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SH5-07

Catalog No. TQ0052   CAS 1456632-41-9

SH5-07 is a hydroxamic acid-based Stat3 inhibitor (IC50: 3.9 μM).

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
SH5-07 Chemical Structure
SH5-07, CAS 1456632-41-9
Pack Size Availability Price/USD Quantity
1 mg In stock $ 51.00
2 mg In stock $ 74.00
5 mg In stock $ 122.00
10 mg In stock $ 198.00
25 mg In stock $ 347.00
50 mg In stock $ 515.00
100 mg In stock $ 747.00
1 mL * 10 mM (in DMSO) In stock $ 169.00
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Purity: 95.54%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description SH5-07 is a hydroxamic acid-based Stat3 inhibitor (IC50: 3.9 μM).
Targets&IC50 STAT3:3.9 μM (cell free)
In vitro SH5-07, a hydroxamic acid analog of BP-1-102, selectively inhibits Stat3 activity in a dose-dependent manner (IC50: 3.9±0.6 μM in vitro), specifically targeting Stat3:Stat3 DNA-binding over Stat1:Stat3, with minimal impact on Stat1:Stat1. By binding to Stat3, it disrupts its interaction with growth factor receptors, thus inhibiting Stat3 phosphorylation. This inhibition leads to reduced expression of Stat3-regulated genes, including Bcl-xL, Bcl-2, c-Myc, Survivin, Cyclin D1, and Mcl-1, following a 24-hour exposure to 5 μM SH5-07, ultimately exerting antitumor effects against cells with constitutively active Stat3.
In vivo Tail vein injection or oral gavage delivery of SH5-07 inhibits the growth of 90-150 mm^3 established subcutaneous mouse xenografts of human glioma (U251MG) and breast (MDA-MB-231) tumors that harbor aberrantly-active Stat3, associated with decreased Mcl-1, c-Myc, and Cyclin D1 expression. No significant changes in body weights, blood cell counts, or the gross anatomy of organs, or obvious signs of toxicity are observed.
Cell Research Cells are treated with 0-8 μM agent for 24-48 h. For cell cycle profile analysis, cells are harvested and fixed with 70% ice-cold ethanol and stained with propidium iodide (PI). For apoptosis analysis, cells are collected and stained with FITC-Annexin V using the Apoptosis Detection Kit. Both the DNA content of cells and the Annexin V-positive cells are analyzed by the flow cytometer. Cell cycle phase distribution is analyzed using the Cell-Fit program. Data acquisition is gated to exclude cell doublets.
Animal Research Mice are injected subcutaneously in the left flank area with U251MG cells in 200 μL of PBS/Matrigel matrix, or MDA-MB-231 cells in 100 μL of PBS. Mice with tumors of 90-150 mm^3 (MDA-MB-231) or 150 mm^3 (U251MG) are grouped for identical mean tumor sizes, administered 3, 5 or 6 mg/kg SH5-07 via oral gavage daily or tail vein injection every 2 or 3 days, and monitored every 3-7 days. Tumor sizes are measured with calipers and converted to tumor volume.
Molecular Weight 625.61
Formula C29H28F5N3O5S
CAS No. 1456632-41-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 50 mg/mL (79.92 mM), Sonification is recommended.

H2O: Insoluble

TargetMolReferences and Literature

1. Yue P,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.

Related compound libraries

This product is contained In the following compound libraries:
Inhibitor Library Cancer Cell Differentiation Compound Library Reprogramming Compound Library Anti-Lung Cancer Compound Library Bioactive Compound Library Immuno-Oncology Compound Library Transcription Factor-Targeted Compound Library JAK-STAT Compound Library NO PAINS Compound Library Anti-Cancer Compound Library

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Keywords

SH5-07 1456632-41-9 JAK/STAT signaling Stem Cells STAT Inhibitor SH5 07 inhibit SH507 SH-5-07 inhibitor

 

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