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TC-E 5003 PRMT inhibitor

Name: TC-E 5003
Brand: Selleck Chemicals
SKU: S0855
Availability: InStock
Rating: 5 (4 reviews)

Cat.No.S0855

TC-E 5003 (NSC 30176, Compound 2e) is a selective inhibitor of protein arginine methyltransferase 1 (PRMT1) with IC50 of 1.5 μM. This compound modulates the lipopolysaccharide (LPS)-induced AP-1 and NF-κB signaling pathways and can possibly be further developed as an anti-inflammatory compound.

Chemical Structure

Molecular Weight: 401.26

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Quality Control

Batch: Purity: 99.56%

99.56

Related Targets	Dehydrogenase HSP Transferase P450 (e.g. CYP17) PDE phosphatase PPAR Vitamin Carbohydrate Metabolism Mitochondrial Metabolism
Other PRMT Inhibitors	LLY-283 GSK3326595 (Pemrametostat, EPZ015938) C7280948 GSK3368715 3HCl BRD0639 Furamidine dihydrochloride LLY-284 TNG-462 AMG 193 MS023 hydrochloride

Solubility

In vitro
Batch:

DMSO : 80 mg/mL (199.37 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	4mg/ml (9.97mM)	Taking the 1 mL working solution as an example, add 50 μL of 80 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.57mg/ml (1.42mM)	Taking the 1 mL working solution as an example, add 50 μL of 11.4 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	401.26	Formula	C₁₆H₁₄Cl₂N₂O₄S	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	17328-16-4	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	NSC 30176			Smiles	ClCC(=O)NC1=CC=C(C=C1)[S](=O)(=O)C2=CC=C(NC(=O)CCl)C=C2

Mechanism of Action

Targets/IC₅₀/Ki	AP-1 PRMT1 (Cell-free assay) 1.5 μM
In vitro	TC-E 5300 regulates inflammatory responses by inhibiting the c-Jun expression and NF-κB signal transduction, which inhibits the expression of various inflammatory genes by downregulating these transcriptional factors.
In vivo	TE-C-5003, a selective protein arginine methyltransferase 1 (PRMT1) inhibitor with good anti-tumor effect on lung cancer, exerts better anti-tumor effect when loaded with injectable NBCA ethyl oleate implant (INEI).
References	[1] https://pubmed.ncbi.nlm.nih.gov/21440447/ [2] https://pubmed.ncbi.nlm.nih.gov/32357521/ [3] https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7170320/

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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