S3I-201
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
- 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
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
Uses
S2I-201 is a small molecule inhibitor that provides a pathway to rational combination therapies for Melanoma.
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-201Supplier
- Tel
- 021-38015121 15000105423
- wulan@absin.cn
- Tel
- sales@boylechem.com
- Tel
- 010-82848833 400-666-7788
- jkinfo@jkchemical.com
- Tel
- +86-21-20908456
- sales@BioChemBest.com
- Tel
- +86 (531) 88811783
- sales@trio-pharmatech.com (International market)
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