S3I-201

SKU: orb1305381

Description

NSC 74859

Research Area

Signal Transduction, Stem Cell & Developmental Biology

Images & Validation

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Key Properties

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CAS Number	501919-59-1
MW	365.36
Purity	97.83%
Formula	C₁₆H₁₅NO₇S
SMILES	Cc1ccc(cc1)S(=O)(=O)OCC(=O)Nc1ccc(C(O)=O)c(O)c1
Target	STAT
Solubility	10% DMSO+40% PEG300+5% Tween 80+45% Saline:5 mg/mL (13.69 mM);DMSO:150 mg/mL (410.55 mM)

Bioactivity

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Target IC50	STAT3:86 nM (cell free)
In Vivo	Compared with control tumors, which continued to grow, human breast tumors in mice that received S3I-201 displayed strong growth inhibition. Strong inhibition of Stat3 DNA-binding activity in residual tumor tissue from mice treated with S3I-201 compared with control tumor . 8- to 10-wk-old p53nullCD45.1 mice were treated with S31-201 3×/wk at 5 mg/kg, using PBS-treated age-matched p53nullCD45.1 mice as controls. STAT3 phosphorylation in the spleen of S31-201-treated mice was markedly reduced as compared with those treated with PBS . S3I-201 attenuated somatotroph tumor growth and GH secretion in a rat xenograft model . Read more...
In Vitro	S3I-201 inhibits Stat3.Stat3 complex formation and Stat3 DNA-binding and transcriptional activities. Furthermore, S3I-201 inhibits growth and induces apoptosis preferentially in tumor cells that contain persistently activated Stat3. Constitutively dimerized and active Stat3C and Stat3 SH2 domain rescue tumor cells from S3I-201-induced apoptosis . Preincubation of CD4 T cells from p53(null)CD45.1 mice with various concentrations of S31-201 suppressed IL-6-induced phosphorylation of STAT3 in a dose-dependent manner as early as 15 min after IL-6 addition. Based on the level of suppression of STAT3 phosphorylation, the IC50 of this inhibitor was determined as 38 μM . Although none of these cell lines was sensitive to S3I-201 (S3I-201) alone, S3I-201 potentiated the antiproliferative effect of cetuximab in all three cell lines (HepG2, SK-HEP1, and Huh-7 cells) . Read more...
Cell Research	Proliferating cells were treated with or without S3I-201 for up to 48 h. In some cases, cells were first transfected with Stat3C, ST3-NT, or ST3-SH2 domain or mock-transfected for 24 h before treatment with compound for an additional 24–48 h. Cells were then detached and analyzed by annexin V binding according to the manufacturer's protocol and flow cytometry to quantify the percent apoptosis . Read more...
Animal Research	Six-week-old female athymic nude mice were purchased from Harlan and maintained in the institutional animal facilities approved by the American Association for Accreditation of Laboratory Animal Care. Athymic nude mice were injected in the left flank area s.c. with 5 × 10^6 human breast cancer MDA-MB-231 cells in 100 μl of PBS. After 5–10 days, tumors with a diameter of 3 mm were established. Animals were given S3I-201 i.v. at 5 mg/kg every 2 or 3 days for 2 weeks and monitored every 2 or 3 days. Animals were stratified so that the mean tumor sizes in all treatment were nearly identical. Tumor volume was calculated according to the formula V = 0.52 × a2× b, where a is the smallest superficial diameter and b is the largest superficial diameter . Read more...

Storage & Handling

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Storage	Powder: -20°C for 3 years \| Shipping with blue ice/Shipping at ambient temperature.
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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Inhibitor, inhibit, NSC 74859, NSC74859, NSC-74859, S3I 201, S3I201, STAT, STAT3

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Compound Identifiers

PubChem CID

252682 ↗

Key Properties

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No computed properties available.

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Purity:	>98%(HPLC)
CAS Number:	501919-59-1
MW:	365.4
Formula:	C₁₆H₁₅NO₇S

S3I-201

Description

Research Area

Images & Validation

Key Properties

Bioactivity

Storage & Handling

Alternative Names

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