581810

(-)-Terreic Acid, Synthetic

a cell-permeable quinone epoxide antibiotic

• 同義詞: (-)-Terreic Acid, Synthetic, (1R,6S)-3-Hydroxy-4-methyl-7-oxabicyclo[4.1.0]hept-3-ene-2,5-dione, BTK Inhibitor II, Bruton′s Tyrosine Kinase Inhibitor II
• 經驗公式（希爾表示法）: C₇H₆O₄
• CAS號碼: 121-40-4
• 分子量：: 154.12
• 分類程式碼代碼: 12352200

屬性

• 品質等級: 100
• 化驗: ≥98% (HPLC)
• 形狀: solid
• 製造商／商標名: Calbiochem^®
• 儲存條件: OK to freeze; protect from light
• 顏色: light beige
• 溶解度: water: 5 mg/mL
• 運輸包裝: wet ice
• 儲存溫度: −20°C
• InChI: 1S/C7H6O4/c1-2-3(8)5(10)7-6(11-7)4(2)9/h6-8H,1H3/t6-,7+/m1/s1
• InChI 密鑰: ATFNSNUJZOYXFC-RQJHMYQMSA-N

描述

一般說明

A cell-permeable quinone epoxide antibiotic that acts as a reversible, substrate competitive, and selective inhibitor of Bruton′s tyrosine kinase (BTK; IC₅₀ = 10 µM and 3 µM for the basal and activation levels), both in vitro and in vivo. Shown to bind to the BTK pleckstrin homology domain (BTK-PH) and block the interaction between BTK-PH and protein kinase C (PKC) (IC₅₀ ~100 µM in human mast cell lysates), thus affecting the catalytic activity of BTK, but not the activity of PKC. Selectively inhibits the autophosphorylation of PKC_βI (IC₅₀ ~8 µM) but not that of PKC_βII. Reported to effectively inhibit the production of TNF-α (IC₅₀ ~3 µM) and block the activation of JNK1 (IC₅₀ ~10 µM) in FcεRI-stimulated mast cells. Also reported to inhibit DNA synthesis in activated spleen cells (IC₅₀ ~1.5 µM). Does not significantly affect the activities of Lyn, Syk, PKA, CK-1, ERK1, ERK2 and p38 kinases.

生化／生理作用

Cell permeable: yes

Primary Target
Bruton′s tyrosine kinase catalytic activity (BTK)

Product competes with ATP.

Reversible: yes

Target IC₅₀: 10 µM against BTK

包裝

Packaged under inert gas

警告

Toxicity: Harmful (C)

重構

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

其他說明

Kawakami, Y., et al. 2000. Proc. Natl. Acad. Sci. USA97, 7423.
Kawakami, Y., et al. 1999. Proc. Natl. Acad. Sci. USA96, 2227.
Yamamoto, H., et al. 1980. Jpn. J. Antibiot.33, 320.

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 3
• 閃點（°F）: Not applicable
• 閃點（°C）: Not applicable