S31-201 | CAS#501919-59-1 | STAT3 inhibitor

MedKoo Cat#: 202541 | Name: S31-201

Description:

WARNING: This product is for research use only, not for human or veterinary use.

S3I-201, also known as NSC 74859, is a cell-permeable Stat3 inhibitor that binds to the Stat3-SH2 domain, prevents Stat3 phosphorylation/activation, dimerization, and DNA-binding.

Chemical Structure

S31-201

CAS#501919-59-1

Theoretical Analysis

MedKoo Cat#: 202541

Name: S31-201

CAS#: 501919-59-1

Chemical Formula: C16H15NO7S

Exact Mass: 365.0569

Molecular Weight: 365.36

Elemental Analysis: C, 52.60; H, 4.14; N, 3.83; O, 30.65; S, 8.78

Price and Availability

Size	Price	Availability
10mg	USD 90.00	Ready to ship
25mg	USD 150.00	Ready to ship
50mg	USD 250.00	Ready to ship
100mg	USD 450.00	Ready to ship
200mg	USD 750.00	Ready to ship
500mg	USD 1,450.00	Ready to ship

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Related CAS #

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Synonym

NSC 74859; NSC74859; NSC-74859; S3I-201; S3I 20; S3I201.

IUPAC/Chemical Name

2-hydroxy-4-(2-(tosyloxy)acetamido)benzoic acid

InChi Key

HWNUSGNZBAISFM-UHFFFAOYSA-N

InChi Code

InChI=1S/C16H15NO7S/c1-10-2-5-12(6-3-10)25(22,23)24-9-15(19)17-11-4-7-13(16(20)21)14(18)8-11/h2-8,18H,9H2,1H3,(H,17,19)(H,20,21)

SMILES Code

O=C(O)C1=CC=C(NC(COS(=O)(C2=CC=C(C)C=C2)=O)=O)C=C1O

Appearance

White to off-white solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO and DMF

Shelf Life

>5 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

In HCC cells with loss of response to TGF-.beta., NSC 74859, a STAT3-specific inhibitor, markedly suppresses growth. In contrast, CD133+ status did not affect the response to STAT3 inhibition: both CD133+ Huh-7 cells and CD133- Huh-7 cells are equally sensitive to NSC 74859 treatment and STAT3 inhibition, with an IC50 of 100 .mu.M. Thus, the TGF-.beta./beta2 spectrin (.beta.2SP) pathway may reflect a more functional 'stem/progenitor' state than CD133. Furthermore, NSC 74859 treatment of Huh-7 xenografts in nude mice significantly retarded tumor growth, with an ED of only 5 mg/kg. Moreover, NSC 74859 inhibited tyrosine phosphorylation of STAT3 in HCC cells in vivo. The authors conclude that inhibiting interleukin 6 (IL6)/STAT3 in HCCs with inactivation of the TGF-.beta./.beta.2SP pathway is an effective approach in management of HCCs. Thus, IL6/STAT3, a major signaling pathway in HCC stem cell renewal and proliferation, can provide a novel approach to the treatment of specific HCCs. see: Oncogene (2009), 28(7), 961-972. Current developer : H. Lee Moffitt Cancer Center & Research Institute, USA; University of South Florida; University of Central Florida

Product Data

Product Data

Certificate of Analysis

View CoA: current batch, Lot#A8T02K23

QC Data

View QC data: current batch, Lot#A8T02K23

Safety Data Sheet (SDS)

View Safety Data Sheet (SDS)

Instruction

View handling instruction

Biological target:

S3I-201 is a Stat3 inhibitor with an IC50 of 86 μM.

In vitro activity:

S3I-201 has the potential to mitigate fibrosis in a cellular context, making it relevant for studying conditions like lupus nephritis. S3I-201 was used in cell culture experiments to suppress the activation of STAT3, which had therapeutic effects by attenuating fibrotic changes in cultured HK-2 cells. Specifically, it reduced the expression of fibrosis-related proteins while improving the expression of E-cadherin. Reference: Int J Biochem Cell Biol. 2021 May;134:105950. https://pubmed.ncbi.nlm.nih.gov/33609746/

In vivo activity:

This study investigated the role of S3I-201 in experimental autoimmune encephalomyelitis (EAE), a model of MS. The severity of clinical scores decreased in S3I-201-treated EAE mice compared to vehicle-treated EAE mice. S3I-201 may have novel therapeutic potential against MS. Reference: Mult Scler Relat Disord. 2023 May;73:104658. https://pubmed.ncbi.nlm.nih.gov/36989705/

	Solvent	mg/mL	mM
Solubility
	DMF	12.5	34.20
	DMSO	16.0	43.80

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 365.36 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

1. Yuan C, Ni L, Wu X. Activin A activation drives renal fibrosis through the STAT3 signaling pathway. Int J Biochem Cell Biol. 2021 May;134:105950. doi: 10.1016/j.biocel.2021.105950. Epub 2021 Feb 17. PMID: 33609746. 2. Cheng Z, Lei Z, Yang P, Si A, Xiang D, Tang X, Guo G, Zhou J, Hüser N. Exosome-transmitted p120-catenin suppresses hepatocellular carcinoma progression via STAT3 pathways. Mol Carcinog. 2019 Aug;58(8):1389-1399. doi: 10.1002/mc.23022. Epub 2019 Apr 17. PMID: 30997702. 3. Ahmad SF, Ansari MA, Nadeem A, Bakheet SA, Al-Mazroua HA, Alomar HA, Al-Hamamah MA, Attia SM. S3I-201, a selective stat3 inhibitor, ameliorates clinical symptoms in a mouse model of experimental autoimmune encephalomyelitis through the regulation of multiple intracellular signalling in Th1, Th17, and treg cells. Mult Scler Relat Disord. 2023 May;73:104658. doi: 10.1016/j.msard.2023.104658. Epub 2023 Mar 23. PMID: 36989705. 4. Du Y, Zhang W, Liu S, Feng X, Gao F, Liu Q. S3I-201 ameliorates tubulointerstitial lesion of the kidneys in MRL/lpr mice. Biochem Biophys Res Commun. 2018 Sep 3;503(1):177-180. doi: 10.1016/j.bbrc.2018.05.207. Epub 2018 Jun 11. PMID: 29885836.

In vitro protocol:

In vivo protocol:

1. Ahmad SF, Ansari MA, Nadeem A, Bakheet SA, Al-Mazroua HA, Alomar HA, Al-Hamamah MA, Attia SM. S3I-201, a selective stat3 inhibitor, ameliorates clinical symptoms in a mouse model of experimental autoimmune encephalomyelitis through the regulation of multiple intracellular signalling in Th1, Th17, and treg cells. Mult Scler Relat Disord. 2023 May;73:104658. doi: 10.1016/j.msard.2023.104658. Epub 2023 Mar 23. PMID: 36989705. 2. Du Y, Zhang W, Liu S, Feng X, Gao F, Liu Q. S3I-201 ameliorates tubulointerstitial lesion of the kidneys in MRL/lpr mice. Biochem Biophys Res Commun. 2018 Sep 3;503(1):177-180. doi: 10.1016/j.bbrc.2018.05.207. Epub 2018 Jun 11. PMID: 29885836.

1: Shen C, Wu N, Chen X, Peng J, Feng M, Wang J, Yu Y. Interleukin-5 alleviates cardiac remodelling via the STAT3 pathway in angiotensin II-infused mice. J Cell Mol Med. 2024 Jul;28(13):e18493. doi: 10.1111/jcmm.18493. PMID: 38963241; PMCID: PMC11223166. 2: Liu H, Yan R, Xiao Z, Huang X, Yao J, Liu J, An G, Ge Y. Targeting DCLK1 attenuates tumor stemness and evokes antitumor immunity in triple-negative breast cancer by inhibiting IL-6/STAT3 signaling. Breast Cancer Res. 2023 Apr 17;25(1):43. doi: 10.1186/s13058-023-01642-3. PMID: 37069669; PMCID: PMC10108533. 3: Ji N, Wu L, Shi H, Li Q, Yu A, Yang Z. VSIG4 Attenuates NLRP3 and Ameliorates Neuroinflammation via JAK2-STAT3-A20 Pathway after Intracerebral Hemorrhage in Mice. Neurotox Res. 2022 Feb;40(1):78-88. doi: 10.1007/s12640-021-00456-5. Epub 2022 Jan 11. PMID: 35013905. 4: Xu J, Lin H, Wu G, Zhu M, Li M. IL-6/STAT3 Is a Promising Therapeutic Target for Hepatocellular Carcinoma. Front Oncol. 2021 Dec 15;11:760971. doi: 10.3389/fonc.2021.760971. PMID: 34976809; PMCID: PMC8714735. 5: Chen B, Yang Y, Wu J, Song J, Lu J. microRNA-17-5p downregulation inhibits autophagy and myocardial remodelling after myocardial infarction by targeting STAT3. Autoimmunity. 2022 Feb;55(1):43-51. doi: 10.1080/08916934.2021.1992754. Epub 2021 Nov 10. PMID: 34755577. 6: Albadrani GM, Binmowyna MN, Bin-Jumah MN, El-Akabawy G, Aldera H, Al-Farga AM. Quercetin protects against experimentally-induced myocardial infarction in rats by an antioxidant potential and concomitant activation of signal transducer and activator of transcription 3. J Physiol Pharmacol. 2020 Dec;71(6). doi: 10.26402/jpp.2020.6.11. Epub 2021 Apr 22. PMID: 33901998. 7: He Y, Fan Z, He L, Zhang C, Ping F, Deng M, Liu S, Wang Y, Cheng B, Xia J. Metformin Combined with 4SC-202 Inhibited the Migration and Invasion of OSCC via STAT3/TWIST1. Onco Targets Ther. 2020 Oct 29;13:11019-11029. doi: 10.2147/OTT.S268851. PMID: 33149616; PMCID: PMC7605634. 8: Liang W, Li J, Bai C, Chen Y, Li Y, Huang G, Wang X. Interleukin-5 deletion promotes sepsis-induced M1 macrophage differentiation, deteriorates cardiac dysfunction, and exacerbates cardiac injury via the NF-κB p65 pathway in mice. Biofactors. 2020 Nov;46(6):1006-1017. doi: 10.1002/biof.1681. Epub 2020 Oct 11. PMID: 33043521. 9: Wang C, Liu N, Yang HT. Desflurane pretreatment can reduce sepsis-evoked lung injury in rats via inhibiting STAT3 pathway. J Biol Regul Homeost Agents. 2020 May-Jun;34(3):935-942. doi: 10.23812/20-173-A-48. PMID: 32693566. 10: Yang Y, Xu C, Tang S, Xia Z. Interleukin-9 Aggravates Isoproterenol-Induced Heart Failure by Activating Signal Transducer and Activator of Transcription 3 Signalling. Can J Cardiol. 2020 Nov;36(11):1770-1781. doi: 10.1016/j.cjca.2020.01.011. Epub 2020 Jan 24. PMID: 32621886. 11: Sugimoto K, Hayashi Y. The Characteristics of Human iPS Cells and siRNA Transfection Under Hypoxia. Methods Mol Biol. 2022;2454:657-664. doi: 10.1007/7651_2020_299. PMID: 32567017. 12: Yang Y, Tang S, Zhai C, Zeng X, Liu Q, Xu C, Chen H. Interleukin-9 Deletion Relieves Vascular Dysfunction and Decreases Blood Pressure via the STAT3 Pathway in Angiotensin II-Treated Mice. Mediators Inflamm. 2020 Feb 14;2020:5741047. doi: 10.1155/2020/5741047. Erratum in: Mediators Inflamm. 2020 Oct 30;2020:8537832. doi: 10.1155/2020/8537832. PMID: 32148441; PMCID: PMC7042522. 13: Shi L, Ji Q, Liu L, Shi Y, Lu Z, Ye J, Zeng T, Xue Y, Yang Z, Liu Y, Lu J, Huang X, Qin Q, Li T, Lin YZ. IL-22 produced by Th22 cells aggravates atherosclerosis development in ApoE-/- mice by enhancing DC-induced Th17 cell proliferation. J Cell Mol Med. 2020 Mar;24(5):3064-3078. doi: 10.1111/jcmm.14967. Epub 2020 Feb 5. PMID: 32022386; PMCID: PMC7077608. 14: Ho Y, Wu CY, Chin YT, Li ZL, Pan YS, Huang TY, Su PY, Lee SY, Crawford DR, Su KW, Chiu HC, Shih YJ, Changou CA, Yang YSH, Whang-Peng J, Chen YR, Lin HY, Mousa SA, Davis PJ, Wang K. NDAT suppresses pro-inflammatory gene expression to enhance resveratrol-induced anti-proliferation in oral cancer cells. Food Chem Toxicol. 2020 Feb;136:111092. doi: 10.1016/j.fct.2019.111092. Epub 2019 Dec 26. PMID: 31883986. 15: Chen YR, Chen YS, Chin YT, Li ZL, Shih YJ, Yang YSH, ChangOu CA, Su PY, Wang SH, Wu YH, Chiu HC, Lee SY, Liu LF, Whang-Peng J, Lin HY, Mousa SA, Davis PJ, Wang K. Thyroid hormone-induced expression of inflammatory cytokines interfere with resveratrol-induced anti-proliferation of oral cancer cells. Food Chem Toxicol. 2019 Oct;132:110693. doi: 10.1016/j.fct.2019.110693. Epub 2019 Jul 20. PMID: 31336132. 16: Jahangiri A, Dadmanesh M, Ghorban K. Suppression of STAT3 by S31-201 to reduce the production of immunoinhibitory cytokines in a HIF1-α-dependent manner: a study on the MCF-7 cell line. In Vitro Cell Dev Biol Anim. 2018 Dec;54(10):743-748. doi: 10.1007/s11626-018-0299-6. Epub 2018 Oct 12. PMID: 30315441. 17: Chang Y, Cui M, Fu X, Zhang L, Li X, Li L, Wu J, Sun Z, Zhang X, Li Z, Nan F, Yan J, Zhang M. MiRNA-155 regulates lymphangiogenesis in natural killer/T-cell lymphoma by targeting BRG1. Cancer Biol Ther. 2019;20(1):31-41. doi: 10.1080/15384047.2018.1504721. Epub 2018 Oct 9. PMID: 30299211; PMCID: PMC6343692. 18: Sugimoto K, Matsuura T, Nakazono A, Igawa K, Yamada S, Hayashi Y. Effects of hypoxia inducible factors on pluripotency in human iPS cells. Microsc Res Tech. 2018 Jul;81(7):749-754. doi: 10.1002/jemt.23032. Epub 2018 Apr 6. PMID: 29633433. 19: Xu X, Zhi T, Chao H, Jiang K, Liu Y, Bao Z, Fan L, Wang D, Li Z, Liu N, Ji J. ERK1/2/mTOR/Stat3 pathway-mediated autophagy alleviates traumatic brain injury-induced acute lung injury. Biochim Biophys Acta Mol Basis Dis. 2018 May;1864(5 Pt A):1663-1674. doi: 10.1016/j.bbadis.2018.02.011. Epub 2018 Feb 18. Erratum in: Biochim Biophys Acta Mol Basis Dis. 2018 Jun;1864(6 Pt A):2214. doi: 10.1016/j.bbadis.2018.04.003. PMID: 29466698. 20: Hu Z, Luo D, Wang D, Ma L, Zhao Y, Li L. IL-17 Activates the IL-6/STAT3 Signal Pathway in the Proliferation of Hepatitis B Virus-Related Hepatocellular Carcinoma. Cell Physiol Biochem. 2017;43(6):2379-2390. doi: 10.1159/000484390. Epub 2017 Oct 27. PMID: 29073625.