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| Targets |
TCS 2210 targets mesenchymal stem cells, promoting their differentiation into a neuronal phenotype. Its mechanism involves upregulating the expression of key neuronal markers, such as β-III tubulin and neuron-specific enolase (NSE). The exact molecular target or signaling pathway through which it exerts this effect is not fully detailed in the provided literature, but it is a valuable tool for studying neuronal differentiation.
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| ln Vitro |
In PC12 cells (primary screening), TCS 2210 induced neurite outgrowth and increased neuronal markers β-III tubulin and neuron-specific enolase (NSE). In rat bone marrow MSCs, treatment with 20 μM TCS 2210 for 2 days caused significant morphological changes (neuronal-like phenotype) and increased β-III tubulin expression (Western blot and immunocytochemistry) without cytotoxicity. Nissl staining showed that >95% of MSCs converted to a neuronal phenotype after 48 h at 20 μM. TCS 2210 time-dependently increased β-III tubulin and NSE expression. Glial fibrillary acidic protein (GFAP, an astroglial marker) was not detected. Whole-cell patch clamp recordings showed that TCS 2210-treated MSCs exhibited outward K+ currents when voltage steps from -30 to 90 mV were applied, indicating neural electrophysiological properties; untreated MSCs showed no detectable outward current. Gene expression profiling by DNA microarray and quantitative PCR revealed that TCS 2210 dose-dependently increased cholinergic neuron receptor genes (Chrna2, Chrnb2, Chrma) and neuron-specific genes Fbxo2 and Sizn1. In FLIPR membrane potential assays, addition of acetylcholine (10 μM) to TCS 2210-treated MSCs induced a change in membrane potential, confirming cholinergic neuron properties [1].
In vitro, TCS 2210 is a potent inducer of neuronal differentiation in mesenchymal stem cells (MSCs). Treatment with TCS 2210 leads to a significant increase in the expression of the neuronal markers β-III tubulin and neuron-specific enolase (NSE). This effect is achieved without associated cytotoxicity, making it a reliable tool for differentiation studies. |
| ln Vivo |
In vivo, TCS 2210 has potential applications in regenerative medicine and the study of neurological disorders. By promoting the differentiation of MSCs into neurons, it could be used to replace damaged neurons or to study neurodevelopmental processes. However, specific in vivo efficacy data are not extensively detailed in the available literature.
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| Enzyme Assay |
In vitro differentiation assays for TCS 2210 involve culturing mesenchymal stem cells (MSCs) in appropriate media. The cells are then treated with varying concentrations of TCS 2210 for a defined period, typically several days. The expression of neuronal markers like β-III tubulin and NSE is then quantified by immunofluorescence staining, Western blot, or RT-PCR to assess the extent of differentiation.
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| Cell Assay |
Rat MSCs were isolated from bone marrow and characterized. Cells were treated with 20 μM TCS 2210 for 2 days. Immunocytochemistry: cells stained with anti-β-III tubulin antibody and DAPI. Western blot: protein lysates probed with antibodies against β-III tubulin, NSE, and GFAP. Nissl staining: used for neuron detection; differentiation efficiency estimated by cell counting. Whole-cell patch clamp: membrane currents recorded; K+ currents assessed by applying voltage pulses from -30 to 90 mV; data analyzed with pClamp 8.1. Quantitative PCR: mRNA levels of Chrna2, Chrnb2, Fbxo2, Sizn1 determined. FLIPR membrane potential assay: MSCs treated with 20 μM TCS 2210 for 48 h, then 10 μM acetylcholine added, and membrane potential changes detected using a FLIPR assay kit and Flex station software [1].
In vitro cell-based assays for TCS 2210 are primarily focused on its ability to induce neuronal differentiation. MSCs are cultured and treated with the compound, and the cells are then analyzed for morphological changes and the expression of neuronal markers. Cell viability assays, such as MTT, are also performed to confirm the lack of cytotoxicity. |
| Animal Protocol |
In vivo animal studies for TCS 2210 are not extensively detailed in the available literature. Potential studies could involve transplanting MSCs that have been pre-treated with TCS 2210 into animal models of neurological disease to assess their ability to integrate and restore function. Alternatively, the compound could be administered directly to promote endogenous neurogenesis.
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| ADME/Pharmacokinetics |
Specific pharmacokinetic properties of TCS 2210, such as half-life and bioavailability, are not detailed in the available literature. As a research compound, it is typically used in vitro at concentrations determined by its activity in cell-based assays. It is soluble in DMSO.
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| Toxicity/Toxicokinetics |
No cytotoxicity was observed in MSCs treated with 20 μM TCS 2210 for 2 days as determined by cell viability assessment (Figure S3 in Supporting Information) [1].
Comprehensive toxicological data for TCS 2210 are not available in the provided text. It is reported to induce differentiation without cytotoxicity in vitro, suggesting a favorable safety profile in cell culture. As a research compound, it is intended for laboratory use only. Safety precautions should be followed when handling this compound. |
| References | |
| Additional Infomation |
TCS 2210 (compound 1) was identified as a novel small molecule that induces neuronal differentiation from mesenchymal stem cells. It is the first reported small molecule that can direct MSCs to differentiate into neurons with demonstrated electrophysiological properties (K+ currents) and cholinergic neuron characteristics (acetylcholine response). It shows no cytotoxicity and is more effective in MSCs than NGF or neuropathiazole. This compound has potential as a tool for studying cell fate determination and for cell therapy applications in neurodegenerative diseases such as Parkinson's and Alzheimer's diseases [1].
TCS 2210 is a neuronal differentiation inducer for mesenchymal stem cells. It increases the expression of neuronal markers β-III tubulin and neuron-specific enolase (NSE). It is a valuable tool for studying neurogenesis and for potential applications in regenerative medicine. This product is for research use only. |
| Molecular Formula |
C18H17N3O3
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|---|---|
| Molecular Weight |
323.352
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| Exact Mass |
323.127
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| Elemental Analysis |
C, 66.86; H, 5.30; N, 13.00; O, 14.84
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| CAS # |
1201916-31-5
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| PubChem CID |
44607172
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
2.792
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
24
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| Complexity |
500
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| Defined Atom Stereocenter Count |
0
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| SMILES |
ONC(C1=CC=2N=C(CCCC3=CC=CC=C3)C(NC2C=C1)=O)=O
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| InChi Key |
ZOFZKGFBKISZRI-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H17N3O3/c22-17(21-24)13-9-10-14-16(11-13)19-15(18(23)20-14)8-4-7-12-5-2-1-3-6-12/h1-3,5-6,9-11,24H,4,7-8H2,(H,20,23)(H,21,22)
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| Chemical Name |
N-hydroxy-2-oxo-3-(3-phenylpropyl)-1H-quinoxaline-6-carboxamide
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| Synonyms |
TCS 2210; TCS-2210; TCS2210
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| HS Tariff Code |
2934.99.9001
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.0926 mL | 15.4631 mL | 30.9262 mL | |
| 5 mM | 0.6185 mL | 3.0926 mL | 6.1852 mL | |
| 10 mM | 0.3093 mL | 1.5463 mL | 3.0926 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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