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Cat. No. M3219
S3I-M2001 Structure
Size Price Availability
5mg USD 170 Custom Synthesis
10mg USD 300 Custom Synthesis
50mg USD 780 Custom Synthesis
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

S3I-M2001 is a novel small-molecule Stat3 inhibitor with IC50 of 79, 92 and 159 uM for Stat3:Stat3, Stat1:Stat3 and Stat1:Stat1, respectively. S3I-M2001 is designed to be an oxazole-based peptidomimetic of the Stat3 Src homology (SH) 2 domain-binding phosphotyrosine peptide that selectively disrupts active Stat3:Stat3 dimers. As a result, hyperactivated Stat3, which hitherto occurs as "dotlike" structures of nuclear bodies, undergoes an early aggregation into nonfunctional perinuclear aggresomes and a late-phase proteasome-mediated degradation in malignant cells treated with S3I-M2001. S3I-M2001 favorably disrupts Stat3 activity in vitro in nuclear extracts containing activated Stat3 or in lysates from Sf-9 cells containing activated Stat3, and preferentially inhibits Stat3 activity over Stat1 by 2-fold. Therefore, S3I-M2001 inhibited Stat3-dependent transcriptional regulation of tumor survival genes, such as Bcl-xL. Furthermore, S3I-M2001 prevented constitutive Stat3 Tyr phosphorylation and activation in the NIH3T3/v-Src and the human breast cancer MDA-MB-231 and MDA-MB-435 cell lines that harbor constitutively active Stat3. Stat3-dependent malignant transformation, survival, and migration and invasion of mouse and human cancer cells harboring persistently activated Stat3 were inhibited by S3I-M2001. In addition, S3I-M2001 prevented growth of human breast tumor xenografts.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 508.5
Formula C27H29N2O6P
CAS Number 1003580-86-6
Purity >98%
Solubility DMSO
Storage at -20°C
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Keywords: S3I-M2001 supplier, STAT, inhibitors

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