Art. -Nr.: HY-16975

SH-4-54

19 Cited Publications

Kundenbewertung

Based on 19 publication(s) in Google Scholar

SH-4-54 is a CNS-penetrant STAT inhibitor that binds to STAT3 and STAT5 with K_Ds of 300, 464 nM, respectively.

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Reinheit: 99.80%
CAS. Nr.: 1456632-40-8
Formel: C₂₉H₂₇F₅N₂O₅S
Molecular Weight:610.59

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

SH-4-54 Chemical Structure

CAS. Nr.: 1456632-40-8

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (19)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

SH-4-54 is a CNS-penetrant STAT inhibitor that binds to STAT3 and STAT5 with K_Ds of 300, 464 nM, respectively^[1].

IC₅₀ & Target

STAT3

300 nM (Kd)

STAT5

464 nM (Kd)

Alle STAT Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
AGS	IC₅₀	5.42 μM Compound: 4; SH4-54	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	[PMID: 36170649]
H9c2	IC₅₀	10.2 μM Compound: 4; SH4-54	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	[PMID: 36170649]
MGC-803	IC₅₀	8.51 μM Compound: 4; SH4-54	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	[PMID: 36170649]

In Vitro

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.

In Vivo

SH-4-54 exhibits blood-brain barrier permeability potently controls glioma tumor growth, and inhibits pSTAT3 in vivo. SH-4-54 demonstrates the power of STAT3 inhibitors for the treatment of BTSCs and validates the therapeutic efficacy of a STAT3 inhibitor for GBM clinical application.SH-4-54 decreases pSTAT3 expression in tumor cells of treated mice. SH-4-54 appears to decrease proliferation and increase apoptosis of treated tumors^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS. Nr. 1456632-40-8
Appearance Solid
Molecular Weight 610.59
Formel C₂₉H₂₇F₅N₂O₅S
Color White to off-white
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
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (19)

All In Vivo Efficacy StudyWB

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Journal Impact Factor

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.
Cell Death Discov

EZH2-STAT3 signaling pathway regulates GSDMD-mediated pyroptosis in glioblastoma. [Abstract]

2024 Jul 28;10(1):341. PMID: 39069522
Oncogene

ApoC1 promotes the metastasis of clear cell renal cell carcinoma via activation of STAT3. [Abstract]

2020 Sep;39(39):6203-6217. PMID: 32826950
Phytother Res

(+)-Matairesinol, Derived From Olive Oil, Enhanced T-Cell Anti-Tumor Immune via JAK3-STAT1 Signal and Synergized With Anti-PD-1 Efficacy. [Abstract]

2026 Apr 27. PMID: 42037203
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
Environ Pollut

Aluminum promotes B1 cells to produce IL-10 and impairs adaptive immune system. [Abstract]

2025 Mar 1:368:125791. PMID: 39914566
Front Immunol

HMGB1 Promotes the Release of Sonic Hedgehog From Astrocytes. [Abstract]

2021 Apr 1:12:584097. PMID: 33868221
J Ethnopharmacol

"Shihu" promote T-cell immunity against breast cancer through bioactive constituent THMB enhancing JAK3-STAT1 signal. [Abstract]

2026 Oct 28:369:121888. PMID: 42202911
CNS Neurosci Ther

Hypoxia Upregulates RIPK1 via the HIF-1α-JAK-STAT Pathway Leading to Astrocyte Necroptosis to Promote Cavitation After Spinal Cord Injury. [Abstract]

2026 May;32(5):e70895. PMID: 42109032
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.
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
Int J Mol Sci

In Vitro Angiogenesis Inhibition and Endothelial Cell Growth and Morphology. [Abstract]

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
Prog Neurobiol

DNMT3L promotes neural differentiation by enhancing STAT1 and STAT3 phosphorylation independent of DNA methylation. [Abstract]

2021 Jun:201:102028. PMID: 33636226
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.
Hematology

Dual inhibition of STAT3 and STAT5 may overcome imatinib resistance in chronic myeloid leukemia. [Abstract]

2023 Dec;28(1):2224625. PMID: 37345979

Lösungsmittel & Löslichkeit

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.6378 mL

8.1888 mL

16.3776 mL

5 mM

0.3276 mL

1.6378 mL

3.2755 mL

10 mM

0.1638 mL

0.8189 mL

1.6378 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (4.09 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (274 KB)
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)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Haftchenary S, 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):1102-1107. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

SH-4-54

19 Cited Publications

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SH-4-54

Stattic

NSC 74859

STAT5-IN-1

Napabucasin

C188-9

Ruxolitinib

AS1517499

BP-1-102

Fludarabine

Ochromycinone

Dasatinib

LLL12

Publications Citing Use of MedChemExpress (MCE) SH-4-54

Alle STAT Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (19)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

SH-4-54

Stattic

NSC 74859

STAT5-IN-1

Napabucasin

C188-9

Ruxolitinib

AS1517499

BP-1-102

Fludarabine

Ochromycinone

Dasatinib

LLL12

Publications Citing Use of MedChemExpress (MCE) SH-4-54

Alle STAT Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (19)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

SH-4-54 Related Classifications

HY-16975 Related Classifications