SH5-07

SKU: orb1296242

Description

SH5-07 is a hydroxamic acid derivative that potently inhibits Stat3 signaling with an IC50 of 3.9 µM. This small molecule is a valuable research tool for studying Stat3-dependent pathways in cancer and inflammation, applicable in both cellular and biochemical assays.

Research Area

Signal Transduction, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 1456632-41-9
• MW: 625.61
• Purity: 95.54% (May vary between batches)
• Formula: C₂₉H₂₈F₅N₃O₅S
• SMILES: CN(CC(=O)N(Cc1ccc(cc1)C1CCCCC1)c1ccc(cc1)C(=O)NO)S(=O)(=O)c1c(F)c(F)c(F)c(F)c1F
• Target: STAT
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (3.2 mM);H2O:Insoluble;DMSO:50 mg/mL (79.92 mM)

Bioactivity

• Target IC50:
  STAT3:3.9 μM (cell free)
• 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 with aberrantly-active Stat3, associated with decreased Mcl-1, c-Myc, and Cyclin D1 expression. No significant changes in body weights, blood cell counts, organ gross anatomy, or signs of toxicity are observed.
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• 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.
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• 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.
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• 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.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Inhibitor, inhibit, SH5-07, SH5 07, SH507, SH-5-07, STAT3, STAT

Compound Identifiers

PubChem CID

72550504