ケンパウロン 化学特性,用途語,生産方法
外観
白色〜褐色, 結晶〜粉末
溶解性
メタノールに溶ける。
使用上の注意
不活性ガス封入
化学的特性
Tan Solid
使用
The paullones are a novel class of kinase inhibitors, initially identified as CDK inhibitors. Kenpaullone has been found to be a useful GSK-3?inhibitor (IC50=23nM).
一般的な説明
A potent, cell-permeable, and reversible inhibitor of glycogen synthase kinase-3β (IC
50 = 230 nM), Lck (IC
50 = 470 nM), and cyclin-dependent kinases (Cdks). Inhibits Cdk1/cyclin B (IC
50 = 400 nM), Cdk2/cyclin A (IC
50 = 680 nM), Cdk2/cyclin E (IC
50 = 7.5 μM), and Cdk5/p25 (IC
50 = 850 nM). Also inhibits other kinases such as c-Src (IC
50 = 15 μM), casein kinase II (IC
50 = 20 μM), ERK1 (IC
50 = 20 μM), and ERK2 (IC
50 = 9 μM). Inhibition is competitive with respect to ATP binding.
生物活性
Potent inhibitor of CDK1/cyclin B and GSK-3 β (IC 50 values are 0.4 and 0.23 μ M respectively). Also inhibits CDK2/cyclin A, CDK2/cyclin E and CDK5/cyclin/p35 (IC 50 values are 0.68, 7.5 and 0.85 μ M respectively). Selective over c-src (IC 50 = 15 μ M), casein kinase 2 (IC 50 = 20 μ M), ERK1 (IC 50 = 20 μ M), ERK2 (IC 50 = 9 μ M) and a range of other protein kinases (IC 50 values > 35 μ M). Generates induced pluripotent stem cells (iPSCs) from somatic cells when used in combination with reprogramming factors; can replace Klf4.
ケンパウロン 上流と下流の製品情報
原材料
準備製品