1954650-11-3
Chemical Structure
JMS-053
- CAS No.: 1954650-11-3
- Formula:C13H8N2O2S
- Molecular Weight:256.28
IUPAC Name: 7-imino-2-phenylthieno[3,2-c]pyridine-4,6(5H,7H)-dione
InChIKey: CQHAROORCYWRRH-UHFFFAOYSA-N
SMILES: O=C1C(C=C(C2=CC=CC=C2)S3)=C3C(C(N1)=O)=N
Biological Activity: 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].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
|
|
JMS-053 | 98.0% | 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. | ||||||||||||||||||||
|
loading...
/
|
|||||||||||||||||||||||
References
- [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. [Content Brief]
- [2]. McQueeney KE, et al. Targeting ovarian cancer and endothelium with an allosteric PTP4A3 phosphatase inhibitor. Oncotarget. 2017 Dec 30;9(9):8223-8240. [Content Brief]
- [3]. 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. [Content Brief]
- [4]. 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. [Content Brief]
- [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. [Content Brief]
