SH-4-54
Based on 16 publication(s) in Google Scholar
SH-4-54 is a CNS-penetrant STAT inhibitor that binds to STAT3 and STAT5 with KDs of 300, 464 nM, respectively.
For research use only. We do not sell to patients.
- Purity: 99.80%
- CAS No.: 1456632-40-8
- Formula: C29H27F5N2O5S
- Molecular Weight:610.59
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) SH-4-54
More- Signal Transduct Target Ther. 2025 Dec 24;10(1):417. [Abstract]
- Environ Pollut. 2025 Feb 4:368:125791. [Abstract]
- Oncogene. 2020 Sep;39(39):6203-6217. [Abstract]
- Cell Death Discov. 2024 Jul 28;10(1):341. [Abstract]
- Cell Rep. 2020 Sep 15;32(11):108158. [Abstract]
- Oncogenesis. 2025 Apr 22;14(1):12. [Abstract]
- Prog Neurobiol. 2021 Jun:201:102028. [Abstract]
- Front Immunol. 2021 Apr 1:12:584097. [Abstract]
- CNS Neurosci Ther. 2023 Aug;29(8):2129-2144. [Abstract]
- Int J Mol Sci. 2022 Apr 12;23(8):4277. [Abstract]
- J Pharm Pharm Sci. 2021:24:1-15. [Abstract]
- Exp Cell Res. 2021 Jan 1;398(1):112371. [Abstract]
- J Steroid Biochem Mol Biol. 2026 May:259:106953. [Abstract]
- Biomed Res Int. 2020 Jan 23;2020:9204708. [Abstract]
- Biochem Biophys Res Commun. 2017 Mar 4;484(2):311-317. [Abstract]
- Hematology. 2023 Dec;28(1):2224625. [Abstract]
Customer Validation & Images
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In Vivo Efficacy Study
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WB
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WB
Biological Activity
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STAT3 300 nM (Kd) |
STAT5 464 nM (Kd) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| AGS | IC50 |
5.42 μM
Compound: 4; SH4-54
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Antiproliferative activity against human AGS cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human AGS cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
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[PMID: 36170649] |
| H9c2 | IC50 |
10.2 μM
Compound: 4; SH4-54
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Antiproliferative activity against human H9c2 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human H9c2 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
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[PMID: 36170649] |
| MGC-803 | IC50 |
8.51 μM
Compound: 4; SH4-54
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Antiproliferative activity against human MGC-803 cells assessed as reduction in cell viability measured after 72 hrs by CCK-8 assay
Antiproliferative activity against human MGC-803 cells assessed as reduction in cell viability measured after 72 hrs by CCK-8 assay
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[PMID: 36170649] |
SH-4-54 potently kills glioblastoma brain cancer stem cells (BTSCs) and effectively suppresses STAT3 phosphorylation and its downstream transcriptional targets at low nM concentrations.SH-4-54 shows unprecedented cytotoxicity in human BTSCs, displays no toxicity in human fetal astrocytes, potently suppresses pSTAT3 with nanomolar IC50s, inhibiting STAT3's downstream targets, and shows no discernible off-target effects at therapeutic doses[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1456632-40-8
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Appearance Solid
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Molecular Weight 610.59
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Formula C29H27F5N2O5S
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Color White to off-white
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SMILES
O=C(O)C1=CC=C(N(CC2=CC=C(C3CCCCC3)C=C2)C(CN(C)S(=O)(C4=C(F)C(F)=C(F)C(F)=C4F)=O)=O)C=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (16)
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Journal Impact Factor
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Most Recent
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Signal Transduct Target Ther
Lipocalin-2 drives brain metastatic progression through reciprocal tumor-microenvironment interactions in lung cancer. [Abstract]2025 Dec 24;10(1):417. PMID: 41436606
SH-4-54 purchased from MedChemExpress. Usage Cited in: Signal Transduct Target Ther. 2025 Dec 24;10(1):417. [Abstract]
Treatment of PC9-BM LCN2-high BM-bearing mice with SH4-54 (10 mg/kg, intraperitoneally, twice per week), Bevacizumab (10mg/kg, intraperitoneally, twice per week), or a combination of both significantly suppressed tumor progression and prolonged overall survival.
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Environ Pollut
2025 Feb 4:368:125791. PMID: 39914566 -
Oncogene
ApoC1 promotes the metastasis of clear cell renal cell carcinoma via activation of STAT3. [Abstract]2020 Sep;39(39):6203-6217. PMID: 32826950 -
Cell Death Discov
2024 Jul 28;10(1):341. PMID: 39069522 -
Cell Rep
The Natural Compound Notopterol Binds and Targets JAK2/3 to Ameliorate Inflammation and Arthritis. [Abstract]2020 Sep 15;32(11):108158. PMID: 32937124 -
Oncogenesis
EPHA5 promotes cell proliferation and inhibits apoptosis in Follicular Thyroid Cancer via the STAT3 signaling pathway. [Abstract]2025 Apr 22;14(1):12. PMID: 40263257 -
Prog Neurobiol
DNMT3L promotes neural differentiation by enhancing STAT1 and STAT3 phosphorylation independent of DNA methylation. [Abstract]2021 Jun:201:102028. PMID: 33636226 -
Front Immunol
2021 Apr 1:12:584097. PMID: 33868221 -
CNS Neurosci Ther
Regulatory T cells promote functional recovery after spinal cord injury by alleviating microglia inflammation via STAT3 inhibition. [Abstract]2023 Aug;29(8):2129-2144. PMID: 36914969
SH-4-54 purchased from MedChemExpress. Usage Cited in: CNS Neurosci Ther. 2023 Aug;29(8):2129-2144. [Abstract]
SH-4-54 effectively blocks OGD/R-induced STAT3 phosphorylation in microglia.
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Int J Mol Sci
2022 Apr 12;23(8):4277. PMID: 35457095 -
J Pharm Pharm Sci
Growth Hormone Signaling Pathway Leading to the Induction of DNA Synthesis and Proliferation in Primary Cultured Hepatocytes of Adult Rats. [Abstract]2021:24:1-15. PMID: 33434118 -
Exp Cell Res
Inactivated STAT5 pathway underlies a novel inhibitory role of EBF1 in chronic lymphocytic leukemia. [Abstract]2021 Jan 1;398(1):112371. PMID: 33188849 -
J Steroid Biochem Mol Biol
Interleukin-2 receptor γ blocks the development of Leydig cells from stem/progenitor cells in male rats via JAK1-STAT3 pathway and GSDMD-mediated pyroptosis. [Abstract]2026 May:259:106953. PMID: 41662993 -
Biomed Res Int
Chronic Hypoxia-Induced Microvessel Proliferation and Basal Membrane Degradation in the Bone Marrow of Rats Regulated through the IL-6/JAK2/STAT3/MMP-9 Pathway. [Abstract]2020 Jan 23;2020:9204708. PMID: 32047820 -
Biochem Biophys Res Commun
TNF-α-inducing protein of Helicobacter pylori induces epithelial-mesenchymal transition (EMT) in gastric cancer cells through activation of IL-6/STAT3 signaling pathway. [Abstract]2017 Mar 4;484(2):311-317. PMID: 28130110
SH-4-54 purchased from MedChemExpress. Usage Cited in: Biochem Biophys Res Commun. 2017 Mar 4;484(2):311-317. [Abstract]
SGC7901 cells are pretreated with IL-6 neutralizing antibody or SH-4-54 for an hour prior to Tipα stimulation. STAT3 (Y705) phosphorylation is significantly inhibited by IL-6 antibody or SH-4-54 pretreatment.
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Hematology
Dual inhibition of STAT3 and STAT5 may overcome imatinib resistance in chronic myeloid leukemia. [Abstract]2023 Dec;28(1):2224625. PMID: 37345979
Solvent & Solubility
DMSO : 100 mg/mL (163.78 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.09 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (274 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.6378 mL | 8.1888 mL | 16.3776 mL | 40.9440 mL |
| 5 mM | 0.3276 mL | 1.6378 mL | 3.2755 mL | 8.1888 mL | |
| 10 mM | 0.1638 mL | 0.8189 mL | 1.6378 mL | 4.0944 mL | |
| 15 mM | 0.1092 mL | 0.5459 mL | 1.0918 mL | 2.7296 mL | |
| 20 mM | 0.0819 mL | 0.4094 mL | 0.8189 mL | 2.0472 mL | |
| 25 mM | 0.0655 mL | 0.3276 mL | 0.6551 mL | 1.6378 mL | |
| 30 mM | 0.0546 mL | 0.2730 mL | 0.5459 mL | 1.3648 mL | |
| 40 mM | 0.0409 mL | 0.2047 mL | 0.4094 mL | 1.0236 mL | |
| 50 mM | 0.0328 mL | 0.1638 mL | 0.3276 mL | 0.8189 mL | |
| 60 mM | 0.0273 mL | 0.1365 mL | 0.2730 mL | 0.6824 mL | |
| 80 mM | 0.0205 mL | 0.1024 mL | 0.2047 mL | 0.5118 mL | |
| 100 mM | 0.0164 mL | 0.0819 mL | 0.1638 mL | 0.4094 mL |
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