2. Epigenetics Immunology/Inflammation NF-κB Stem Cell/Wnt TGF-beta/Smad
  3. Histone Methyltransferase AP-1 NF-κB PKA
  4. TC-E 5003

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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TC-E 5003 Chemical Structure

TC-E 5003 Chemical Structure

CAS No. : 17328-16-4

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Based on 1 publication(s) in Google Scholar

TC-E 5003 Related Antibodies

Top Publications Citing Use of Products

View All Histone Methyltransferase Isoform Specific Products:

View All Isoforms
EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

View All AP-1 Isoform Specific Products:

View All Isoforms
c-Fos c-Jun

View All NF-κB Isoform Specific Products:

View All Isoforms
NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

View All PKA Isoform Specific Products:

View All Isoforms
PKA PKAR

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1][2][3][4].

IC50 & Target

PRMT1

 

Cellular Effect
Cell Line Type Value Description References
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]
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.

TC-E 5003 Related Antibodies

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.
Molecular Weight

401.26

Formula

C16H14Cl2N2O4S
CAS No.
Appearance

Solid

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4921 mL 12.4607 mL 24.9215 mL
5 mM 0.4984 mL 2.4921 mL 4.9843 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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.

  • 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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • 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.

    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:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation
References

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
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TC-E 5003 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

TC-E 500317328-16-4Histone MethyltransferaseAP-1NF-κBPKAActivator Protein 1Nuclear factor-κBNuclear factor-kappaBProtein kinase APRMT1anti-inflammatory propertiesUcp1Fgf21obesity and associated metabolic disordersoxidative stressinflammationcancersInhibitorinhibitorinhibit

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