5.30750

STAT3 Inhibitor XX, APT _STAT3-9R

• 同義詞: STAT3 Inhibitor XX, APT _STAT3-9R, H₂N- HGFQWPG(SWTWENGKWTWK)G AYQFLK-GGGGS-RRRRRRRRR-CO₂H
• 經驗公式（希爾表示法）: C₂₂₃H₃₃₀N₈₀O₅₁
• 分子量：: 4947.51
• 分類程式碼代碼: 12352200
• NACRES: NA.77

屬性

• 化驗: ≥95% (HPLC)
• 品質等級: 100
• 形狀: solid
• 製造商／商標名: Calbiochem^®
• 儲存條件: OK to freeze; desiccated (hygroscopic); protect from light
• 顏色: white
• 溶解度: H₂O: 50 mg/mL
• 儲存溫度: 2-8°C

描述

一般說明

A cell-permeable STAT3 inhibiting peptide that corresponds to the high affinity STAT3-interacting aptide APT_STAT3 (K_D = 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 APT_STAT3 affinity is mediated via STAT2 SH2 domain interaction and only moderate affinity is detected toward DNA-binding domain (DBD).

A cell-permeable, 26-mer peptide (APT_STAT3) that binds to STAT3 with high affinity (K_d = 231 nM) and blocks its DNA binding activity.

生化／生理作用

Cell permeable: yes

Primary Target
STAT3

警告

Toxicity: Standard Handling (A)

序列

H-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

外觀

Supplied as a trifluoroacetate salt.

重構

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

其他說明

Kim, D., et al. 2014. Cancer Res.74, 2144.

法律資訊

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

安全資訊

• 儲存類別代碼: 11 - Combustible Solids
• 水污染物質分類（WGK）: WGK 1
• 閃點（°F）: Not applicable
• 閃點（°C）: Not applicable