient and reversible PTP4A3 inhibitor, with an IC50 value of 18 nM. JMS-053 demonstrates broad PTP4A inhibitory activity with IC50s of 50 nM and 53 nM for PTP4A1 and PTP4A2, respectively. JMS-053 exhibits IC50 values of 92.6 nM and 207.6 nM for CDC25B and DUSP3, respectively. JMS-053 can effectively inhibit the activity of PTP4A3, inhibit tumor cell proliferation and migration through multiple mechanisms such as interfering with RhoA and STAT3/p38 signaling pathway. JMS-053 can be used for the study of cancers such as ovarian cancer, breast cancer and colon cancer[1][2][3][4][5].

Product Specifications

CAS Number

[1954650-11-3]

UNSPSC

12352005

Target

Phosphatase; Ras; STAT

Type

Reference compound

Related Pathways

GPCR/G Protein; JAK/STAT Signaling; MAPK/ERK Pathway; Metabolic Enzyme/Protease; Stem Cell/Wnt

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/jms-053.html

Purity

98.0

Solubility

DMSO : 10 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

O=C1C(C=C(C2=CC=CC=C2)S3)=C3C(C(N1)=O)=N

Molecular Formula

C13H8N2O2S

Molecular Weight

256.28

References & Citations

[1]Lazo JS, et, al. Next-Generation Cell-Active Inhibitors of the Undrugged Oncogenic PTP4A3 Phosphatase. J Pharmacol Exp Ther. 2019 Dec;371 (3) :652-662.|[2]McQueeney KE, et al. Targeting ovarian cancer and endothelium with an allosteric PTP4A3 phosphatase inhibitor. Oncotarget. 2017 Dec 30;9 (9) :8223-8240.|[3]Rastelli EJ, et al. Synthesis and evaluation of bifunctional PTP4A3 phosphatase inhibitors activating the ER stress pathway. Bioorg Med Chem Lett. 2021 Aug 15;46:128167. |[4]Lazo JS, Isbell KN, Vasa SA, Llaneza DC, Rastelli EJ, Wipf P, Sharlow ER. Disruption of Ovarian Cancer STAT3 and p38 Signaling with a Small-Molecule Inhibitor of PTP4A3 Phosphatase. J Pharmacol Exp Ther. 2023 Mar;384 (3) :429-438. doi: 10.1124/jpet.122.001401. Epub 2023 Jan 10. PMID: 36627205; PMCID: PMC9976793.|[5]McQueeney KE, et al. A chemical genetics approach identifies PTP4A3 as a regulator of colon cancer cell adhesion. FASEB J. 2018 Oct;32 (10) :5661-5673. doi: 10.1096/fj.201701446R. Epub 2018 May 10. PMID: 29746167; PMCID: PMC6133700.