G?6976

• 产品编号：CST-12060S      品牌：CST       原厂货号：12060S
• 产品分类：生化试剂 > 生物试剂 > 生物活性小分子 > 抑制剂
• 应用分类：

描述：

提供的Gö6976为冻干粉。对于1mM浓度贮存液，在500 µg冻干粉中加入1.32 ml DMSO。工作浓度和处理时间根据所需的预期效果来确定，一般在用兴奋剂处理前，以0.1-10 µM，处理0.5-1 小时或者单独使用，能作用不同的时间，可持续作用24小时。能溶于DMSO（25 mg/ml），很难溶于乙醇和水，在水中的最大溶解度约为1-5µM。这是一种ATP竞争性PKC抑制剂，特异性针对Ca2+依赖的PKCα (IC50 = 2.3 nM)和PKCβ1 (IC50 = 6.2 nM)同工酶（1）。它也是一种有效的PKD (IC50 = 20 nM)抑制剂（2）。研究者已经证明Gö6976能阻断JNK活化（3-5）和抑制Ser133上PKCα介导的，TPA刺激的CREB的磷酸化（6,7）。Gö6976也是酪氨酸激酶Jak2和FLT3（8）以及TrkA和TrkB的有效抑制剂（9）。

原厂资料：

Molecular Characterization

C24H18N4O

Purity

>99%

Directions for Use

Gö6976 is supplied as a lyophilized powder. For a 1 mM stock, reconstitute the 500 µg in 1.32 ml DMSO. Working concentrations and length of treatment can vary depending on the desired effect, but it is typically used as a pretreatment at 0.1-10 µM for 0.5-1 hr prior to treating with a stimulator or is used alone with varying treatment times lasting up to 24 hr. Soluble in DMSO at 25 mg/ml; very poorly soluble in ethanol and water with maximum solubility in water at ~1-5 µM.

Background

Gö6976 is an ATP-competitive PKC inhibitor specific for Ca2+-dependent PKCα (IC50 = 2.3 nM) and PKCβ1 (IC50 = 6.2 nM) isozymes (1). It is also a potent inhibitor of PKD (IC50 = 20 nM) (2). Researchers have demonstrated that Gö6976 blocks JNK activation (3-5) and inhibits PKCα-mediated, TPA-stimulated phosphorylation of CREB at Ser133 (6,7). Gö6976 is also an effective inhibitor of the tyrosine kinases Jak2 and FLT3 (8), as well as TrkA and TrkB (9).

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