TC-E 5003

Catalog No.S0855 Batch:S085501

Technical Data

Formula	C₁₆H₁₄Cl₂N₂O₄S
Molecular Weight	401.26	CAS No.	17328-16-4
Solubility (25°C)*	In vitro	DMSO	80 mg/mL (199.37 mM)
		Water	Insoluble
		Ethanol	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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

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]

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]

Protocol (from reference)

Cell Assay:^{^[2]}	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.
Animal Study:^{^[3]}	Animal Models Nude/ICR mice model implanted with A549 cell xenografts Dosages 0.5, 1.0, 2.0 mg Administration s.c.

Cell Assay:^{^[2]}

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.

Animal Study:^{^[3]}

Animal Models
Nude/ICR mice model implanted with A549 cell xenografts
Dosages
0.5, 1.0, 2.0 mg
Administration
s.c.

References

Selleck's TC-E 5003 has been cited by 2 publications

Targeting PRMT1 prevents acute and chronic graft-versus-host disease [ Mol Ther, 2023, 10.1016/j.ymthe.2023.09.011]	PubMed: 37735873
PRMT1 reverts the immune escape of necroptotic colon cancer through RIP3 methylation [ Cell Death Dis, 2023, 14(4):233]	PubMed: 37005412

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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