S3I-201 (NSC 74859)

Alias: NSC 7485; S3I-201; NSC74859; S3I 20;NSC-74859; S3I201
Cat No.:V1378 Purity: ≥98%
S3I-201 (also called S3I201;NSC74859;S3I 201;NSC-74859) is a cell permeable and selective Stat3 inhibitor with potential anticancer activity.
S3I-201 (NSC 74859) Chemical Structure CAS No.: 501919-59-1
Product category: STAT
This product is for research use only, not for human use. We do not sell to patients.
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

S3I-201 (also called S3I201; NSC74859; S3I 201; NSC-74859) is a cell permeable and selective Stat3 inhibitor with potential anticancer activity. It inhibits Stat3 with an IC50 of 86±33 μM. S3I-201 shows potent inhibition of STAT3 DNA-binding activity with IC50 of 86 μM in cell-free assays, and exhibits low activity towards STAT1 and STAT5. 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.

Biological Activity I Assay Protocols (From Reference)
ln Vitro
Stat3 DNA-binding activity is preferentially inhibited by NSC 74859 (S3I-201) over Stat1 (IC50 values: Stat3•Stat3, 86±33 μM; Stat1•Stat3, 160±43 μM; and Stat1•Stat1, >300 μM), while Stat5 DNA-binding activity is inhibited with an IC50 of 166±17 μM). The proliferation of transformed mouse fibroblasts NIH 3T3/v-Src and breast carcinoma cell lines (MDA-MB-231, MDA-MB-435, and MDA-MB-468) is inhibited and the number of viable cells is dramatically reduced by NSC 74859. NSC 74859 significantly promotes apoptosis in the constitutively active Stat3-containing human breast cancer cell lines MDA-MB-435 and NIH 3T3/v-Src at concentrations between 30 and 100 μM. The MDA-MB-435 cell line exhibits increased sensitivity to 30 μM NSC 74859. On the other hand, the normal mouse fibroblasts (NIH 3T3) and the human breast cancer MDA-MB-453 cells are less sensitive to NSC 74859 at 100 μM or less because they do not exhibit aberrant Stat3 activation. NSC 74859 produced non-specific, overall cytotoxicity at 300 μM or above, regardless of Stat3 activation status[1]. Huh-7 cells, independent of CD133+ status, are susceptible to STAT3 inhibition and do not express β2SP or TBGFR2. The IC50 for NSC 74859 is 100 μM. In Huh-7 and SNU-398 cells, the IC50 of NSC 74859 is 150 μM; in SNU-475 and SNU-182 cells, it is 15 μM. With an IC50 near 100 μM, NSC 74859 inhibits the MDA-MB-435, MDA-MB-453, and MDA-MB-231 cell lines that are used to treat breast cancer[2].
ln Vivo
For two weeks, NSC 74859 (S3I-201) or a vehicle is injected intravenously (i.v.) into human breast (MDA-MB-231) tumor-bearing mice every two or three days. Tumor measurements are obtained every two to three days. Mice treated with S3I-201 for human breast cancers show significant growth suppression as compared to control (vehicle-treated) tumors, which did not stop growing. Following treatment termination, an ongoing assessment of the treated mice reveals no return of tumor growth, indicating that S3I-201 may have a long-lasting effect on tumor growth[1]. For the duration of the trial, S3I-201 treatment of somatotroph tumor xenografts (n=15) dramatically reduced tumor development in comparison with vehicle-treated control tumors (n=15), which kept growing. As early as five days following NSC 74859 injection, tumors derived from rats treated with NSC 74859 are significantly less than those from the untreated group (220±16 mm3 vs. 287±16 mm3, P<0.01). Rats treated with NSC 74859 had an average tumor volume that is 64% smaller than that of controls fifteen days after treatment (449±40 mm3 vs. 708±83 mm3, P<0.01). Fifteen days after the start of treatment, the rats are killed and the tumors are extracted. Rats treated with NSC 74859 had an average tumor weight of 78±8 mg, whereas tumors from control rats weighed 114±13 mg (32% reduction; P<0.05)[3].
Animal Protocol
Dissolved in DMSO; ≤5 mg/kg; i.v. injection
Human breast cancer MDA-MB-231 cells are injected s.c. into the left flank of athymic nu/nu mice.
References
[1]. Siddiquee K, et al. Selective chemical probe inhibitor of Stat3, identified through structure-based virtual screening, induces antitumor activity. Proc Natl Acad Sci U S A. 2007 May 1;104(18):7391-6.
[2]. Lin L, et al. The STAT3 inhibitor NSC 74859 is effective in hepatocellular cancers with disrupted TGF-β signaling. Oncogene. 2009 Feb 19;28(7):961-72.
[3]. Zhou C, et al. STAT3 upregulation in pituitary somatotroph adenomas induces hypersecretion. J Clin Invest. 2015 Apr;125(4):1692-702
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C16H15NO7S
Molecular Weight
365.36
CAS #
501919-59-1
SMILES
S(C1C([H])=C([H])C(C([H])([H])[H])=C([H])C=1[H])(=O)(=O)OC([H])([H])C(N([H])C1C([H])=C([H])C(C(=O)O[H])=C(C=1[H])O[H])=O
Synonyms
NSC 7485; S3I-201; NSC74859; S3I 20;NSC-74859; S3I201
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: 73 mg/mL (199.8 mM)
Water:<1 mg/mL
Ethanol:<1 mg/mL
Solubility (In Vivo)
5% DMSO, 95% PEG 300 :15 mg/mL
 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.7370 mL 13.6851 mL 27.3703 mL
5 mM 0.5474 mL 2.7370 mL 5.4741 mL
10 mM 0.2737 mL 1.3685 mL 2.7370 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

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Biological Data
  • S3I-201

    VZV infection directs STAT3 phosphorylation in human fibroblasts independently of secreted factors.Proc Natl Acad Sci U S A.2012 Jan 10;109(2):600-5.



    S3I-201

    Assessment of the effects of inhibiting STAT3 phosphorylation on VZV replication in skin xenografts in vivo.Proc Natl Acad Sci U S A.2012 Jan 10;109(2):600-5.
  • S3I-201

    Inhibition of STAT3 phosphorylation restricts VZV replication and spread in vitro.Proc Natl Acad Sci U S A.2012 Jan 10;109(2):600-5.
  • S3I-201

    Inhibition of STAT3 phosphorylation restricts VZV replication in skin in vivo.Proc Natl Acad Sci U S A.2012 Jan 10;109(2):600-5.

  • S3I-201

    STAT3 phosphorylation in VZV-infected skin in vivo.Proc Natl Acad Sci U S A.2012 Jan 10;109(2):600-5.


  • S3I-201

    VZV infection leads to up-regulation of survivin transcription and translation in vitro and in vivo.Proc Natl Acad Sci U S A.2012 Jan 10;109(2):600-5.
  • S3I-201

    Evaluation for effects of S3I-201 on STATs, Shc, Src, and Erks activation, and on Lck-SH2 domain phosphopeptide binding.Proc Natl Acad Sci U S A.2007 May 1;104(18):7391-6.
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