WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 202541
Description: 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.
MedKoo Cat#: 202541
Chemical Formula: C16H15NO7S
Exact Mass: 365.05692
Molecular Weight: 365.36
Elemental Analysis: C, 52.60; H, 4.14; N, 3.83; O, 30.65; S, 8.78
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, not soluble in water.
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
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|
1. Pang M, Ma L, Gong R, Tolbert E, Mao H, Ponnusamy M, Chin YE, Yan H, Dworkin LD, Zhuang S. A novel STAT3 inhibitor, S3I-201, attenuates renal interstitial fibroblast activation and interstitial fibrosis in obstructive nephropathy. Kidney Int. 2010 Aug;78(3):257-68. Epub 2010 Jun 2. PubMed PMID: 20520592.
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