Kahalalide F 

Kahalalide F is a novel antitumor agent of marine origin. Kahalalide F can inhibit DNA synthesis. Kahalalide F cytotoxicity did not correlate with the expression level of the multidrug resistance MDR1 and of the tyrosine kinase HER2/NEU, and only slightly by the anti-apoptotic BCL-2 protein. Kahalalide F inhibits the PI3K-Akt signaling pathway by depleting ErbB3. Kahalalide F action was triggered rapidly by short pulse treatments. Kahalalide F induces cell death via oncosis preferentially in tumor cells. Kahalalide F can be used for the study of prostate cancer, breast cancer, vulval cancer, and non-small cell lung cancer^[1][2][3].

Kahalalide F (1 μM, 1 小时) 可引起 PC3 和 SKBR-3 细胞发生显著的形态学变化，包括严重的细胞质肿胀和空泡化，但未观察到明显的核破裂^[1]。
Kahalalide F (0.1-10 μM，24 小时) 对前列腺癌细胞 (PC3 (IC₅₀ = 0.07 μM)、DU145 (IC₅₀ = 0.18 μM)、LNCaP (IC₅₀ = 0.26 μM)) 和乳腺癌细胞 (SKBR-3 (IC₅₀ = 0.23 μM)、MCF7 (IC₅₀ = 0.28 μM)、BT474 (IC₅₀ = 0.26 μM)) 的 DNA 合成表现出剂量依赖性抑制作用，表明其具有强效的细胞毒性^[1]。
Kahalalide F (0.5-1 μM，0-24 小时) 即使在短时脉冲暴露下也对 PC3 细胞具有细胞毒性，因为 45 分钟的处理与 24 小时的处理一样能降低细胞存活率，而 15 分钟的处理则达到了半数最大效应^[1]。
Kahalalide F (0.25-0.5 μM, 0-48 h) 诱导的 PC3 细胞细胞毒性不需要基因表达或 caspase 活性，也不会引起细胞周期阻滞或 DNA 降解^[1]。
Kahalalide F (0.25-0.5 μM, 0-24 h) 可导致 PC3 细胞线粒体膜电位快速短暂丧失 (绿色荧光增强，红色荧光减弱) ，随后在 24 小时后出现高自发荧光碎片，并破坏溶酶体完整性^[1]。
Kahalalide F (0.5 μM) 可诱导内质网微囊泡的形成和破坏，并维持核膜完整性。在 PC3 细胞中观察到染色质凝聚成不规则聚集体，但未形成凋亡小体[1]。 Kahalalide F 对白色念珠菌 ATCC 90028 (IC₅₀ = 3.02 μM)、新型隐球菌 ATCC 90113 (IC₅₀ = 1.53 μM) 和烟曲霉 ATCC 90906 (IC₅₀ = 3.21 μM) 具有抗真菌活性^[2]。
Kahalalide F的体外细胞毒性以 ErbB3 蛋白表达为关键决定因素^[3]。
Kahalalide F (1 μM，4 h) 可选择性下调敏感的、高 ErbB3 表达的 SKBR3 细胞中的 ErbB3 表达^[3]。
Kahalalide F (1-2 μM，4-72 h) 对 H460 细胞表现出增强的细胞毒性，并伴有外源性抑制。ErbB3 表达，使细胞更加敏感，并显著降低 IC₅₀ 值 (从 4.7 μM 降至 3.1 μM)^[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

1477.87

C₇₅H₁₂₄N₁₄O₁₆

149204-42-2

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Suárez Y, et al. Kahalalide F, a new marine-derived compound, induces oncosis in human prostate and breast cancer cells. Mol Cancer Ther. 2003 Sep;2(9):863-72.  [Content Brief]

  [2]. Shilabin AG, Hamann MT. In vitro and in vivo evaluation of select kahalalide F analogs with antitumor and antifungal activities. Bioorg Med Chem. 2011 Nov 15;19(22):6628-32.  [Content Brief]

  [3]. Janmaat ML, et al. Kahalalide F induces necrosis-like cell death that involves depletion of ErbB3 and inhibition of Akt signaling. Mol Pharmacol. 2005 Aug;68(2):502-10.  [Content Brief]