Art. -Nr.: HY-100753

STAT3-IN-1

11 Cited Publications

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Based on 11 publication(s) in Google Scholar

STAT3-IN-1 (compound 7d) is an excellent, selective and orally active STAT3 inhibitor, with IC₅₀ values of 1.82 μM and 2.14 μM in HT29 and MDA-MB 231 cells, respectively. STAT3-IN-1 (compound 7d) induces tumor cells apoptosis.

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Reinheit: 96.28%
CAS. Nr.: 2059952-75-7
Formel: C₂₈H₂₉NO₆
Molecular Weight:475.53

Speicherung:

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

STAT3-IN-1 Chemical Structure

CAS. Nr.: 2059952-75-7

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (11)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

Stat-3

1.82 μM (IC₅₀, in HT29 cells)

Stat-3

2.14 μM (IC₅₀, in MDA-MB 231 cells)

Alle STAT Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
HT-29	IC₅₀	1.82 μM Compound: 7d	Growth inhibition of human HT-29 cells after 48 hrs by MTT assay Growth inhibition of human HT-29 cells after 48 hrs by MTT assay	[PMID: 27783972]
MDA-MB-231	IC₅₀	2.14 μM Compound: 7d	Growth inhibition of human MDA-MB-231 cells after 48 hrs by MTT assay Growth inhibition of human MDA-MB-231 cells after 48 hrs by MTT assay	[PMID: 27783972]

In Vitro

STAT3-IN-1 (compound 7d: 0-10 μM, 48 h) inhibits the STAT3 acetylation at lysine 685 and affected its specific genes expressions^[1].
? STAT3-IN-1 (compound 7d: 0-10 μM, 48 h) induces tumor cells apoptosis in MDA-MB-231 cells^[1].

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

Apoptosis Analysis^[1]

Cell Line:

MDA-MB-231 cell lines.
Concentration:

0-10 μM.
Incubation Time:

48 hours.
Result:

The induced apoptosis rates (early and late apoptosis) at 1, 2, 5, 8 and 10 μM were 9.0%, 11.2%, 20.9%, 43.3% and 85.2% versus control 3.0%.

Western Blot Analysis^[1]

Cell Line:

MDA-MB-231 and HT-29 cell lines.
Concentration:

0-10 μM.
Incubation Time:

48 hours.
Result:

Inhibited STAT3 acetylation and STAT3 tyrosine phosphorylation in MDA-MB-231 cells.
Increased the expressions of these tumor-suppressor genes (PTPN6 (SHP-1), CDKN2A and DLEC1) which were related to STAT3 acetylation at Lys685.

In Vivo

STAT3-IN-1 (compound 7d: 10, 20 mg/kg, two weeks) arrests tumor growth with low toxicity in mouse-xenograft model^[1].

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

Animal Model:

Mouse-xenograft model bearing inoculation of mice breast cancer 4T1 cells^[1].
Dosage:

10, 20 mg/kg.
Administration:

Oral administration once every other day for two weeks.
Result:

Arrested tumor growth with no obvious body weight loss.

Chemical Information

CAS. Nr. 2059952-75-7
Appearance Solid
Molecular Weight 475.53
Formel C₂₈H₂₉NO₆
Color Light yellow to orange
SMILES

COC1=CC(OC)=CC(/C=C/C2=CC=C(NC(/C=C/C3=CC(OC)=C(OC)C(OC)=C3)=O)C=C2)=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 (11)

All WB

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Journal Impact Factor

Int J Oral Sci

LncRNA EUDAL shapes tumor cell response to hypoxia-induced constitutive EGFR activation and promotes chemoresistance in oral cancer. [Abstract]

2025 Sep 12;17(1):64. PMID: 40940319
Redox Biol

HDAC11 negatively regulates antifungal immunity by inhibiting Nos2 expression via binding with transcriptional repressor STAT3. [Abstract]

2022 Oct:56:102461. PMID: 36087429
Acta Pharm Sin B

The suppression of cervical cancer ferroptosis by macrophages: The attenuation of ALOX15 in cancer cells by macrophages-derived exosomes. [Abstract]

2023 Jun;13(6):2645-2662. PMID: 37425043
Neurotherapeutics

Reticuline modulates astrocyte and microglial responses to enhance prognosis after traumatic brain injury. [Abstract]

2025 Aug 5:e00709. PMID: 40769849
Biochem Pharmacol

Macrophages confer resistance to BET inhibition in triple-negative breast cancer by upregulating IKBKE. [Abstract]

2020 Oct;180:114126. PMID: 32603665
Cancer Biol Ther

PCBP1 regulates LIFR through FAM3C to maintain breast cancer stem cell self-renewal and invasiveness. [Abstract]

2023 Dec 31;24(1):2271638. PMID: 37927213
Cell Biol Toxicol

The mtDNA-STING pathway plays an important role in both navitoclax- and S63845-induced autophagy and enhances cell death. [Abstract]

2023 Dec;39(6):2821-2839. PMID: 37002446
Cell Oncol (Dordr)

OTUD1 downregulates PD-L1 expression by deubiquitinating STAT3 and promotes the immune response in CcRCC. [Abstract]

2025 Jun 12. PMID: 40506611
Int Immunopharmacol

PLD2 deletion alleviates disruption of tight junctions in sepsis-induced ALI by regulating PA/STAT3 phosphorylation pathway. [Abstract]

2023 Jan:114:109561. PMID: 36700766

STAT3-IN-1 purchased from MedChemExpress. Usage Cited in: Int Immunopharmacol. 2023 Jan:114:109561. [Abstract]

STAT3-IN-1 (5 µM) attenuates PA-induced degradation of endothelial TJs by inhibiting phosphorylation of STAT3 in HUVECs.
Cell Biol Int

Tumor-associated macrophage-derived CCL5 promotes chemotherapy resistance and metastasis in prostatic cancer. [Abstract]

2021 Oct;45(10):2054-2062. PMID: 34003531
Research Square Print

2022 May.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 125 mg/mL (262.86 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

2.1029 mL

10.5146 mL

21.0292 mL

5 mM

0.4206 mL

2.1029 mL

4.2058 mL

10 mM

0.2103 mL

1.0515 mL

2.1029 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: 6.25 mg/mL (13.14 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 6.25 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (62.5 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.

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 (276 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]. Li S, et al. Discovery of oral-available resveratrol-caffeic acid based hybrids inhibiting acetylated and phosphorylated STAT3 protein. Eur J Med Chem. 2016 Nov 29;124:1006-1018. [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	2.1029 mL	10.5146 mL	21.0292 mL	52.5729 mL
	5 mM	0.4206 mL	2.1029 mL	4.2058 mL	10.5146 mL
	10 mM	0.2103 mL	1.0515 mL	2.1029 mL	5.2573 mL
	15 mM	0.1402 mL	0.7010 mL	1.4019 mL	3.5049 mL
	20 mM	0.1051 mL	0.5257 mL	1.0515 mL	2.6286 mL
	25 mM	0.0841 mL	0.4206 mL	0.8412 mL	2.1029 mL
	30 mM	0.0701 mL	0.3505 mL	0.7010 mL	1.7524 mL
	40 mM	0.0526 mL	0.2629 mL	0.5257 mL	1.3143 mL
	50 mM	0.0421 mL	0.2103 mL	0.4206 mL	1.0515 mL
	60 mM	0.0350 mL	0.1752 mL	0.3505 mL	0.8762 mL
	80 mM	0.0263 mL	0.1314 mL	0.2629 mL	0.6572 mL
	100 mM	0.0210 mL	0.1051 mL	0.2103 mL	0.5257 mL

Keywords

STAT3-IN-1

11 Cited Publications

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STAT3-IN-1

Apoptosis Compound Library

Immunology/Inflammation Compound Library

JAK/STAT Compound Library

Kinase Inhibitor Library

Stem Cell Signaling Compound Library

Anti-Cancer Compound Library

Small Molecule Immuno-Oncology Compound Library

Anti-Aging Compound Library

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Transcription Factor-Targeted Library

Anti-Liver Cancer Compound Library

Anti-Prostate Cancer Compound Library

Cancer Stem Cells Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Covalent Screening Library Plus

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) STAT3-IN-1

Alle STAT Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (11)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

STAT3-IN-1 Related Classifications

HY-100753 Related Classifications