Chelerythrine Chloride

产品编号：CST-11916S 品牌：CST 原厂货号：11916S
产品分类：生化试剂 > 生物试剂 > 生物活性小分子 > 抑制剂
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包装：

运保温度:

-20°C

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描述：

提供白屈菜赤碱氯化物（Chelerythrine Chloride）冻干粉。将5mg冻干粉溶于1.30ml DMSO，作为10 mM储存液。工作浓度和处理时间长短，取决于期望得到的效果，但通常在用刺激物处理之前，使用1-20μM浓度预处理15分钟至1小时，或单独使用最长长达24小时的不同处理时间。

白屈菜赤碱（Chelerythrine）是一种苯菲生物碱，可引了广泛的生物学反应。最初是作为一种有效的蛋白激酶C抑制剂（IC 50=660 nm）发现，通过与催化结构域的相互作用，与磷酸受体竞争，不与ATP竞争（1），并通常被作为一种研究抑制PKC活化的手段（2-4）。然而，随后的研究表明，白屈菜赤碱并不是一种强有力的PKC抑制剂，且其效果不依赖于PKC的抑制作用(5,6)。研究人员已经证明，白屈菜赤碱通过氧化应激机制激活JNK和p38（6），通过抑制Bcl-xL-Bak BH3肽段结合(IC50 = 1.5 μM)破坏Bcl-xL 和 Bax的相互作用抑制Bcl-xL (7)，诱导凋亡(6-8)。

原厂资料：

Directions for Use

Chelerythrine Chloride is supplied as a lyophilized powder. For a 10 mM stock, reconstitute the 5 mg in 1.30 ml DMSO. Working concentrations and length of treatment can vary depending on the desired effect, but it is typically used at 1-20 µM either as a pretreatment for 15 min-1 hr prior to treating with a stimulator or used alone with varying treatment times lasting up to 24 hr.

Background

Chelerythrine is a benzophenanthridine alkaloid that elicits a wide range of biological responses. It was initially reported to be a potent PKC inhibitor (IC50 = 660 nM) through interaction with the catalytic domain, competitive with respect to the phosphate acceptor, noncompetitive with respect to ATP (1), and is often used in research as a means to inhibit PKC activation (2-4). However, subsequent studies have shown that chelerythrine is not a potent PKC inhibitor and its effects are independent of PKC inhibition (5,6). Researchers have demonstrated that chelerythrine activates JNK and p38 through an oxidative stress mechanism (6), inhibits Bcl-xL by preventing Bcl-xL-Bak BH3 peptide binding (IC50 = 1.5 μM) and disrupting the interaction between Bcl-xL and Bax (7), and induces apoptosis (6-8).

注意事项：

Storage: Store lyophilized or in solution at -20°C, desiccated. Protect from light. In lyophilized form, the chemical is stable for 24 months. Once in solution, use within 3 months to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.