TC-E 5003
Based on 4 publication(s) in Google Scholar
TC-E 5003 is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 of 1.5 µM against hPRMT1. TC-E 5003 modulates the lipopolysaccharide (LPS) (HY-D1056)-induced AP-1 and NF-κB signaling pathways with anti-inflammatory properties. TC-E 5003 also upregulates the expression of Ucp1 and Fgf21, activates protein kinase A signaling and lipolysis in primary subcutaneous adipocytes from both mouse and humans. TC-E 5003 is promising for research of obesity and associated metabolic disorders, oxidative stress, inflammation and cancers.
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- Purity : 98.06%
- CAS No.: 17328-16-4
- 화학식: C16H14Cl2N2O4S
- 분자량:401.26
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- Protocol
- 순도&문서
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) TC-E 5003
MoreAll Histone Methyltransferase Isoforms
MoreAll AP-1 Isoforms
More
Biological Activity
제품 설명
IC50 & Target
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PRMT1 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | GI50 |
0.702 μM
Compound: 44; Te-C-5003
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Anticancer activity against human A549 cells assessed as cell growth inhibition measured after 48 hrs by CCK-8 assay
Anticancer activity against human A549 cells assessed as cell growth inhibition measured after 48 hrs by CCK-8 assay
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[PMID: 36528996] |
| LNCaP | GI50 |
4.49 μM
Compound: 2e
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Growth inhibition of human LNCAP cells by MTS assay
Growth inhibition of human LNCAP cells by MTS assay
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[PMID: 21440447] |
| MCF7 | GI50 |
0.413 μM
Compound: 44; Te-C-5003
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Anticancer activity against human MCF7 cells assessed as cell growth inhibition measured after 48 hrs by CCK-8 assay
Anticancer activity against human MCF7 cells assessed as cell growth inhibition measured after 48 hrs by CCK-8 assay
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[PMID: 36528996] |
| MDA-MB-231 | GI50 |
0.597 μM
Compound: 44; Te-C-5003
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Anticancer activity against human MDA-MB-231 cells assessed as cell growth inhibition measured after 48 hrs by CCK-8 assay
Anticancer activity against human MDA-MB-231 cells assessed as cell growth inhibition measured after 48 hrs by CCK-8 assay
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[PMID: 36528996] |
| NCI-H1299 | GI50 |
0.684 μM
Compound: 44; Te-C-5003
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Anticancer activity against human NCI-H1299 cells assessed as cell growth inhibition measured after 48 hrs by CCK-8 assay
Anticancer activity against human NCI-H1299 cells assessed as cell growth inhibition measured after 48 hrs by CCK-8 assay
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[PMID: 36528996] |
In Vitro
TC-E 5003 (0-1 μM, 24 h) suppresses LPS-induced NO production in RAW264.7 cells[1].
TC-E 5003 (1 μM, 15-60 min) regulates LPS-induced AP-1 transcriptional activity by modulating the c-Jun gene expression in RAW264.7 cells[1].
TC-E 5003 (10 μM, 4 h) augments thermogenesis through increase in UCP1 expression without changing mitochondrial content and activates the downstream molecules of PKA signaling in primary iWAT cells[2].
TC-E 5003 (6 μM, 48 h) has a good inhibition on the proliferation of cancer cells[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:RAW264.7 cells
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Concentration:0-1 μM
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Incubation Time:24 h
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Result:Significantly and dose-dependently decreased NO production without cytotoxicity in RAW264.7 cells.
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Cell Line:RAW264.7 cells
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Concentration:1 μM
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Incubation Time:15-60 min
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Result:Remarkably reduced the expression of inducible NO synthase (iNOS), COX-2, TNF-α, IL-1β, IL-6 and suppressed the c-Jun transcription exposure to LPS in RAW264.7 cells.
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Cell Line:Primary iWAT cells
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Concentration:10 μM
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Incubation Time:4 h
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Result:Led significant increase in Ucp1 mRNA and protein expressions up to 24 h in primary iWAT cells.
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Cell Line:A549, A549-INEI, H1299, MCF-7, and MDAMB-231 cells
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Concentration:6 μM
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Incubation Time:48 h
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Result:Significantly inhibited the proliferation of A549, A549-INEI, H1299, MCF-7, and MDAMB-231 (77.11%, 45.44%, 80.11%, 86.77%, 71.43%) at 6.0 μM.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:A549 tumor xenograft ICR mouse model[3]
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Dosage:0.5-2.0 mg
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Administration:s.c., a single dose for 28 days
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Result:Achieved better antitumor effect in combination with INEI system in A549 tumor xenograft ICR mouse model.
Chemical Information
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CAS No. 17328-16-4
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Appearance Solid
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분자량 401.26
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화학식 C16H14Cl2N2O4S
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Color Off-white to light brown
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SMILES
O=S(C1=CC=C(NC(CCl)=O)C=C1)(C2=CC=C(NC(CCl)=O)C=C2)=O
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (4)
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Journal Impact Factor
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Most Recent
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Cell Mol Life Sci
Dietary advanced glycation end-products exacerbate sarcopenia onset by activating apoptosis through PRMT1-mediated CRTC3 arginine methylation. [Abstract]2025 Apr 7;82(1):142. PMID: 40192801 -
Hepatol Commun
PRMT1-mediated modification of H4R3me2a promotes liver cancer progression by enhancing the transcriptional activity of SOX18. [Abstract]2025 Mar 24;9(4):e0647. PMID: 40130992 -
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용액&용해도
In Vitro:
DMSO : 125 mg/mL (311.52 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (5.18 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (5.18 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Protocol
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How to Select the Route of Administration for Mammals
Route-of-administration selection in mammals is a pharmacokinetic, pharmacodynamic, formulation, animal-welfare, and translational decision, not a default technical choice. The selected route should match the study goal: intravenous dosing is most useful when complete systemic exposure and rapid onset are required, oral dosing is most translational for orally intended medicines but is affected by absorption and first-pass metabolism, subcutaneous or intramuscular dosing can provide slower systemic exposure, and intraperitoneal dosing can be useful in rodent proof-of-concept studies but may have limited clinical translation. Published route-comparison studies show that the same compound can produce different exposure, onset, bioavailability, tissue distribution, and tolerability depending on route; therefore, route choice should be supported by pilot pharmacokinetic or pharmacodynamic evidence when the literature is insufficient. Unresolved questions include how to standardize route sel
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RNA extraction experimental
By lysing cells, releasing RNA, and removing impurities such as proteins and DNA, high-purity RNA products are finally obtained. The commonly used traditional method is the guanidine isothiocyanate/phenol/chloroform method (Trizol), which is suitable for a variety of animal materials including animal tissues, microorganisms, cultured cells, etc., and most plant materials.
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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ROS/oxidative-stress fluorescent staining
ROS/oxidative-stress fluorescent staining uses cell-permeant fluorogenic probes that become fluorescent after oxidation inside cells or tissues; commonly used examples include DCFH-DA/DCFDA for broad cellular oxidant detection, DHE for superoxide-related signal detection, MitoSOX for mitochondrial superoxide-related signal detection, and CellROX probes for oxidative-stress-associated fluorescence readouts. The assay detects probe oxidation rather than a single ROS species unless the probe and analysis method have been chemically validated for that species. DCFH-DA enters cells, is deacetylated by intracellular esterases to DCFH, and produces fluorescent DCF after oxidation, so the readout is used as an operational measure of total cellular oxidative stress rather than a species-specific ROS measurement. DHE and MitoSOX can report superoxide-related oxidation, but red fluorescence alone can include non-specific ethidium-like oxidation products; HPLC or optimized spectral approaches are
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Large-size fat particle sorting
Large-size fat particle sorting is widely used to isolate cells up to 200 μm in diameter. Single-cell flow sorting will allow greater insight into adipocyte heterogeneity by identifying gene expression, protein composition, and metabolic signatures at the single-cell level.
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Research Protocol for Inflammation-related Diseases
The NLRP3 inflammasome is a cytosolic innate immune signaling platform that integrates priming signals and danger-signal activation to promote caspase-1 activation, maturation of IL-1β and IL-18, and gasdermin D-mediated pyroptotic cell death. The core experimental logic is to determine whether inflammatory disease phenotypes are driven by increased NLRP3 expression, ASC-containing inflammasome assembly, caspase-1 cleavage, GSDMD cleavage, and extracellular release of IL-1β/IL-18 rather than by nonspecific cell injury alone. The pathway is strongly linked to inflammation-related disease phenotypes because monosodium urate crystals activate NALP3/NLRP3 inflammasome signaling in gout-like crystal inflammation, cholesterol crystals activate NLRP3 inflammasomes in atherogenesis models, and DSS-induced intestinal inflammation has been reported to involve NLRP3 inflammasome activity. However, experimental colitis studies also show context-dependent protective effects of NLRP3 inflammasome co
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Research Protocol for Metabolic Diseases
AMP-activated protein kinase, AMPK, is a conserved cellular energy sensor that responds to reduced cellular energy status and coordinates metabolism by increasing ATP-generating catabolic pathways while suppressing ATP-consuming anabolic processes. In metabolic disease research, the AMPK pathway is experimentally relevant because it regulates hepatic lipid synthesis, fatty acid oxidation, glucose production, skeletal-muscle glucose disposal, mTORC1-linked biosynthesis, autophagy, mitochondrial homeostasis, and whole-body energy balance. The central pathway logic is that energy stress, metformin, exercise-like stimulation, or direct AMPK activators increase AMPKα Thr172 phosphorylation and downstream substrate phosphorylation, including ACC and RAPTOR. Phosphorylation of ACC suppresses lipogenesis and supports fatty acid oxidation, whereas phosphorylation of RAPTOR suppresses mTORC1 signaling and links cellular energy status to growth and protein synthesis control. The pathway is linked
순도&문서
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Data Sheet (278 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Kim E, et al. Protein Arginine Methyltransferase 1 (PRMT1) Selective Inhibitor, TC-E 5003, Has Anti-Inflammatory Properties in TLR4 Signaling. Int J Mol Sci. 2020;21(9):3058. Published 2020 Apr 26. [Content Brief]
[2]. Park MJ, et al. TC-E 5003, a protein methyltransferase 1 inhibitor, activates the PKA-dependent thermogenic pathway in primary murine and human subcutaneous adipocytes. FEBS Lett. 2020 Sep;594(17):2923-2930. [Content Brief]
[3]. Zhang P, et al. Developing protein arginine methyltransferase 1 (PRMT1) inhibitor TC-E-5003 as an antitumor drug using INEI drug delivery systems. Drug Deliv. 2020 Dec;27(1):491-501. [Content Brief]
[4]. Shen NY, et al. Protein arginine methyltransferase expression and activity during myogenesis. Biosci Rep. 2018 Jan 10;38(1):BSR20171533. [Content Brief]
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 | 2.4921 mL | 12.4607 mL | 24.9215 mL | 62.3037 mL |
| 5 mM | 0.4984 mL | 2.4921 mL | 4.9843 mL | 12.4607 mL | |
| 10 mM | 0.2492 mL | 1.2461 mL | 2.4921 mL | 6.2304 mL | |
| 15 mM | 0.1661 mL | 0.8307 mL | 1.6614 mL | 4.1536 mL | |
| 20 mM | 0.1246 mL | 0.6230 mL | 1.2461 mL | 3.1152 mL | |
| 25 mM | 0.0997 mL | 0.4984 mL | 0.9969 mL | 2.4921 mL | |
| 30 mM | 0.0831 mL | 0.4154 mL | 0.8307 mL | 2.0768 mL | |
| 40 mM | 0.0623 mL | 0.3115 mL | 0.6230 mL | 1.5576 mL | |
| 50 mM | 0.0498 mL | 0.2492 mL | 0.4984 mL | 1.2461 mL | |
| 60 mM | 0.0415 mL | 0.2077 mL | 0.4154 mL | 1.0384 mL | |
| 80 mM | 0.0312 mL | 0.1558 mL | 0.3115 mL | 0.7788 mL | |
| 100 mM | 0.0249 mL | 0.1246 mL | 0.2492 mL | 0.6230 mL |
TC-E 5003 Related Classifications
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