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S3I-201

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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
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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
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Safety Information

WGK Germany 
3
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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

Absin Bioscience Inc. Gold
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021-38015121 15000105423
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wulan@absin.cn
Shanghai Boyle Chemical Co., Ltd.
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sales@boylechem.com
J & K SCIENTIFIC LTD.
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010-82848833 400-666-7788
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jkinfo@jkchemical.com
Chembest Research Laboratories Limited
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+86-21-20908456
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sales@BioChemBest.com
Jinan Trio PharmaTech Co., Ltd.
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+86 (531) 88811783
Email
sales@trio-pharmatech.com (International market)