HJC0152

製品コードS8561 バッチS856101

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C15H13Cl2N3O4.HCl
分子量 406.65 CAS No. 1420290-99-8
Solubility (25°C)* 体外 DMSO 88 mg/mL (216.4 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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 HJC0152 is a signal transducer and activator of transcription 3 (STAT3) inhibitor with remarkably improved aqueous solubility.
in vitro HJC0152 inhibits STAT3 promoter activity in MDA-MB-231 cells in a dose-dependent manner. It has a comparable potency in downregulating STAT3 protein production and phosphorylation at the Tyr-705 site. HJC0152 induces cleaved caspase-3 and downregulated cyclin D1 in MDA-MB-231 cells, inhibits cell cycle progression and promotes apoptosis[1]. HJC0152 treatment efficiently suppresses HNSCC cell proliferation, arrests the cell cycle at the G0/G1 phase, induces apoptosis, and reduced cell invasion in both SCC25 and CAL27 cell lines. Moreover, HJC0152 inhibits nuclear translocation of phosphorylated STAT3 at Tyr705 and decreases VHL/β-catenin signaling activity via regulation of microRNA-21[2].
in vivo HJC0152 significantly suppresses MDA-MB-231 xenograft tumor growth in vivo (ip and po), indicating its great potential as efficacious and orally bioavailable therapeutics for human cancer. It has an improved oral bioavailability and an enhanced suppression of tumor growth in mice. HJC0152 does not show significant signs of toxicity at a dose of 75 mg/kg[1]. In SCC25-derived orthotopic mouse models, HJC0152 treatment significantly abrogates STAT3/β-catenin expression in vivo, which leading to a global decrease of tumor growth and invasion[2].

プロトコル(参考用のみ)

細胞アッセイ 細胞株 MDA-MB-231 breast cancer cells
濃度 1, 5, and 10 μM
反応時間 24 h
実験の流れ

The cells are treated with different doses of compound 11 for 24 h, and levels of total STAT3 and phosphorylated STAT3 at Tyr-705 are then examined by Western blot.
動物実験 動物モデル MDA-MB-231 xenograft model (nude mice)
投薬量 2.5 and 7.5 mg/kg
投与方法 i.p.

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：

Early Infiltration of Innate Immune Cells to the Liver Depletes HNF4α and Promotes Extrahepatic Carcinogenesis [ Cancer Discov, 2023, 13(7):1616-1635] PubMed: 36972357
High baseline tumor burden-associated macrophages promote an immunosuppressive microenvironment and reduce the efficacy of immune checkpoint inhibitors through the IGFBP2-STAT3-PD-L1 pathway [ Cancer Commun (Lond), 2023, 43(5):562-581] PubMed: 37031362
Nifuroxazide boosts the anticancer efficacy of palbociclib-induced senescence by dual inhibition of STAT3 and CDK2 in triple-negative breast cancer [ Cell Death Discov, 2023, 9(1):355] PubMed: 37752122
Nifuroxazide boosts the anticancer efficacy of palbociclib-induced senescence by dual inhibition of STAT3 and CDK2 in triple-negative breast cancer [ Cell Death Discov, 2023, 9(1):355] PubMed: 37752122
Human α-Defensin 51-9 and Human β-Defensin 2 Improve Metabolic Parameters and Gut Barrier Function in Mice Fed a Western-Style Diet [ Int J Mol Sci, 2023, 24(18)13878] PubMed: 37762180
Human α-Defensin 51-9 and Human β-Defensin 2 Improve Metabolic Parameters and Gut Barrier Function in Mice Fed a Western-Style Diet [ Int J Mol Sci, 2023, 24(18)13878] PubMed: 37762180
STAT3 inhibition enhances CDN-induced STING signaling and antitumor immunity [Pei J Cancer Lett, 2019, 10.1016/j.canlet.2019.02.029] PubMed: 30790684
hJC0152, a novel sTaT3 inhibitor with promising anti-tumor effect in gastric cancer [Jiang X Cancer Manag Res, 2018, 10:6857-6867] PubMed: 30588091

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。

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