GLPBio

SH-4-54

Catalog No.: GC14658Purity:>99.50%
COASDSData Sheet
SH-4-54 ist ein STAT-Inhibitor, der an STAT3 und STAT5 mit KDs von 300 bzw. 464 nM bindet.

Die Produkte sind ausschließlich für Forschungszwecke bestimmt. Nicht zur Anwendung am Menschen. Wir verkaufen nicht an Patienten.

SH-4-54
Cas No.: 1456632-40-8
10mM (in 1mL DMSO)In Stock
$131.00
1
5mgIn Stock
$90.00
1
25mgIn Stock
$242.00
1
100mgIn Stock
$488.00
1
Tel: (909) 407-4943 / (909) 689-7124Email: sales@glpbio.com

Zitate (Citations)

Für dieses Produkt sind derzeit keine Zitate verfügbar. Nachfolgend finden Sie ausgewählte Publikationen, die GlpBio-Produkte zitieren.
  • Nature cover
    Nature
    641, 529–536 (2025)
  • Nature cover
    Nature
    628, 630–638 (2024)
  • Nature cover
    Nature
    632, 686–694 (2024)
  • Nature cover
    Nature
    618, 1017–1023 (2023)
  • Nature cover
    Nature
    610, 366–372 (2022)
  • Cell cover
    Cell
    187(9):2288-2304 (2024)
  • Cell cover
    Cell
    183(7):1867-1883 (2020)
  • Science cover
    Science
    388(6745) (2025)
  • Science cover
    Science
    387(6739) (2025)
  • Science cover
    Science
    387(6734) (2025)
  • Cell Research cover
    Cell Research
    35, 97–116 (2025)
  • Cell Research cover
    Cell Research
    34, 683–706 (2024)
  • Cell Research cover
    Cell Research
    33, 273–287 (2023)
  • Cell Research cover
    Cell Research
    33, 546–561 (2023)
  • Cell Research cover
    Cell Research
    33, 904–922 (2023)
  • Cell Research cover
    Cell Research
    31, 1291–1307 (2021)

Beschreibung (Description)

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.

Protokoll (Protocol)

Cell experiment [1]:

Cell lines

U251MG; U87MG

Preparation Method

Cells were cultured in Roswell Park Memorial Institute medium-1640 supplemented with 1% nonessential amino acids and 10% heat-inactivated fetal bovine serum. Cells in 96-well plates were treated with either SH-4-54 or a vehicle control for 72 hours, after which they were subjected to a CyQuant cell proliferation assay. Alternatively, cells were harvested, and viable cells were counted using trypan blue exclusion and phase contrast microscopy.

Reaction Conditions

0-10 μM ; 72 hours

Applications

SH-4-54 exhibits potent cytotoxic effects against malignant cells harboring aberrantly active Stat3.

Animal experiment [2]:

Animal models

NOD-SCID mice (Glioma model)

Preparation Method

NOD-SCID mice were orthotopically xenografted with 105 BT73 glioma cells. Starting on day 7, the mice received intraperitoneal injections of 10 mg/kg of SH-4-54 or vehicle control on a schedule of 4 days on followed by 3 days off. Animals were sacrificed 2 hours after the last dose, and brain tumors were extracted for immunohistochemical analysis of pSTAT3, Ki67 (proliferation), and TUNEL (apoptosis).

Dosage form

10 mg/kg; 4 days on/3 days off; i.p.

Applications

SH-4-54 reduced pSTAT3 expression in tumor cells and decreased proliferation while increasing apoptosis in treated tumors.

References:
[1]. 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.
[2]. 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.

Produktdokumente (Product Documents)

Purity:>99.50%Appearance:A solid
COASDSData Sheet

Chemische Eigenschaften (Chemical Properties)

CAS-Nr.
1456632-40-8
SMILES
FC(C(S(=O)(N(C)CC(N(C1=CC=C(C(O)=O)C=C1)CC2=CC=C(C=C2)C3CCCCC3)=O)=O)=C(C(F)=C4F)F)=C4F
Summenformel
C29H27F5N2O5S 
Molekulargewicht
610.59
Löslichkeit
≥ 20.25mg/mL in DMSO
Lagerung
Desiccate at -20°C
Allgemeine Hinweise
Wählen Sie anhand der Löslichkeitsdaten des Produkts ein geeignetes Lösungsmittel. Aliquotieren Sie die Stammlösung nach der Herstellung, um wiederholte Gefrier-Auftau-Zyklen zu vermeiden.
Verwenden Sie Stammlösungen bei Lagerung bei -80°C innerhalb von 6 Monaten bzw. bei -20°C innerhalb von 1 Monat.
Zur Verbesserung der Löslichkeit das Röhrchen auf 37°C erwärmen und für eine angemessene Dauer beschallen.
Versandbedingungen
Evaluierungsmuster werden mit Kühlakkus versandt. Andere verfügbare Größen werden bei Raumtemperatur oder auf Anfrage mit Kühlakkus versandt.

Rechner (Calculators)Molarität / Verdünnung / Molekulargewicht / Einheitenumrechnung / In-vivo-Formulierung / Löslichkeit

g/mol

Reviews

Review for SH-4-54

Rating: 5
  • 5 Star100%
  • 4 Star0%
  • 3 Star0%
  • 2 Star0%
  • 1 Star0%