| Size | Price | Stock | Qty |
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| 100mg |
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| 250mg |
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| 500mg | |||
| 1g | |||
| Other Sizes |
| Targets |
TC-E 5003 targets protein arginine methyltransferase 1 (PRMT1), an enzyme that catalyzes the methylation of arginine residues in proteins. PRMT1 is the major type I protein arginine methyltransferase and is involved in various cellular processes including transcription regulation, signal transduction, and DNA repair. By inhibiting PRMT1, TC-E 5003 modulates arginine methylation and downstream signaling pathways.
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| ln Vitro |
In vitro, TC-E 5003 is a selective PRMT1 inhibitor with an IC50 of 1.5 μM. It displays no activity against CARM1 and Set7/9 methyltransferases. The compound has anti-inflammatory properties in TLR4 signaling and inhibits the growth of MCF7 breast cancer cells and LNCaP prostate cancer cells.
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| ln Vivo |
In vivo, TC-E 5003 has been studied for its anti-inflammatory properties in TLR4 signaling. By inhibiting PRMT1, the compound may modulate inflammatory responses and has potential applications in cancer research. Its anti-inflammatory effects have been demonstrated in experimental settings, suggesting potential for the study of inflammatory diseases.
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| Enzyme Assay |
In vitro enzyme assays for TC-E 5003 measure its inhibition of PRMT1 activity. The enzyme is incubated with its substrate and the methyl donor S-adenosylmethionine in the presence of varying concentrations of the compound. Methylation of the substrate is measured by radioactive or fluorescence-based methods. The IC50 of 1.5 μM is determined from dose-response curves.
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| Cell Assay |
In vitro cell-based assays for TC-E 5003 use cancer cell lines such as MCF7 breast cancer cells and LNCaP prostate cancer cells. Cells are treated with serial dilutions of the compound, and cell viability is measured using MTT or other assays. PRMT1 inhibition is assessed by measuring protein arginine methylation levels by Western blotting. Anti-inflammatory activity is assessed in TLR4 signaling assays.
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| Animal Protocol |
In vivo animal models for TC-E 5003 include models of inflammation and cancer. The compound is administered via appropriate routes, and its effects on inflammatory markers, tumor growth, and survival are evaluated. Pharmacodynamic studies measure PRMT1 inhibition and arginine methylation levels in target tissues.
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| ADME/Pharmacokinetics |
TC-E 5003 has a molecular weight of 401.26 g/mol and a molecular formula of C16H14Cl2N2O4S. It is insoluble in ethanol and water, but soluble in DMSO at ≥49 mg/mL. The compound is stored at +4°C and has a purity of ≥98%. It is also known as N,N'-(Sulfonyldi-4,1-phenylene)bis(2-chloroacetamide).
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| Toxicity/Toxicokinetics |
The toxicity profile of TC-E 5003 is characterized in preclinical safety studies. As a PRMT1 inhibitor, the compound may affect protein methylation-dependent processes. The compound is for research use only and is not approved for clinical use. Appropriate safety precautions should be taken during handling.
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| References |
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| Additional Infomation |
TC-E 5003 is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 of 1.5 μM. It displays no activity against CARM1 and Set7/9 methyltransferases. The compound has anti-inflammatory properties in TLR4 signaling and inhibits the growth of MCF7 breast cancer cells and LNCaP prostate cancer cells. TC-E 5003 is also known as NSC-30176 and is intended for laboratory research use only.
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| Molecular Formula |
C16H14CL2N2O4S
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|---|---|
| Molecular Weight |
401.25
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| Exact Mass |
400.005
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| CAS # |
17328-16-4
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| PubChem CID |
87052
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| Appearance |
Off-white to light brown solid powder
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| Density |
1.504g/cm3
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| Boiling Point |
704.2ºC at 760 mmHg
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| Flash Point |
379.7ºC
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| Vapour Pressure |
1.12E-19mmHg at 25°C
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| Index of Refraction |
1.639
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| LogP |
4.1
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
25
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| Complexity |
519
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
SHRCVZJKZJGIHQ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H14Cl2N2O4S/c17-9-15(21)19-11-1-5-13(6-2-11)25(23,24)14-7-3-12(4-8-14)20-16(22)10-18/h1-8H,9-10H2,(H,19,21)(H,20,22)
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| Chemical Name |
2-chloro-N-[4-[4-[(2-chloroacetyl)amino]phenyl]sulfonylphenyl]acetamide
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| Synonyms |
TCE 5003 TC E 5003 TC-E 5003
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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) |
DMSO : ~125 mg/mL (~311.52 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.18 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (5.18 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (5.18 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4922 mL | 12.4611 mL | 24.9221 mL | |
| 5 mM | 0.4984 mL | 2.4922 mL | 4.9844 mL | |
| 10 mM | 0.2492 mL | 1.2461 mL | 2.4922 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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