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530750 STAT3 Inhibitor XX, APTSTAT3-9R - Calbiochem

530750
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Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₂₂₃H₃₃₀N₈₀O₅₁

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      Glass bottle 5 mg
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      Description
      OverviewA cell-permeable, 26-mer peptide (APTSTAT3) with tryptophan zipper scaffold that forms a robust β-hairpin structure and binds to STAT3 with high affinity (Kd = 231 nM) and blocks its DNA binding activity. Its cell permeability is conferred by fusion of peptide to 9 arginine residues via a GGGGS linker. Selectively targets SH2 domain of STAT3 and disrupts STAT3-JAK2 interaction and STAT3 phosphorylation (Tyr705) and dimerization without affecting STAT1 and STAT5. Shown to effectively reduce mRNA levels of cyclin D1, Bcl-xL, and survivin in A549 cells and suppresses their viability and proliferation (~10-20 µM). Exerts antitumor properties in both xenograft (8 mg/kg, q.o.d., intratumorally) and allograft tumors in BABL/c nude mice and prolongs their survival. Note: Tryptophen zipper sequence in parentheses; STAT3-targeting sequence underlined.

      Please note that the molecular weight for this compound is batch-specific due to variable water content.
      Catalogue Number530750
      Brand Family Calbiochem®
      SynonymsH₂N-HGFQWPG(SWTWENGKWTWK)GAYQFLK-GGGGS-RRRRRRRRR-CO₂H
      References
      ReferencesKim, D., et al. 2014. Cancer Res. 74, 2144.
      Product Information
      FormWhite solid
      FormulationSupplied as a trifluoroacetate salt.
      Hill FormulaC₂₂₃H₃₃₀N₈₀O₅₁
      Chemical formulaC₂₂₃H₃₃₀N₈₀O₅₁
      Hygroscopic Hygroscopic
      ReversibleY
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetSTAT3
      Purity≥95% by HPLC
      Physicochemical Information
      Cell permeableY
      Peptide SequenceH-His-Gly-Phe-Gln-Trp-Pro-Gly-(Ser-Trp-Thr-Trp-Glu-Asn-Gly-Lys-Trp-Thr-Trp-Lys)-Gly-Ala-Tyr-Gln-Phe-Leu-Lys-Gly-Gly-Gly-Gly-Ser-Arg-Arg-Arg-Arg-Arg-Arg-Arg-Arg-Arg-OH
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      Storage and Shipping Information
      Ship Code Ambient Temperature Only
      Toxicity Standard Handling
      Storage +2°C to +8°C
      Protect from Light Protect from light
      Hygroscopic Hygroscopic
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      STAT3 Inhibitor XX, APTSTAT3-9R - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      References

      Reference overview
      Kim, D., et al. 2014. Cancer Res. 74, 2144.
      Data Sheet

      Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

      Revision31-July-2015 JSW
      SynonymsH₂N-HGFQWPG(SWTWENGKWTWK)GAYQFLK-GGGGS-RRRRRRRRR-CO₂H
      DescriptionA cell-permeable STAT3 inhibiting peptide that corresponds to the high affinity STAT3-interacting aptide APTSTAT3 (KD = 231 nM), originally identified by phage peptide library screening, with the addition of 9 arginines at the C-terminus via a GGGGS linker sequence. Reported to inhibit JAK2-catalyzed STAT3 phosphorylation in cell-free kinase assays and suppress cellular STAT3 phosphorylation as well as DNA-binding activity (by 54% post 6 h 30 µM treatment) in human lung carcinoma A549 cultures, resulting in downregulation of cell cycle progression regulator cyclin D1 and reduced expression of anti-apoptic survivin & Bcl-xL, while exhibiting little effect toward cellular phosphorylation levels of STAT1/5 and Akt. Shown to inhibit A549 proliferation (GI50 = 10 to 20 µM in 12 h by MTT assay; complete inhibition by 30 µM in 2-wk colony formation assay) via apoptosis induction (PI+/Annexin V+ population = 15% vs. 2.8% with or without 6 h 30 µM drug treatment) in vitro and intratumoral injection is efficacious in suppressing the growth of established tumors derived from B16F1 murine melanoma allograft as well as from human U87MG glioblastoma and A549 (8 mg/kg, q.o.d.) xenografts in mice in vivo. Binding study indicates that the majority of APTSTAT3 affinity is mediated via STAT2 SH2 domain interaction and only moderate affinity is detected toward DNA-binding domain (DBD).
      FormWhite solid
      FormulationSupplied as a trifluoroacetate salt.
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₂₂₃H₃₃₀N₈₀O₅₁
      Peptide SequenceH-His-Gly-Phe-Gln-Trp-Pro-Gly-(Ser-Trp-Thr-Trp-Glu-Asn-Gly-Lys-Trp-Thr-Trp-Lys)-Gly-Ala-Tyr-Gln-Phe-Leu-Lys-Gly-Gly-Gly-Gly-Ser-Arg-Arg-Arg-Arg-Arg-Arg-Arg-Arg-Arg-OH
      Purity≥95% by HPLC
      SolubilityH₂O (50 mg/ml)
      Storage +2°C to +8°C
      Hygroscopic
      Protect from light
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
      Toxicity Standard Handling
      ReferencesKim, D., et al. 2014. Cancer Res. 74, 2144.