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Purity: ≥98%
TCS-401 HCI is a novel, potent and selective inhibitor of protein-tyrosine phosphatase 1B (PTP1B) with Ki of 0.29 µM. PTP1B was expressed in the RPE layer of the normal retina. After retinal detachment, weak immunolabeling of PTP1B was seen in the RPE cells. TCS-401 promoted the proliferation and expression of cyclin A and cyclin D1 in RPE cells. TCS-401 induced RPE cells to differentiate toward better contractility and motility. A migration assay proved that inhibiting PTP1B improved the migratory activity of RPE cells. TCS-401 activated extracellular signal-regulated kinase (Erk) and protein kinase B (Akt) phosphorylation. Pretreatment with PD98059 and LY294002 abolished TCS-401-induced activation of Erk, Akt, cell proliferation, and cell migration.
| ln Vitro |
The proliferation of RPE cells was greatly enhanced by TCS-401 (0.5, 1, and 2 μM). At 1 and 2 μM concentrations, TCS-401 dramatically enhanced the expression of cyclin A and cyclin D1. This increase was concentration-dependent. Erk and Akt phosphorylation was considerably elevated by TCS-401 at concentrations of 0.5, 1, and 2 μM in comparison to the control group. Pretreatment with PD98059 or LY294002 can inhibit TCS-401's activation of Erk and Akt, respectively. Proliferation, differentiation, and migration of RPE cells are induced by CS-401 treatment through the activation of the MEK/Erk and PI3K/Akt signaling pathways [1]. Fibronectin and α-SMA reductions caused by RPTC-Sup were reduced by CS-401 in a dose-dependent manner. TCS-401 reverses fibronectin and α-SMA levels almost twice at a dose of 1 μM, and returns fibronectin and α-SMA expression to nearly normal levels at a dose of 2 μM [2].
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| References |
[1]. Du ZD, et al. Protein tyrosine phosphatase 1B regulates the activity of retinal pigment epithelial cells. Mol Vis. 2015 May 1;21:523-31.
[2]. Ponnusamy M, et al. Necrotic renal epithelial cell inhibits renal interstitial fibroblast activation: role of protein tyrosine phosphatase 1B. Am J Physiol Renal Physiol. 2013 Mar 15;304(6):F698-709 |
| Molecular Formula |
C10H11CLN2O5S
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|---|---|
| Molecular Weight |
306.7227
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| CAS # |
243966-09-8
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| Related CAS # |
243966-09-8 (HCI);243967-42-2 (free);
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| SMILES |
O=C(C1=C(NC(C(O)=O)=O)SC2=C1CCNC2)O.[H]Cl
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| InChi Key |
LQGCAMWQDSYOAY-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C10H10N2O5S.ClH/c13-7(10(16)17)12-8-6(9(14)15)4-1-2-11-3-5(4)18-8;/h11H,1-3H2,(H,12,13)(H,14,15)(H,16,17);1H
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| Chemical Name |
2-(Oxaloamino)-4,5,6,7-tetrahydrothieno[2,3-c]pyridine-3-carboxylic acid hydrochloride
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| Synonyms |
TCS-401 (HCI), TCS 401 (HCI), TCS401 (HCI), TCS-401 Hydrochloride
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
0.1 M NaOH : ~6.67 mg/mL (~21.75 mM)
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.2603 mL | 16.3015 mL | 32.6030 mL | |
| 5 mM | 0.6521 mL | 3.2603 mL | 6.5206 mL | |
| 10 mM | 0.3260 mL | 1.6302 mL | 3.2603 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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