Millipore Sigma Vibrant Logo
Attention: We have moved. Merck Millipore products are no longer available for purchase on MerckMillipore.com.Learn More

530750 STAT3 Inhibitor XX, APTSTAT3-9R - Calbiochem

A cell-permeable, 26-mer peptide (APTSTAT3) that binds to STAT3 with high affinity (Kd = 231 nM) and blocks its DNA binding activity.

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

同义词: H₂N-HGFQWPG(SWTWENGKWTWK)GAYQFLK-GGGGS-RRRRRRRRR-CO₂H

Primary Target: STAT3
530750
Purchase on Sigma-Aldrich

概述

Replacement Information

重要规格表

Empirical Formula
C₂₂₃H₃₃₀N₈₀O₅₁

Products

产品目录编号包装 数量 / 包装
5.30750.0001 玻璃瓶 5 mg
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
Global Trade Item Number
产品目录编号 GTIN
5.30750.0001 04055977283228

Documentation

STAT3 Inhibitor XX, APTSTAT3-9R - Calbiochem MSDS

职位

物料安全数据表 (MSDS) 

参考

参考信息概述
Kim, D., et al. 2014. Cancer Res. 74, 2144.
数据表

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 Protect from light
+2°C to +8°C
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.
Toxicity Standard Handling
ReferencesKim, D., et al. 2014. Cancer Res. 74, 2144.