Art. -Nr.: HY-15146

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NSC 74859

(Synonyms: S3I-201)

62 Cited Publications

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Based on 62 publication(s) in Google Scholar

NSC 74859 (S3I-201) is a selective Stat3 inhibitor with an IC₅₀ of 86 μM.

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Reinheit: 98.35%
CAS. Nr.: 501919-59-1
Formel: C₁₆H₁₅NO₇S
Molecular Weight:365.36

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years

* The compound is unstable in solutions, freshly prepared is recommended.

NSC 74859 Chemical Structure

CAS. Nr.: 501919-59-1

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Top Publications Citing

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 (62)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Bioz

Biologische Aktivität

Beschreibung

NSC 74859 (S3I-201) is a selective Stat3 inhibitor with an IC₅₀ of 86 μM^[1].

IC₅₀ & Target^[1]

STAT3

86 μM (IC₅₀)

Alle STAT Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
NIH3T3	IC₅₀	>300 μM Compound: 21, S3I-201	Inhibition of STAT1 dimerization in EGF-stimulated mouse NIH/3T3 cells overexpressing human EGFR assessed as suppression of STAT1-DNA interaction after 30 mins by EMSA Inhibition of STAT1 dimerization in EGF-stimulated mouse NIH/3T3 cells overexpressing human EGFR assessed as suppression of STAT1-DNA interaction after 30 mins by EMSA	[PMID: 22650325]
NIH3T3	IC₅₀	>300 μM Compound: S3I-201, NSC-74859	Inhibition of Stat1:Stat1 dimerization in EGF-stimulated mouse NIH3T3 cells expressing hEGFR with activated Stat1, Stat3, Stat5 Inhibition of Stat1:Stat1 dimerization in EGF-stimulated mouse NIH3T3 cells expressing hEGFR with activated Stat1, Stat3, Stat5	[PMID: 17463090]
NIH3T3	IC₅₀	160 μM Compound: 21, S3I-201	Inhibition of STAT1/STAT3 in EGF-stimulated mouse NIH/3T3 cells overexpressing human EGFR assessed as suppression of STAT1/STAT3-DNA interaction after 30 mins by EMSA Inhibition of STAT1/STAT3 in EGF-stimulated mouse NIH/3T3 cells overexpressing human EGFR assessed as suppression of STAT1/STAT3-DNA interaction after 30 mins by EMSA	[PMID: 22650325]
NIH3T3	IC₅₀	160 μM Compound: S3I-201, NSC-74859	Inhibition of Stat1:Stat3 dimerization in EGF-stimulated mouse NIH3T3 cells expressing hEGFR with activated Stat1, Stat3, Stat5 Inhibition of Stat1:Stat3 dimerization in EGF-stimulated mouse NIH3T3 cells expressing hEGFR with activated Stat1, Stat3, Stat5	[PMID: 17463090]
NIH3T3	IC₅₀	166 μM Compound: S3I-201, NSC-74859	Inhibition of Stat5:Stat5 dimerization in EGF-stimulated mouse NIH3T3 cells expressing hEGFR with activated Stat1, Stat3, Stat5 Inhibition of Stat5:Stat5 dimerization in EGF-stimulated mouse NIH3T3 cells expressing hEGFR with activated Stat1, Stat3, Stat5	[PMID: 17463090]
NIH3T3	IC₅₀	86 μM Compound: 21, S3I-201	Inhibition of STAT3 dimerization in EGF-stimulated mouse NIH/3T3 cells overexpressing human EGFR assessed as suppression of STAT3-DNA interaction after 30 mins by EMSA Inhibition of STAT3 dimerization in EGF-stimulated mouse NIH/3T3 cells overexpressing human EGFR assessed as suppression of STAT3-DNA interaction after 30 mins by EMSA	[PMID: 22650325]
NIH3T3	IC₅₀	86 μM Compound: 21, S3I-201	Inhibition of STAT3 dimerization in v-Src transformed mouse NIH/3T3 cells overexpressing human EGFR assessed as suppression of STAT3-DNA interaction in nucleus after 30 mins by EMSA Inhibition of STAT3 dimerization in v-Src transformed mouse NIH/3T3 cells overexpressing human EGFR assessed as suppression of STAT3-DNA interaction in nucleus after 30 mins by EMSA	[PMID: 22650325]
NIH3T3	IC₅₀	86 μM Compound: S3I-201, NSC-74859	Inhibition of Stat3 DNA binding activity in EGF-stimulated mouse NIH3T3 cells expressing hEGFR with activated Stat1, Stat3, Stat5 Inhibition of Stat3 DNA binding activity in EGF-stimulated mouse NIH3T3 cells expressing hEGFR with activated Stat1, Stat3, Stat5	[PMID: 17463090]
NIH3T3	IC₅₀	86 μM Compound: S3I-201, NSC-74859	Inhibition of Stat3:Stat3 dimerization in EGF-stimulated mouse NIH3T3 cells expressing hEGFR with activated Stat1, Stat3, Stat5 Inhibition of Stat3:Stat3 dimerization in EGF-stimulated mouse NIH3T3 cells expressing hEGFR with activated Stat1, Stat3, Stat5	[PMID: 17463090]

In Vitro

NSC 74859 (S3I-201) preferentially inhibits Stat3 DNA-binding activity over that of Stat1 (IC₅₀ values, Stat3?Stat3, 86±33 μM; Stat1?Stat3, 160±43 μM; and Stat1?Stat1, >300 μM) and inhibits that of Stat5 with IC₅₀ of 166±17 μM). NSC 74859 significantly reduces viable cell numbers and inhibits growth of transformed mouse fibroblasts NIH 3T3/v-Src and breast carcinoma cell lines (MDA-MB-231, MDA-MB-435, and MDA-MB-468). At 30-100 μM, NSC 74859 induces significant apoptosis in the representative human breast carcinoma cell line MDA-MB-435 and NIH 3T3/v-Src, both of which harbor constitutively active Stat3. The breast carcinoma MDA-MB-435 cell line is more sensitive to 30 μM NSC 74859. By contrast, the human breast cancer MDA-MB-453 cells and the normal mouse fibroblasts (NIH 3T3), which do not contain abnormal Stat3 activity, are less sensitive to NSC 74859 at 100 μM or less. At 300 μM or higher, NSC 74859 induced general, nonspecific cytotoxicity independent of Stat3 activation status^[1]. Huh-7 cells do not express β2SP or TBGFR2 and are sensitive to STAT3 inhibition, with an IC₅₀ of 100 μM for NSC 74859, regardless of CD133⁺ status. The IC₅₀ of NSC 74859 is 150 μM for Huh-7 and SNU-398 cells, 15 μM for SNU-475 cells and 200 μM for SNU-182 cells. NSC 74859 inhibits breast carcinoma MDA-MB-435, MDA-MB-453 and MDA-MB-231 cell lines with an IC₅₀ close to 100 μM^[2].

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

In Vivo

Human breast (MDA-MB-231) tumor-bearing mice are given an i.v. injection of NSC 74859 (S3I-201) or vehicle every 2 or every 3 days for 2 weeks, and tumor measurements are taken every 2-3 days. Compared with control (vehicle-treated) tumors, which continued to grow, human breast tumors in mice that received S3I-201 display strong growth inhibition. Continued evaluation of treated mice on termination of treatment shows no resumption of tumor growth, suggesting potentially a long-lasting effect of S3I-201 on tumor growth^[1]. Compared with vehicle-treated control tumors (n=15), which continued to grow, S3I-201 treatment of somatotroph tumor xenografts (n=15) significantly attenuated tumor growth for the duration of the experiment. Tumors derived from NSC 74859-treated rats are significantly smaller than those from the untreated group (220±16 mm³ vs. 287±16 mm³, P<0.01) as early as 5 days after NSC 74859 injection. Fifteen days after treatments, the average tumor volume of NSC 74859-treated rats is 64% of that of controls (449±40 mm³ vs. 708±83 mm³, P<0.01). Rats are sacrificed and tumors are harvested 15 days after treatment initiation. The average tumor weight of NSC 74859-treated rats is 78±8 mg, while tumors derived from control rats weighed 114±13 mg (32% reduction; P<0.05)^[3].

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

Chemical Information

CAS. Nr. 501919-59-1
Appearance Solid
Molecular Weight 365.36
Formel C₁₆H₁₅NO₇S
Color White to gray
SMILES

OC1=CC(NC(COS(=O)(C2=CC=C(C=C2)C)=O)=O)=CC=C1C(O)=O
Synonyms

S3I-201
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years

* The compound is unstable in solutions, freshly prepared is recommended.

Publications (62)

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Journal Impact Factor

Nat Commun

Blockade of glucagon receptor induces α-cell hypersecretion by hyperaminoacidemia in mice. [Abstract]

2025 Mar 12;16(1):2473. PMID: 40075066
Nat Commun

TMEM25 inhibits monomeric EGFR-mediated STAT3 activation in basal state to suppress triple-negative breast cancer progression. [Abstract]

2023 Apr 24;14(1):2342. PMID: 37095176
Acta Pharm Sin B

Dimeric natural product panepocyclinol A inhibits STAT3 via di-covalent modification. [Abstract]

2025 Jan;15(1):409-423. PMID: 40041920
Adv Sci (Weinh)

CD63+ Cancer-Associated Fibroblasts Confer Tamoxifen Resistance to Breast Cancer Cells through Exosomal miR-22. [Abstract]

2020 Sep 24;7(21):2002518. PMID: 33173749
Theranostics

Neuronal STAT3/HIF-1α/PTRF axis-mediated bioenergetic disturbance exacerbates cerebral ischemia-reperfusion injury via PLA2G4A. [Abstract]

2022 Apr 4;12(7):3196-3216. PMID: 35547748
J Exp Clin Cancer Res

Integrative analysis of bulk and single-cell gene expression profiles to identify tumor-associated macrophage-derived CCL18 as a therapeutic target of esophageal squamous cell carcinoma. [Abstract]

2023 Feb 27;42(1):51. PMID: 36850011

NSC 74859 purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2023 Feb 27;42(1):51. [Abstract]

The enhanced phosphorylation level of JAK2 and STAT3 mediated by rhCCL18 can be reversed by NSC 74859 (S3I-201) in EC-109, EC-109 Vector and EC-109 shPITPNM3 cells.
Sci Adv

Transition of pseudorabies virus from latency to reactivation state selectively triggered by pathogenic bacteria. [Abstract]

2025 Nov 21;11(47):eadw4206. PMID: 41259522
Cancer Lett

CD146 mediates an E-cadherin-to-N-cadherin switch during TGF-β signaling-induced epithelial-mesenchymal transition. [Abstract]

2018 Aug 28:430:201-214. PMID: 29777784

NSC 74859 purchased from MedChemExpress. Usage Cited in: Cancer Lett. 2018 Aug 28:430:201-214. [Abstract]

CD146^WT or CD146^KO MEFs are stimulated with or without TGF-β1 (10 ng/mL) for 24 h in the presence or absence of NSC74859 (200 μM). The expression of CD146, the expression and activation of STAT3, and the expression levels of E-cadherin, N-cadherin, and Twist are assessed by immunoblotting.
Cell Death Dis

Myeloid-derived suppressor cells-induced exhaustion of CD8 + T-cell participates in rejection after liver transplantation. [Abstract]

2024 Jul 16;15(7):507. PMID: 39013845
Cell Death Dis

Hypoxic glioma-derived exosomes promote M2-like macrophage polarization by enhancing autophagy induction. [Abstract]

2021 Apr 7;12(4):373. PMID: 33828078
Genes Dis

Autophagy-induced NR2F1 activation promotes the apoptosis of lens epithelial cells and facilitates cataract-associated fibrosis through targeting STAT3. [Abstract]

2025 Jan 28;12(5):101549. PMID: 40641526
Dev Cell

STAT3-controlled CHI3L1/SPP1 positive feedback loop demonstrates the spatial heterogeneity and immune characteristics of glioblastoma. [Abstract]

2025 Jun 23;60(12):1751-1767.e9. PMID: 39933531
Int J Biol Macromol

Bone marrow tyrosine kinase on chromosome X promotes epithelial-mesenchymal transition through signal transducer and activator of transcription 3 in colorectal cancer. [Abstract]

2026 Feb;344(Pt 1):150362. PMID: 41565140
Int J Biol Macromol

Angelica sinensis polysaccharide attenuates CCl4-induced liver fibrosis via the IL-22/STAT3 pathway. [Abstract]

2020 Nov 1;162:273-283. PMID: 32569681
Phytomedicine

Puerarin mitigates cognitive decline and white matter injury via CD36-Mediated microglial phagocytosis in chronic cerebral hypoperfusion. [Abstract]

2025 Jan 16:138:156396. PMID: 39827816
Basic Res Cardiol

HIMF deletion ameliorates acute myocardial ischemic injury by promoting macrophage transformation to reparative subtype. [Abstract]

2021 Apr 23;116(1):30. PMID: 33893593
Brain Behav Immun

Spinal interleukin-10 produces antinociception in neuropathy through microglial β-endorphin expression, separated from antineuroinflammation. [Abstract]

2018 Oct:73:504-519. PMID: 29928964
Biomed Pharmacother

Inhibition the ubiquitination of ENaC and Na,K-ATPase with erythropoietin promotes alveolar fluid clearance in sepsis-induced acute respiratory distress syndrome. [Abstract]

2024 May:174:116447. PMID: 38518606
Arch Pharm Res

Chemerin reverses the malignant phenotype and induces differentiation of human hepatoma SMMC7721 cells. [Abstract]

2021 Feb;44(2):194-204. PMID: 33502677
Chin Med J (Engl)

Sphingosine-1-phosphate induces pulmonary artery smooth muscle cell proliferation, migration and pulmonary arterial remodeling by modulating sonic hedgehog signaling effector FoxM1. [Abstract]

2026 May 5;139(9):1375-1387. PMID: 41859863
Cell Rep

A basophil-fibroblast pro-inflammatory axis fuels type 2 skin inflammation. [Abstract]

2025 Aug 7;44(8):116114. PMID: 40782349
Clin Transl Med

Tumor-derived exosomal miR-19b-3p facilitates M2 macrophage polarization and exosomal LINC00273 secretion to promote lung adenocarcinoma metastasis via Hippo pathway. [Abstract]

2021 Sep;11(9):e478. PMID: 34586722
Mol Med

JAK2/STAT3/HMGCS2 signaling aggravates mitochondrial dysfunction and oxidative stress in hyperuricemia-induced cardiac dysfunction. [Abstract]

2025 May 13;31(1):184. PMID: 40361044
J Agric Food Chem

Chlorogenic Acid Alleviates Chronic Stress-Induced Duodenal Ferroptosis via the Inhibition of the IL-6/JAK2/STAT3 Signaling Pathway in Rats. [Abstract]

2022 Apr 13;70(14):4353-4361. PMID: 35380825
J Gastroenterol

Inhibition of integrin α3 suppresses gastric cancer progression via STAT3-mediated regulation of SLC1A5-dependent glutamine uptake. [Abstract]

2025 Oct 8. PMID: 41060436
Inflamm Res

Activating α7nAChR helps post-myocardial infarction healing by regulating macrophage polarization via the STAT3 signaling pathway. [Abstract]

2023 Apr;72(4):879-892. PMID: 36912917
Virulence

Vagus nerve plays a pivotal role in CD4+ T cell differentiation during CVB3-induced murine acute myocarditis. [Abstract]

2021 Dec;12(1):360-376. PMID: 33380272
Cells

Targeting JAK2/STAT3-Dependent Macrophage Polarization by Chlorogenic Acid Attenuates Hepatic Inflammation in Chronic Stress. [Abstract]

2025 Nov 24;14(23):1848. PMID: 41369337
Cancer Immunol Immunother

STAT3 promotes differentiation of monocytes to MDSCs via CD39/CD73-adenosine signal pathway in oral squamous cell carcinoma. [Abstract]

2023 May;72(5):1315-1326. PMID: 36436019
Mech Ageing Dev

AMPK alleviates oxidative stress‑induced premature senescence via inhibition of NF-κB/STAT3 axis-mediated positive feedback loop. [Abstract]

2020 Oct;191:111347. PMID: 32882228
Cancer Gene Ther

GPR107: A key driver of breast cancer invasion and metastasis through collagen IV modulation. [Abstract]

2025 Dec;32(12):1414-1427. PMID: 41073571
Biofactors

HMGB1 knock-down promoting tumor cells viability and arrest pro-apoptotic proteins via Stat3/NFκB in HepG2 cells. [Abstract]

2018 Nov;44(6):570-576. PMID: 30375073

NSC 74859 purchased from MedChemExpress. Usage Cited in: Biofactors. 2018 Nov;44(6):570-576. [Abstract]

Westen Blot analysis of HMGB1 expression in HepG2 cells in the treatment of Stat3 inhibitor NSC74859 (SI3), or activator (NAC).
Int J Mol Sci

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

2022 Apr 12;23(8):4277. PMID: 35457095
Pharm Biol

Majoon Ushba alleviated IL-17A sensitized keratinocyte ferroptosis via JAK-2-STAT-3 signaling axis and reversed imiquimod induced psoriasiform inflammation. [Abstract]

2026 Dec;64(1):575-598. PMID: 41973793
Int Immunopharmacol

IL-17A/IL-17RA interaction blockade sensitizes synovial macrophages to efferocytosis and PD-L1 signaling via rewiring STAT-3/ADAM17/MERTK axis in rheumatoid arthritis animal model. [Abstract]

2024 May 28:136:112343. PMID: 38810305
Int Immunopharmacol

3, 3'- diindolylmethane hinders IL-17A/IL-17RA interaction and mitigates imiquimod-induced psoriasiform in mice. [Abstract]

2022 Apr 26;109:108795. PMID: 35487087
Int Immunopharmacol

Dexmedetomidine ameliorates LPS induced acute lung injury via GSK-3β/STAT3-NF-κB signaling pathway in rats. [Abstract]

2019 Sep:74:105717. PMID: 31254953
Toxicology

Recombinant Klotho alleviates vancomycin-induced acute kidney injury by upregulating anti-oxidative capacity via JAK2/STAT3/GPx3 axis. [Abstract]

2023 Nov:499:153657. PMID: 37884167
Biochim Biophys Acta Mol Basis Dis

TAX1BP1 downregulation by STAT3 in cardiac fibroblasts contributes to diabetes-induced heart failure with preserved ejection fraction. [Abstract]

2024 Feb;1870(2):166979. PMID: 38065272
J Cell Mol Med

Periplocymarin alleviates pathological cardiac hypertrophy via inhibiting the JAK2/STAT3 signalling pathway. [Abstract]

2022 May;26(9):2607-2619. PMID: 35365949
Oncol Res

Gallic acid suppresses esophageal squamous cell carcinoma progression and enhances cisplatin chemosensitivity through IL-6/STAT3/Notch pathway. [Abstract]

2025 May 29;33(6):1473-1484. PMID: 40486873
J Cell Physiol

Leptin excites basolateral amygdala principal neurons and reduces food intake by LepRb-JAK2-PI3K-dependent depression of GIRK channels. [Abstract]

2024 Feb;239(2):e31117. PMID: 37683049
J Cell Physiol

CXCL6 fuels the growth and metastases of esophageal squamous cell carcinoma cells both in vitro and in vivo through upregulation of PD-L1 via activation of STAT3 pathway. [Abstract]

2021 Jul;236(7):5373-5386. PMID: 33368292
J Cell Physiol

Fucoidan inhibits tooth movement by promoting restorative macrophage polarization through the STAT3 pathway. [Abstract]

2020 Sep;235(9):5938-5950. PMID: 31967324
J Neurosci

Autocrine Interleukin-10 Mediates Glucagon-Like Peptide-1 Receptor-Induced Spinal Microglial β-Endorphin Expression. [Abstract]

2017 Nov 29;37(48):11701-11714. PMID: 29084866
Cytokine

Cyanidin attenuates IL-17A cytokine signaling mediated monocyte migration and differentiation into mature osteoclasts in rheumatoid arthritis. [Abstract]

2021 Jun:142:155502. PMID: 33810944
Exp Cell Res

Down-regulation of A3AR signaling by IL-6-induced GRK2 activation contributes to Th17 cell differentiation. [Abstract]

2021 Feb 15;399(2):112482. PMID: 33434531
Front Physiol

P-STAT3 Inhibition Activates Endoplasmic Reticulum Stress-Induced Splenocyte Apoptosis in Chronic Stress. [Abstract]

2020 Jun 30;11:680. PMID: 32714202
Toxicol Appl Pharmacol

Cyanidin prevents the hyperproliferative potential of fibroblast-like synoviocytes and disease progression via targeting IL-17A cytokine signalling in rheumatoid arthritis. [Abstract]

2020 Mar 15;391:114917. PMID: 32044269
Mol Carcinog

Tex10 interacts with STAT3 to regulate hepatocellular carcinoma growth and metastasis. [Abstract]

2023 Dec;62(12):1974-1989. PMID: 37792308
Mol Immunol

Interleukin 17 regulates SHP-2 and IL-17RA/STAT-3 dependent Cyr61, IL-23 and GM-CSF expression and RANKL mediated osteoclastogenesis by fibroblast-like synoviocytes in rheumatoid arthritis. [Abstract]

2017 Nov:91:134-144. PMID: 28898718

NSC 74859 purchased from MedChemExpress. Usage Cited in: Mol Immunol. 2017 Nov:91:134-144. [Abstract]

AA-FLS cultured in the presence or absence of S3I-201 for 24 h, then treated with IL-17 for an additional 24 h and phosphorylation of STAT-3 is detected by western blotting.
3 Biotech

Selective blockade of IL-21 by myricetin impedes T follicular helper cell differentiation by negatively regulating the JAK/STAT/Bcl-6 pathway in a rheumatoid arthritis animal model. [Abstract]

2024 Jan;14(1):25. PMID: 38164247
J Cell Biochem

Ferulic acid inhibits interleukin 17-dependent expression of nodal pathogenic mediators in fibroblast-like synoviocytes of rheumatoid arthritis. [Abstract]

2019 Feb;120(2):1878-1893. PMID: 30160792

NSC 74859 purchased from MedChemExpress. Usage Cited in: J Cell Biochem. 2019 Feb;120(2):1878-1893. [Abstract]

AA-FLS are treated with different concentrations (25, 50, and 100 µM) of Ferulic acid (FA) and 50 µM of S3I-201 and then cultured in the presence or absence of IL-17 (10 ng/mL). The cell lysates are subjected to Western blot analysis to assess the expression levels of TLR-3, Cyr61, IL-23 and GM-CSF proteins.
Microbes Infect

Absence of PD-L1 signaling hinders macrophage defense against Mycobacterium tuberculosis via upregulating STAT3/IL-6 pathway. [Abstract]

2024 May 8:105352. PMID: 38729294
Oncol Lett

Exosomes derived from endoplasmic reticulum-stressed liver cancer cells enhance the expression of cytokines in macrophages via the STAT3 signaling pathway. [Abstract]

2020 Jul;20(1):589-600. PMID: 32565984
Environ Monit Assess

Assessment of the physicochemical characteristics of by-products of cassava processing and their effects on biodiversity. [Abstract]

2025 Apr 10;197(5):533. PMID: 40208441
Indian J Pharm Sci

2022: 117-124.
Authorea

December 16, 2022.
Research Square Preprint

2021 Sep.
Research Square Preprint

2020 Jul.
Nationwide Children’s Hospital

Columbus. 01 Jun 2017.
Oncotarget

Ponatinib promotes a G1 cell-cycle arrest of merlin/NF2-deficient human schwann cells. [Abstract]

2017 May 9;8(19):31666-31681. PMID: 28427224

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (273.70 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

2.7370 mL

13.6851 mL

27.3703 mL

5 mM

0.5474 mL

2.7370 mL

5.4741 mL

10 mM

0.2737 mL

1.3685 mL

2.7370 mL

Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.

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: ≥ 7.5 mg/mL (20.53 mM); Clear solution

This protocol yields a clear solution of ≥ 7.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (75.0 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% (20% SBE-β-CD in Saline)

Solubility: ≥ 7.5 mg/mL (20.53 mM); Clear solution

This protocol yields a clear solution of ≥ 7.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (75.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

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

Solubility: ≥ 7.5 mg/mL (20.53 mM); Clear solution

This protocol yields a clear solution of ≥ 7.5 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 (75.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Protocol 4

Add each solvent one by one: 5% DMSO 40% PEG300 5% Tween-80 50% Saline

Solubility: ≥ 2.5 mg/mL (6.84 mM); Clear solution

Protocol 5

Add each solvent one by one: 5% DMSO 95% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (6.84 mM); Clear solution

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

Protokoll

Cell Assay^[1]

Proliferating cells are treated with or without NSC 74859 (30-100 μM) for up to 48 h. In some cases, cells are first transfected with Stat3C, ST3-NT, or ST3-SH2 domain or mock-transfected for 24 h before treatment with compound for an additional 24-48 h. Cells are then detached and analyzed by annexin V binding and flow cytometry to quantify the percent apoptosis^[1].

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

Animal Administration^[1]^[3]

Mice^[1]
Six-week-old female athymic nude mice are used. Athymic nude mice are injected in the left flank area s.c. with 5×10⁶ human breast cancer MDA-MB-231 cells in 100 μL of PBS. After 5-10 days, tumors with a diameter of 3 mm are established. Animals are given NSC 74859 i.v. at 5 mg/kg every 2 or 3 days for 2 weeks and monitored every 2 or 3 days. Animals are stratified so that the mean tumor sizes in all treatment are nearly identical. Tumor volume is calculated according to the formula V=0.52×a²×b, where a is the smallest superficial diameter and b is the largest superficial diameter.
Rats^[3]
Four-week-old female Wistar Furth rats are used. GH3 cells (5×10⁵ cells in 100 μL Matrigel) are subcutaneously injected into the left lumbar area. After 7 days, tumors with a volume of approximately 100 mm³ are established. Rats are given NSC 74859 intravenously at 5 mg/kg every 2 or 3 days for 2 weeks. Tumor size is measured by caliper measurements twice a week, and volume is calculated as follows: volume=(length×width²)/2. Three weeks after cell inoculations, animals are euthanized and excised tumors are weighed. Blood samples are collected 1 day before S3I-201 treatment and again on the day of euthanization. Serum GH and prolactin are assessed by RIA or ELISA, respectively.

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (280 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)
- 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]. Siddiquee K, et al. Selective chemical probe inhibitor of Stat3, identified through structure-based virtual screening, induces antitumor activity. Proc Natl Acad Sci U S A. 2007 May 1;104(18):7391-6. [Content Brief]

[2]. Lin L, et al. The STAT3 inhibitor NSC 74859 is effective in hepatocellular cancers with disrupted TGF-β signaling. Oncogene. 2009 Feb 19;28(7):961-72. [Content Brief]

[3]. Zhou C, et al. STAT3 upregulation in pituitary somatotroph adenomas induces hypersecretion. J Clin Invest. 2015 Apr;125(4):1692-702 [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

Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.7370 mL	13.6851 mL	27.3703 mL	68.4257 mL
	5 mM	0.5474 mL	2.7370 mL	5.4741 mL	13.6851 mL
	10 mM	0.2737 mL	1.3685 mL	2.7370 mL	6.8426 mL
	15 mM	0.1825 mL	0.9123 mL	1.8247 mL	4.5617 mL
	20 mM	0.1369 mL	0.6843 mL	1.3685 mL	3.4213 mL
	25 mM	0.1095 mL	0.5474 mL	1.0948 mL	2.7370 mL
	30 mM	0.0912 mL	0.4562 mL	0.9123 mL	2.2809 mL
	40 mM	0.0684 mL	0.3421 mL	0.6843 mL	1.7106 mL
	50 mM	0.0547 mL	0.2737 mL	0.5474 mL	1.3685 mL
	60 mM	0.0456 mL	0.2281 mL	0.4562 mL	1.1404 mL
	80 mM	0.0342 mL	0.1711 mL	0.3421 mL	0.8553 mL
	100 mM	0.0274 mL	0.1369 mL	0.2737 mL	0.6843 mL

Keywords

NSC 74859

62 Cited Publications

100 mg Angebot einholen

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NSC 74859

MCE Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) NSC 74859

Alle STAT Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (62)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

NSC 74859

MCE Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) NSC 74859

Alle STAT Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (62)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

NSC 74859 Related Classifications

Art. -Nr.: HY-15146