2. Metabolic Enzyme/Protease Stem Cell/Wnt JAK/STAT Signaling GPCR/G Protein MAPK/ERK Pathway
  3. Phosphatase STAT Ras
  4. 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.

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JMS-053

JMS-053 Chemical Structure

CAS No. : 1954650-11-3

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Customer Review

Based on 3 publication(s) in Google Scholar

JMS-053 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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].

IC50 & Target[3]

STAT3

 

Cellular Effect
Cell Line Type Value Description References
MDA-MB-231 EC50
42.7 μM
Compound: 1; JMS-053
Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability measured after 72 hrs by CellTiter-Glo assay
Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability measured after 72 hrs by CellTiter-Glo assay
[PMID: 34089839]
In Vitro

JMS-053 (48 h) exhibits antiproliferative activity against MDA-MB-231 (IC50 = 32.67 μM; cytotoxicity: EC50 = 42.7 μM), Hs578T (IC50 = 8.48 μM), OVCAR4 (IC50 = 4.42 μM), Kuramochi (IC50 = 13.25 μM), A2780 (IC50 = 0.6 μM)[1][2][4].
JMS-053 (0.1-5 μM, 14 d) exhibits concentration-dependent inhibition of clone formation in PTP4A3 fl/fl cells, but has no inhibition in PTP4A3 -/- cells[5].
JMS-053 (0 nM-10 μM, 0-2 h) does not increased the level of ROS in OVCAR4 cells and no typical characteristics of oxidative stress is observed[1].
JMS-053 (5 μM, 0-24 h) normalizes trans-endothelial electrical resistance (TEER) after vascular endothelial growth factor (VEGF) or lipopolysaccharide (LPS) challenge in MVEC cells[2].
JMS-053 (0.1-40 μM, 15-24 h) inhibits the migration of HeyA8 cells, OVCAR4 WT cells and PTP4A3 fl/fl cells, but cannot in OVCAR4 RES cells and PTP4A3 -/- cells[2][3][5].
JMS-053 (0.1-1 μM) inhibits serum-induced RhoA activation in a concentration-dependent manner in HeyA8 cells[2].
JMS-053 (1.5-40 μM, 7 min-24 h) rapidly downregulates STAT3 activation by inhibiting PTP4A3, while rapidly upregulating the phosphorylation of SHP-2 phosphatase and p38 kinase in OVCAR4 WT cells[3].
JMS-053 (85.4 μM, 2 h) cannot activate the endoplasmatic reticulum (ER) stress/unfolded protein response (UPR) signaling pathway[4].
JMS-053 (1-5 μM) significantly reduces PTP4A3 fl/fl cell adhesion index and significantly inhibits the activation of RhoA induced by PDGF-β[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

JMS-053 Related Antibodies

Cell Migration Assay [2]

Cell Line: HeyA8 cells
Concentration: 0.75, 1.25, 2.5 μM
Incubation Time: 15 h
Result: Inhibited the migration of HeyA8 cells in a concentration-dependent manner.

Cell Migration Assay [3]

Cell Line: OVCAR4 WT and OVCAR4 RES cells
Concentration: 4.5 and 40 μM
Incubation Time: 24 h
Result: Effectively inhibited the cell migration stimulated by IL-6 in OVCAR4 WT cells, but not in OVCAR4 RES cells.

Western Blot Analysis[3]

Cell Line: OVCAR4 WT and OVCAR4 RES cells
Concentration: 1.5, 4.5, 40 μM
Incubation Time: 7, 15, 30 min, 1, 2, 4, 6 and 24 h
Result: Significantly reduced pY705-STAT3 in OVCAR4 WT cells.
Significantly increased the phosphorylation of SHP-2 at the Y580 and Y542 sites and the total level of SHP-2 protein remained unchanged in OVCAR4 WT cells.
Rapidly increased p38 phosphorylation in OVCAR4 WT cells.
Significantly weakened or eliminated the signal response, and the levels of p-p38 and pY705-STAT3 remained almost unchanged in OVCAR4 RES cells.

Cell Migration Assay [4]

Cell Line: PTP4A3 fl/fl cells and PTP4A3 -/- cells
Concentration: PTP4A3 fl/fl cells, but has no inhibition in PTP4A3 -/- cells
Incubation Time: 16 h
Result: Effectively inhibited the cell migration stimulated by IL-6 in PTP4A3 fl/fl cells, but not in PTP4A3 -/- cells.
In Vivo

JMS-053 (10 mg/kg, i.p., once daily for 5 consecutive days, followed by a 2-day break and then a 4-day continuous administration) effectively inhibit the growth of drug-resistant ovarian cancer in mice[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: HeyA8-MDR cells xenograft models established in female athymic nude mice[1]
Dosage: 10 mg/kg
Administration: intraperitoneal injection (i.p.), once daily for 5 consecutive days, followed by a 2-day break and then a 4-day continuous administration
Result: Reduced the average tumor weight by 45% compared to the control group with no significant difference in weight.
Molecular Weight

256.28

Formula

C13H8N2O2S
CAS No.
Appearance

Solid

Color

Light brown to brown

SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 10 mg/mL (39.02 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.9020 mL 19.5099 mL 39.0198 mL
5 mM 0.7804 mL 3.9020 mL 7.8040 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 1 mg/mL (3.90 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 1 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.9020 mL 19.5099 mL 39.0198 mL 97.5496 mL
5 mM 0.7804 mL 3.9020 mL 7.8040 mL 19.5099 mL
10 mM 0.3902 mL 1.9510 mL 3.9020 mL 9.7550 mL
15 mM 0.2601 mL 1.3007 mL 2.6013 mL 6.5033 mL
20 mM 0.1951 mL 0.9755 mL 1.9510 mL 4.8775 mL
25 mM 0.1561 mL 0.7804 mL 1.5608 mL 3.9020 mL
30 mM 0.1301 mL 0.6503 mL 1.3007 mL 3.2517 mL
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JMS-053 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

JMS-0531954650-11-3JMS053JMS 053PhosphataseSTATRasPTP4A phosphataseEndoplasmatic reticulum stressDual-pathway agentsCancer cell deathChaperonesInhibitorinhibitorinhibit

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