NSC 74859
Based on 62 publication(s) in Google Scholar
NSC 74859 (S3I-201) is a selective Stat3 inhibitor with an IC50 of 86 μM.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 98.35%
- CAS No.: 501919-59-1
- Formule: C16H15NO7S
- Masse moléculaire:365.36
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Stockage:Powder -20°C, 3 years , 4°C, 2 years
* The compound is unstable in solutions, freshly prepared is recommended.
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) NSC 74859
More- Nat Commun. 2025 Mar 12;16(1):2473. [Abstract]
- Nat Commun. 2023 Apr 24;14(1):2342. [Abstract]
- Acta Pharm Sin B. 2025 Jan;15(1):409-423. [Abstract]
- Adv Sci (Weinh). 2020 Sep 24;7(21):2002518. [Abstract]
- Theranostics. 2022 Apr 4;12(7):3196-3216. [Abstract]
- J Exp Clin Cancer Res. 2023 Feb 27;42(1):51. [Abstract]
- Sci Adv. 2025 Nov 21;11(47):eadw4206. [Abstract]
- Cancer Lett. 2018 Aug 28:430:201-214. [Abstract]
- Cell Death Dis. 2024 Jul 16;15(7):507. [Abstract]
- Cell Death Dis. 2021 Apr 7;12(4):373. [Abstract]
- Genes Dis. 2025 Jan 28;12(5):101549. [Abstract]
- Dev Cell. 2025 Jun 23;60(12):1751-1767.e9. [Abstract]
- Int J Biol Macromol. 2026 Feb;344(Pt 1):150362. [Abstract]
- Int J Biol Macromol. 2020 Nov 1;162:273-283. [Abstract]
- Phytomedicine. 2025 Jan 16:138:156396. [Abstract]
- Basic Res Cardiol. 2021 Apr 23;116(1):30. [Abstract]
- Brain Behav Immun. 2018 Oct:73:504-519. [Abstract]
- Biomed Pharmacother. 2024 May:174:116447. [Abstract]
- Arch Pharm Res. 2021 Feb;44(2):194-204. [Abstract]
- Chin Med J (Engl). 2026 May 5;139(9):1375-1387. [Abstract]
- Cell Rep. 2025 Aug 7;44(8):116114. [Abstract]
- Clin Transl Med. 2021 Sep;11(9):e478. [Abstract]
- Mol Med. 2025 May 13;31(1):184. [Abstract]
- J Agric Food Chem. 2022 Apr 13;70(14):4353-4361. [Abstract]
- J Gastroenterol. 2025 Oct 8. [Abstract]
- Inflamm Res. 2023 Apr;72(4):879-892. [Abstract]
- Virulence. 2021 Dec;12(1):360-376. [Abstract]
- Cells. 2025 Nov 24;14(23):1848. [Abstract]
- Cancer Immunol Immunother. 2023 May;72(5):1315-1326. [Abstract]
- Mech Ageing Dev. 2020 Oct;191:111347. [Abstract]
- Cancer Gene Ther. 2025 Dec;32(12):1414-1427. [Abstract]
- Biofactors. 2018 Nov;44(6):570-576. [Abstract]
- Int J Mol Sci. 2022 Apr 12;23(8):4277. [Abstract]
- Pharm Biol. 2026 Dec;64(1):575-598. [Abstract]
- Int Immunopharmacol. 2024 May 28:136:112343. [Abstract]
- Int Immunopharmacol. 2022 Apr 26;109:108795. [Abstract]
- Int Immunopharmacol. 2019 Sep:74:105717. [Abstract]
- Toxicology. 2023 Nov:499:153657. [Abstract]
- Biochim Biophys Acta Mol Basis Dis. 2024 Feb;1870(2):166979. [Abstract]
- J Cell Mol Med. 2022 May;26(9):2607-2619. [Abstract]
- Oncol Res. 2025 May 29;33(6):1473-1484. [Abstract]
- J Cell Physiol. 2024 Feb;239(2):e31117. [Abstract]
- J Cell Physiol. 2021 Jul;236(7):5373-5386. [Abstract]
- J Cell Physiol. 2020 Sep;235(9):5938-5950. [Abstract]
- J Neurosci. 2017 Nov 29;37(48):11701-11714. [Abstract]
- Cytokine. 2021 Jun:142:155502. [Abstract]
- Exp Cell Res. 2021 Feb 15;399(2):112482. [Abstract]
- Front Physiol. 2020 Jun 30;11:680. [Abstract]
- Toxicol Appl Pharmacol. 2020 Mar 15;391:114917. [Abstract]
- Mol Carcinog. 2023 Dec;62(12):1974-1989. [Abstract]
- Mol Immunol. 2017 Nov:91:134-144. [Abstract]
- 3 Biotech. 2024 Jan;14(1):25. [Abstract]
- J Cell Biochem. 2019 Feb;120(2):1878-1893. [Abstract]
- Microbes Infect. 2024 May 8:105352. [Abstract]
- Oncol Lett. 2020 Jul;20(1):589-600. [Abstract]
- Environ Monit Assess. 2025 Apr 10;197(5):533. [Abstract]
- 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. 2017 May 9;8(19):31666-31681. [Abstract]
Customer Validation & Images
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Activité biologique
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STAT3 86 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| NIH3T3 | IC50 |
>300 μM
Compound: 21, S3I-201
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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
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[PMID: 22650325] |
| NIH3T3 | IC50 |
>300 μM
Compound: S3I-201, NSC-74859
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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
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[PMID: 17463090] |
| NIH3T3 | IC50 |
160 μM
Compound: 21, S3I-201
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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
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[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
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[PMID: 17463090] |
| NIH3T3 | IC50 |
166 μM
Compound: S3I-201, NSC-74859
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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
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[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
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[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
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[PMID: 17463090] |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 501919-59-1
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Appearance Solid
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Masse moléculaire 365.36
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Formule C16H15NO7S
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Color White to gray
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SMILES
OC1=CC(NC(COS(=O)(C2=CC=C(C=C2)C)=O)=O)=CC=C1C(O)=O
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Synonyms
S3I-201
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
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
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Most Recent
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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
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.
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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]
CD146WT or CD146KO 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.
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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
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).
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Int J Mol Sci
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
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.
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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.
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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 -
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Oncotarget
2017 May 9;8(19):31666-31681. PMID: 28427224
Solvant et solubilité
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)
Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.
Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.
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: ≥ 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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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. * The compound is unstable in solutions, freshly prepared is recommended.
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.
Protocole
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.
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.
Pureté et documentation
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Fiche technique (280 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
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Instruction de manipulation (2659 KB)
Références
[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]
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 |
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