化合物6-BIO T1917

Product Introduction
Bioactivity


英文名: GSK 3 Inhibitor IX

描述: GSK 3 Inhibitor IX (6-BIO) 是一种选择性可逆的，ATP 竞争性的 GSK-3α/β和 CDK1-cyclinB 复合体抑制剂，能够抑制 (GSK-3α/β)/CDK1/CDK5 的活性，IC50值分别为 5 nM/320 nM/83 nM。

细胞实验: COS1, Hepa (wild-type, CEM/LM AhR deficient and ELB1 ARNT deficient), or SH-SY5Y cells are grown in 6 cm culture dishes in Dulbecco's Modified Medium (DMEM) containing 10% fetal bovine serum. For treatment, IO (5 μM), BIO (5 or 10 μM), MeBIO (5 or 50 μM), LiCl (20 or 40 mM), or mock solution (DMSO, 0.5% final concentration) is added to medium when cell density reaches ～70% confluence. After 12 (SH-SY5Y) or 24 hours, the cells, while still in plate, are lysed with lysis buffer (1% SDS, 1 mM sodium orthovanadate, 10 mM Tris [pH 7.4]). The lysate is passed several times through a 26 g needle, centrifuged at 10,000 × g for 5 min, and adjusted to equal protein concentration. About 8 μg of each sample is loaded for immunoblotting. Enhanced chemiluminescence is used for detection. The following primary antibodies are used: mouse anti-β-catenin CT (Upstate Biotechnolgies, Clone 7D8, recognizes total β-catenin), mouse anti-phospho-β-catenin (Upstate Biotechnologies, Clone 8E7, recognizes dephosphorylated β-catenin), mouse anti-GSK-3 β, mouse anti-GSK-3 phosphoTyr216, rabbit anti-AhR (Aryl hydrocarbon receptor), and rabbit anti-actin.(Only for Reference)

激酶实验: Kinase assay: Kinase activities are assayed in Buffer A or C at 30°C, at a final ATP concentration of 15 μM. Blank values are subtracted and activities calculated as pmoles of phosphate incorporated during a 10 min incubation. Controls are performed with appropriate dilutions of dimethylsulfoxide. In a few cases phosphorylation of the substrate is assessed by autoradiography after SDS-PAGE. GSK-3α/β is purified from porcine brain by affinity chromatography on immobilized axin. It is assayed, following a 1/100 dilution in 1 mg BSA/ml 10 mM DTT, with 5 μl 40 μM GS-1 peptide, a specific GSK-3 substrate, (YRRAAVPPSPSLSRHSSPHQSpEDEEE), in buffer A, in the presence of 15 μM [γ-32P] ATP (3,000 Ci/mmol; 1 mCi/ml) in a final volume of 30 μl. After 30 min incubation at 30°C, 25 μl aliquots of supernatant are spotted onto 2.5 × 3 cm pieces of Whatman P81 phosphocellulose paper, and 20 seconds later, the filters are washed five times (for at least 5 min each time) in a solution of 10 ml phosphoric acid/liter of water. The wet filters are counted in the presence of 1 ml ACS scintillation fluid.

体外活性: BIO抑制小鼠移植瘤模型中黑色素瘤生长.

体内活性: BIO是pan-JAK抑制剂,作用于TYK2,JAK1,JAK2 和 JAK3,IC50值分别为0.03,1.5,8.0,0.5 μM。BIO是糖原合成酶激酶-3（GSK-3）的特异性抑制剂,GSK-3α/β的IC50为5 nM,比CDK5选择性高16倍以上。BIO与这些激酶的ATP结合口袋相互作用,减少细胞模型中GSK-3特异性位点上的β-连环蛋白磷酸化。BIO促进哺乳动物心肌细胞增殖。BIO选择性抑制STAT3磷酸化,并诱导人类黑色素瘤细胞凋亡。在人类和小鼠胚胎干细胞中,BIO维持未分化表型并维持多能状态特异性转录因子Oct-3/4,Rex-1和Nanog的表达。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 45 mg/mL (126.34 mM)
Ethanol : 21 mg/mL (58.96 mM)


关键字: Cyclin dependent kinase | Apoptosis | Inhibitor | Glycogen synthase kinase-3 | CDK | Glycogen synthase kinase 3 | MLS-2052 | MLS2052 | GSK-3 | inhibit | GSK 3 Inhibitor IX

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相关库: Drug Repurposing Compound Library | Cell Cycle Compound Library | Anti-Cancer Drug Library | Inhibitor Library | Kinase Inhibitor Library | Anti-Cancer Clinical Compound Library | Anti-Diabetic Compound Library | Tyrosine Kinase Inhibitor Library | Stem Cell Differentiation Compound Library | Glycolysis Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途