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HomeProduct name listS3I-201

S3I-201

Synonym(s):2-Hydroxy-4-(((4-methylphenyl)sulfonyloxy)acetyl)amino)-benzoic acid, NSC 74859;2-Hydroxy-4-[[[[(4-methylphenyl)sulfonyl]oxy]acetyl]amino]-benzoic acid;NSC 74859;STAT3 Inhibitor VI, S3I-201 - CAS 501919-59-1 - Calbiochem

S3I-201 Structural

What is S3I-201?

The Uses of S3I-201

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

The Uses of S3I-201

A chemical probe inhibitor of STAT3 with an IC50 of 86 μM.

The Uses of S3I-201

S2I-201 is a small molecule inhibitor that provides a pathway to rational combination therapies for Melanoma.

What are the applications of Application

Stat3 Inhibitor VI, S3I-201 is an inhibitor of Stat3 phosphorylation and dimerization

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.

Properties of S3I-201

Melting point: >185oC (dec.)
Boiling point: 654.7±55.0 °C(Predicted)
Density  1.507
storage temp.  -20°C
solubility  DMSO: >10mg/mL
form  powder
pka 2.98±0.10(Predicted)
color  white to beige

Safety information for S3I-201

Signal word Warning
Pictogram(s)
ghs
Exclamation Mark
Irritant
GHS07
GHS Hazard Statements H302:Acute toxicity,oral
H315:Skin corrosion/irritation
H319:Serious eye damage/eye irritation
Precautionary Statement Codes P264:Wash hands thoroughly after handling.
P264:Wash skin thouroughly after handling.
P270:Do not eat, drink or smoke when using this product.
P280:Wear protective gloves/protective clothing/eye protection/face protection.
P302+P352:IF ON SKIN: wash with plenty of soap and water.
P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
P332+P313:IF SKIN irritation occurs: Get medical advice/attention.
P337+P313:IF eye irritation persists: Get medical advice/attention.

Computed Descriptors for S3I-201

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