Art. -Nr.: HY-107574

TC-E 5003

4 Cited Publications

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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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Reinheit: 98.06%
CAS. Nr.: 17328-16-4
Formel: C₁₆H₁₄Cl₂N₂O₄S
Molecular Weight:401.26

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

TC-E 5003 Chemical Structure

CAS. Nr.: 17328-16-4

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (4)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

PRMT1

Alle Histone Methyltransferase Isoform-spezifische Produkte anzeigen :

Alle AP-1 Isoform-spezifische Produkte anzeigen :

Alle NF-κB Isoform-spezifische Produkte anzeigen :

Alle PKA Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	GI₅₀	0.702 μM Compound: 44; Te-C-5003	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	[PMID: 36528996]
LNCaP	GI₅₀	4.49 μM Compound: 2e	Growth inhibition of human LNCAP cells by MTS assay Growth inhibition of human LNCAP cells by MTS assay	[PMID: 21440447]
MCF7	GI₅₀	0.413 μM Compound: 44; Te-C-5003	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	[PMID: 36528996]
MDA-MB-231	GI₅₀	0.597 μM Compound: 44; Te-C-5003	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	[PMID: 36528996]
NCI-H1299	GI₅₀	0.684 μM Compound: 44; Te-C-5003	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	[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.

Real Time qPCR^[1]

Cell Line:

RAW264.7 cells
Concentration:

0-1 μM
Incubation Time:

24 h
Result:

Significantly and dose-dependently decreased NO production without cytotoxicity in RAW264.7 cells.

Western Blot Analysis^[1]

Cell Line:

RAW264.7 cells
Concentration:

1 μM
Incubation Time:

15-60 min
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.

Real Time qPCR^[2]

Cell Line:

Primary iWAT cells
Concentration:

10 μM
Incubation Time:

4 h
Result:

Led significant increase in Ucp1 mRNA and protein expressions up to 24 h in primary iWAT cells.

Cell Viability Assay^[3]

Cell Line:

A549, A549-INEI, H1299, MCF-7, and MDAMB-231 cells
Concentration:

6 μM
Incubation Time:

48 h
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

TC-E 5003 (0.5-2.0 mg, s.c., a single dose for 28 days) has an excellent tumor-suppressing effect in A549 tumor xenograft ICR mouse models ^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

A549 tumor xenograft ICR mouse model^[3]
Dosage:

0.5-2.0 mg
Administration:

s.c., a single dose for 28 days
Result:

Achieved better antitumor effect in combination with INEI system in A549 tumor xenograft ICR mouse model.

Chemical Information

CAS. Nr. 17328-16-4
Appearance Solid
Molecular Weight 401.26
Formel C₁₆H₁₄Cl₂N₂O₄S
Color Off-white to light brown
SMILES

O=S(C1=CC=C(NC(CCl)=O)C=C1)(C2=CC=C(NC(CCl)=O)C=C2)=O
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

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
Sports Med Health Sci

2025 Apr 4.
bioRxiv

2026 May 29.

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.4921 mL

12.4607 mL

24.9215 mL

5 mM

0.4984 mL

2.4921 mL

4.9843 mL

10 mM

0.2492 mL

1.2461 mL

2.4921 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (5.18 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

TC-E 5003

4 Cited Publications

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TC-E 5003

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Publications Citing Use of MedChemExpress (MCE) TC-E 5003

Alle Histone Methyltransferase Isoform-spezifische Produkte anzeigen

Alle AP-1 Isoform-spezifische Produkte anzeigen

Alle NF-κB Isoform-spezifische Produkte anzeigen

Alle PKA Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (4)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

TC-E 5003 Related Classifications

HY-107574 Related Classifications