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Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $51 | In Stock | |
2 mg | $74 | In Stock | |
5 mg | $122 | In Stock | |
10 mg | $198 | In Stock | |
25 mg | $347 | In Stock | |
50 mg | $515 | In Stock | |
100 mg | $747 | In Stock | |
1 mL x 10 mM (in DMSO) | $169 | In Stock |
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 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. |
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 | Shipping with blue ice. | ||||||||||||||||||||||||||||||
Solubility Information | DMSO: 50 mg/mL (79.92 mM), Sonication is recommended. H2O: Insoluble | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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