SH-4-54 |
| Catalog No.GC14658 |
SH-4-54 is a specific STAT3 inhibitor with a KD of 300 nM. It is commonly used in the study of treatments for brain cancers such as glioblastoma.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1456632-40-8
Sample solution is provided at 25 µL, 10mM.
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SH-4-54 is a specific STAT3 inhibitor with a KD of 300 nM[1]. It is commonly used in the study of treatments for brain cancers such as glioblastoma[2-3].
SH-4-54 demonstrates potent cytotoxic effects on tumor cells with aberrantly active STAT3, exhibiting an IC50 range of 1.0-2.7μM for glioma U251MG and U87MG cells[3]. SH-4-54 (16μM; 72h) effectively induces apoptosis in temozolomide-resistant glioblastoma multiforme cells by mitoSTAT3 pathway, leading to disrupted oxidative phosphorylation and negative regulation of mitochondrial-encoded genes[4]. In addition, SH-4-54 reduces cell survival and phosphorylated STAT3 levels in various tumors, including bladder cancer and pancreatic cancer[5-6].
SH-4-54 (6 mg/kg; every 2 or 3 days; intravenous administration) effectively blocked the DNA binding activity of STAT3, leading to the inhibition of STAT3-dependent gene transcription in human glioma, breast, and prostate cancer cells, as well as in v-Src-transformed murine fibroblasts. And effectively suppressed tumor growth in mouse xenograft models of glioma and breast cancer [3].
References:
[1]. Haftchenary S, Luchman HA, Jouk AO, et al. Potent Targeting of the STAT3 Protein in Brain Cancer Stem Cells: A Promising Route for Treating Glioblastoma. ACS Med Chem Lett. 2013 Sep 8;4(11):1102-7.
[2]. Yu D, Wang S, Wang J, et al. EZH2-STAT3 signaling pathway regulates GSDMD-mediated pyroptosis in glioblastoma. Cell Death Discov. 2024 Jul 28;10(1):341.
[3]. Yue P, Lopez-Tapia F, Paladino D, et al. Hydroxamic Acid and Benzoic Acid-Based STAT3 Inhibitors Suppress Human Glioma and Breast Cancer Phenotypes In Vitro and In Vivo. Cancer Res. 2016 Feb 1;76(3):652-63.
[4]. Cui P, Wei F, Hou J, et al. STAT3 inhibition induced temozolomide-resistant glioblastoma apoptosis via triggering mitochondrial STAT3 translocation and respiratory chain dysfunction. Cell Signal. 2020 Jul;71:109598.
[5]. Hindupur SV, Schmid SC, Koch JA, et al. STAT3/5 Inhibitors Suppress Proliferation in Bladder Cancer and Enhance Oncolytic Adenovirus Therapy. Int J Mol Sci. 2020 Feb 7;21(3):1106.
[6]. Arpin CC, Mac S, Jiang Y, et al. Applying Small Molecule Signal Transducer and Activator of Transcription-3 (STAT3) Protein Inhibitors as Pancreatic Cancer Therapeutics. Mol Cancer Ther. 2016 May;15(5):794-805.
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