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一键询价梅里埃 10400奈瑟氏球菌嗜血菌鉴定盒API NH
两周
面议
梅里埃 API氧化酶试剂
两周
面议
CCFSTTG1 人脑星形细胞瘤 QCH828
一周
3500¥
MM28 人眼葡萄膜黑色瘤細胞 QCH829
一周
5500¥
HCC202 人乳腺原发性导管癌 QCH830
一周
3000¥
HCC2157 人乳腺导管癌细胞(三阴性)QCH831
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5000¥
hCMEC/D3-RFP红色荧光蛋白标记的人脑微血管内皮细胞 QCH346R
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3500¥
KHYG-1 人NK细胞淋巴瘤细胞 QCH833
一周
3500¥
NCI-h1869 人非小细胞肺癌鳞癌细胞 QCH834
一周
3500¥
NCI-H1417 人小细胞肺癌细胞 QCH835
钦诚生物 | 一周
3500¥
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抑制剂描述: 产品名称:CHIR-98014 产品别名:见爱必信官网 英文别名:CHIR-98014 靶点:GSK-3 CAS:252935-94-7 纯度:>98% 外观:见爱必信官网 保存方法:store at -20℃ for one year(Powder); in DMSO or others solvent store at 2-4℃ for two weeks, at -20℃ for six months. 描述: CHIR98014是一种有效的GSK-3α/β抑制剂,无细胞试验中IC50为0.65 nM/0.58 nM,作用于GSK-3比作用于其最密切的同源物Cdc2 和 ERK2选择性高。 溶解性:DMSO :8 mg/mL (16.45 mM) 体外研究: CHIR-98014 inhibits human GSK-3β with Ki of 0.87 nM. CHIR-98014 is very effective in preventing murine and rat GSK-3. Although CHIR-98014 acts as a simple competitive inhibitor of ATP binding, it displays from 500-fold to >1000-fold selectivity for GSK-3 versus 20 other protein kinases including Cdc2, ERK2, Tie-2 and KDR. CHIR-98014 prevents Cdc2 with IC50 of 3.7 μM. However, CHIR 98014 reveals similar ptoency against the highly homologous ɑ and β isoforms of GSK-3, it is noteworthy that it stronly discriminated between GSK-3 and its closest homologs CDC2 and ERK2. Exposure of insulin receptor-expressing CHO-IR cells or primary rat hepatocytes to increasing concentrations of inhibitor CHIR98014 results in a two- to three-fold stimulation of the GS activity ratio above basal. The concentrations of CHIR-98014 giving rise to half-maximal GS stimulation (EC50) is 106 nM and 107 nM for CHO-IR and rat hepatocytes, respectively. 体内研究:GSK-3 inhibitor CHIR-98014 activates the GS activity ratio in isolated type I skeletal muscle from insulin-sensitive lean Zucker and from insulin-ressitant ZDF rats. Soleus muscle isolated from ZDF rats shows significant resistance to insulin for activation of GS but responded to 500 nM CHIR-98014 to the same extent (40% increase) as muscle from lean Zucker rats. Notably, GS activation by insulin plus CHIR-98014 is additive in muscle from lean Zucker rats and greater than additive in muscle from the ZDF rats. Total GS activity is not altered by either CHIR-98014 or insulin in these cells and muscles. Meanwhile, CHIR-98014 does not influence the insulin dose-response in muscle from lean animals. The reduction in hyperglycemia and improved glucose disposal are not limited to db/db mice and ZDF rats, as similar results are observed with ob/ob mice, diet-induced diabetic C57BL/6 mice, and glucose-intolerant SHHF rats treated with CHIR-98014. Additionally, CHIR-98014 decreases the phosphorylation (Ser396) of tau protein in the cortex and hippocampus of postnatal rats.
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