Home Metabolism PRMT inhibitor - AP-1 modulator TC-E 5003 For research use only.

TC-E 5003

Synonyms: NSC 30176

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

TC-E 5003 Chemical Structure

TC-E 5003 Chemical Structure

CAS No. 17328-16-4

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TC-E 5003 Related Products

Biological Activity

Description TC-E 5003 (NSC 30176, Compound 2e) is a selective inhibitor of protein arginine methyltransferase 1 (PRMT1) with IC50 of 1.5 μM. TC-E 5003 modulates the lipopolysaccharide (LPS)-induced AP-1 and NF-κB signaling pathways and can possibly be further developed as an anti-inflammatory compound.
Targets
AP-1 [1] PRMT1 [1]
(Cell-free assay)
1.5 μM
In vitro
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.[2]
Cell Research Cell lines RAW264.7 cells
Concentrations 0.5, 1 µM
Incubation Time 6 h
Method

The total cell lysates or nuclear fraction were prepared from RAW264.7 cells under the indicated conditions. The protein samples were separated by sodium dodecyl sulfate-polyacrylamide gel electrophoresis, and immunoblotting was performed with specific antibodie. The nuclear fractions were analyzed with antibodies against the phosphorylated or total forms of c-Jun, p65, p50, and Lamin A/C. With whole cell lysates, the protein levels were examined with antibodies against the phosphorylated or total forms of c-Jun, ERK, JNK, p38, IκBα, Src, Syk, PRMT1, HA, and β-actin. The band intensity in each blot was measured and quantified using image J.
In Vivo
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).[3]
Animal Research Animal Models Nude/ICR mice model implanted with A549 cell xenografts
Dosages 0.5, 1.0, 2.0 mg
Administration s.c.

Chemical Information & Solubility

Molecular Weight 401.26 Formula

C16H14Cl2N2O4S
CAS No. 17328-16-4 SDF --
Smiles ClCC(=O)NC1=CC=C(C=C1)[S](=O)(=O)C2=CC=C(NC(=O)CCl)C=C2
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 80 mg/mL ( (199.37 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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