| Identification | Back Directory | [Name]
S3I-201 | [CAS]
501919-59-1 | [Synonyms]
CS-450
106202
S31-201
S3I-201
S2I-201
NSC 74859
S3I-201, >98%
NSC 74859, >=98%
S3I-201 USP/EP/BP
NSC 74859(S31-201)
OTAVA-BB 7070707021
S31-201 (NSC 74859)
NSC 74859 (S3I-201)
S3I-201 (NSC 74859)
S3I-201, 501919-59-1
Stat3 Inhibitor I, S3I-201
Stat3 Inhibitor VI, S3I-201
S3I201; NSC74859; NSC 74859; S3I 201
S3I201; NSC74859; NSC 74859;NSC-74859; S3I 201
OTAVA-BB 7070707021S31-201 (NSC 74859)，S3I-201
2-hydroxy-4-(2-(tosyloxy)acetaMido)benzoic acid
STAT3 Inhibitor VI, S3I-201 - CAS 501919-59-1 - Calbiochem
2-Hydroxy-4-[[[[(4-methylphenyl)sulfonyl]oxy]acetyl]amino]-benzoic acid
2-Hydroxy-4-[[2-[[(4-methylphenyl)sulfonyl]oxy]acetyl]amino]benzoic acid
Benzoic acid, 2-hydroxy-4-[[2-[[(4-methylphenyl)sulfonyl]oxy]acetyl]amino]-
2-Hydroxy-4-[[2-[[(4-methylphenyl)sulfonyl]oxy]acetyl]amino]benzoic acid NSC 74859(S3I-201) | [Molecular Formula]
C16H15NO7S | [MDL Number]
MFCD09907564 | [MOL File]
501919-59-1.mol | [Molecular Weight]
365.358 |
| Chemical Properties | Back Directory | [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 |
| Hazard Information | Back Directory | [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. | [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]
Store at -20°C,unstable in solution, ready to use. | [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. |
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