|
| | S3I-201 Basic information |
| Product Name: | S3I-201 | | Synonyms: | S31-201;2-hydroxy-4-(2-(tosyloxy)acetaMido)benzoic acid;NSC 74859 (S3I-201);NSC 74859;S3I-201;S3I-201 (NSC 74859);2-Hydroxy-4-[[2-[[(4-methylphenyl)sulfonyl]oxy]acetyl]amino]benzoic acid;S2I-201 | | CAS: | 501919-59-1 | | MF: | C16H15NO7S | | MW: | 365.36 | | EINECS: | | | Product Categories: | Inhibitors;JAK;STAT | | Mol File: | 501919-59-1.mol |  |
| | S3I-201 Chemical Properties |
| Melting point | >185oC (dec.) | | Boiling point | 654.7±55.0 °C(Predicted) | | density | 1.507 | | storage temp. | -20°C | | solubility | DMSO: >10mg/mL | | pka | 2.98±0.10(Predicted) | | form | powder | | color | white to beige |
| | S3I-201 Usage And Synthesis |
| Uses | A chemical probe inhibitor of STAT3 with an IC50 of 86 μM. | | Uses | S2I-201 is a small molecule inhibitor that provides a pathway to rational combination therapies for Melanoma. | | Uses | S3I-201 has been used as a signal transducer and activator of transcription 3 (STAT3) inhibitor:
- to confirm the role of STAT3 phosphorylation in interleukin (IL)-33 production in lung epithelial cells and IL-22 mRNA expression in sorted group 3 innate lymphoid cells (ILC3s)
- to study the cellular response of STAT3 triggered by β-hexaclorocyclohexane (β-HCH) in various cell lines
- to examine the influence of STAT3 in response to angiotensin II (ang II) on induction of fibrotic proteins in kidney epithelial cells
| | Definition | ChEBI: An amidobenzoic acid obtained by formal condensation of the carboxy group of [(4-methylbenzene-1-sulfonyl)oxy]acetic acid with the amino group of 4-amino-2-hydroxybenzoic acid. | | Biological Activity | s3i-201 is a selective inhibitor of stat3 with ic50 value of 86 μm [1].in the in vitro stat3 dna-binding assay, s3i-201 showed potent inhibition of the stat3 dna-binding activity with an average ic50 of 86 μm. in the emsa assay, s3i-201 selectively inhibited stat3 dna-binding activity over that of stat1 and stat5. it suppressed the complex formation of stat1-stat3 and stat1-stat1 with ic50 values of 160 and > 300 μm, respectively. besides that, the unphosphorylated, inactive stat3 monomer was found to restore the stat3 dna-binding activity inhibited by s3i-201, suggesting that the inhibition was independent on the activation status. in nih 3t3/v-src fibroblasts, s3i-201 inhibited the constitutive activation of stat3 and reduced the ptyr-705 stat3 levels. moreover, s3i-201 was found to significantly induce apoptosis in cells with constitutively active stat3 at concentration of 30–100 μm. s3i-201 also reduced the expression of cyclin d1, bcl-xl and surviving in these cells [1]. | | Biochem/physiol Actions | S3I-201 is a cell-permeable Stat3 inhibitor that binds to the Stat3-SH2 domain, prevents Stat3 phosphorylation/activation, dimerization, and DNA-binding. | | storage | -20°C | | references | [1] siddiquee k, zhang s, guida w c, et al. selective chemical probe inhibitor of stat3, identified through structure-based virtual screening, induces antitumor activity. proceedings of the national academy of sciences, 2007, 104(18): 7391-7396. |
| | S3I-201 Preparation Products And Raw materials |
|
