TC-E 5003

製品コードS0855 バッチS085501

印刷

化学情報

Synonyms

NSC 30176

Storage
(From the date of receipt)

3 years -20°C powder

化学式

C₁₆H₁₄Cl₂N₂O₄S

分子量

401.26

CAS No.

17328-16-4

Solubility (25°C)*

体外

DMSO

80 mg/mL (199.37 mM)

Water

Insoluble

Ethanol

Insoluble

体内（毎回新しく調製した物を用意してください）

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.

* <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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	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.
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]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	RAW264.7 cells
	濃度	0.5, 1 µM
	反応時間	6 h
	実験の流れ	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.
動物実験	動物モデル	Nude/ICR mice model implanted with A549 cell xenografts
	投薬量	0.5, 1.0, 2.0 mg
	投与方法	s.c.

参考

https://pubmed.ncbi.nlm.nih.gov/21440447/
https://pubmed.ncbi.nlm.nih.gov/32357521/
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7170320/

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Prmt1-mediated methylation regulates Ncoa4 stability to transactivate Adamts genes and promote bone extracellular matrix degradation in chronic hematogenous osteomyelitis [ Biol Direct, 2025, 20(1):60]	PubMed: 40346625
PRMT1-mediated modification of H4R3me2a promotes liver cancer progression by enhancing the transcriptional activity of SOX18 [ Hepatol Commun, 2025, 9(4)e0647]	PubMed: 40130992
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

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。