产品名称

英文名称：CHIR-98014

同义词

CHIR-98014、252935-94-7、CHIR98014、6-N-[2-[[4-(2,4-dichlorophenyl)-5-imidazol-1-ylpyrimidin-2-yl]amino]ethyl]-3-nitropyridine-2,6-diamine、CT-98014、CHEMBL3185148、2,6-PYRIDINEDIAMINE, N6-[2-[[4-(2,4-DICHLOROPHENYL)-5-(1H-IMIDAZOL-1-YL)-2-PYRIMIDINYL]AMINO]ETH、N-6-[2-[[4-(2,4-二氯苯基)-5-(1H-咪唑-1-基)-2-嘧啶基]氨基]乙基] -3-硝基-2,6-吡啶二胺、CHIR-98014

产品性质

CAS编号：252935-94-7

分子式：C20H17Cl2N9O2

分子量：486.31

PubChem编号：53396311

别名：N-6-[2-[[4-(2,4-二氯苯基)-5-(1H-咪唑-1-基)-2-嘧啶基]氨基]乙基] -3-硝基-2,6-吡啶二胺|CHIR-98014

英文别名：CHIR-98014|252935-94-7|CHIR98014|6-N-[2-[[4-(2,4-dichlorophenyl)-5-imidazol-1-ylpyrimidin-2-yl]amino]ethyl]-3-nitropyridine-2,6-diamine|CT-98014|CHEMBL3185148|2,6-PYRIDINEDIAMINE, N6-[2-[[4-(2,4-DICHLOROPHENYL)-5-(1H-IMIDAZOL-1-YL)-2-PYRIMIDINYL]AMINO]ETH

规格或纯度：98%

英文名称：CHIR-98014

生化机理：高效和选择性GSK-3抑制剂（β和α同工型的IC50值分别为0.58和0.65 nM）。在一系列其他激酶中，GSK-3β的选择性> 500倍。在体外提高糖尿病大鼠肌肉条的胰岛素敏感性，并在体内口服葡萄糖耐量测试中降低胰岛素和葡萄糖水平。激活人脂肪干细胞（hASC）中的Wnt信号，并促进定形内胚层的产生。已用于从hPSC衍生心外膜细胞的协议中。Chir 98014是一种糖原合成酶激酶 -3(gsk-3)抑制剂，对 gsk3α 和 gsk3β 的 ic50分别为0.65 nm 和0.58 nm。Chir98014对 gsk-3的选择性是其他20种蛋白激酶的500到10000倍，其中包括最接近的同源 cdc2和 erk2。

储存温度：-20°C储存

运输条件：超低温冰袋运输

产品介绍：产品介绍CHIR-98014是一种有效的GSK-3α和GSK-3β抑制剂，IC50值分别为0.65 nM 和0.58 nM。 GSK-3（糖原合酶激酶3）是一种丝氨酸/苏氨酸蛋白激酶，在许多细胞内信号通路中具有关键作用，包括细胞增殖、迁移、炎症和免疫反应、葡萄糖调节和细胞凋亡。据报道，GSK-3在多种疾病中异常表达，包括II型糖尿病、阿尔茨海默病、炎症、癌症和躁郁症。 CHIR-98014是一种有效的GSK-3α和GSK-3β抑制剂。在表达胰岛素受体的CHO-IR细胞或原代大鼠肝细胞中，CHIR-98014以剂量依赖的方式刺激GS活性比，比基础水平高2-3倍。同样地，在胰岛素敏感的lean Zucker 大鼠和胰岛素抗性的ZDF大鼠来源的I型骨骼肌中，CHIR-98014激活GS活性比[1]。在小鼠ES-D3细胞中，CHIR-98014处理48和72小时后通过抑制GSK-3，从而显著激活Wnt/beta-catenin信号通路。 在明显糖尿病和胰岛素抗性db/db小鼠模型中，CHIR-98014（30 mg/kg）口服给药后4小时内显著减少空腹高血糖，在口服或静脉注射葡萄糖时改善了葡萄糖处理。产品应用CHIR-98014 (CT98014)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。Product descriptionCHIR-98014 is an effective GSK-3Α and GSK-3Β inhibitor with IC50 values of 0.65 nM and 0.58 NM respectively. GSK-3(glycogen synthase Kinase 3) is a serine/threonine protein kinase that plays a key role in many intracellular signaling pathways, including Cell Proliferation, migration, inflammation and immune response, glucose regulation and apoptosis. GSK-3 is reported to be abnormally expressed in a variety of diseases, including type 2 diabetes, Alzheimer’s Disease, inflammation, cancer and bipolar disorder. CHIR-98014 is an effective inhibitor of GSK-3 Α and GSK-3 β. In CHO-IR cells or primary rat hepatocytes expressing INSR, CHIR-98014 stimulated GS activity in a dose-dependent manner, 2-3 times higher than baseline level. Similarly, CHIR-98014 activates GS more than [1] in type I skeletal muscles from insulin-sensitive Lean Zucker rats and insulin-resistant ZDF rats. In mouse ES-D3 cells, CHIR-98014 significantly activates Wnt/beta-catenin signaling pathway by inhibiting GSK-3 after 48 and 72 hours of treatment. CHIR-98014(30 mg/kg) significantly reduced fasting hyperglycemia within 4 hours after Oral Administration, and improved glucose treatment during oral or intravenous administration in a mouse model with marked diabetes and insulin resistance (DB/DB) .Product ApplicationCHIR 98014 has been used for the generation of small molecules neural progenitor cells and differentiation towards motor neurons. It has also been used as a Wnt/β-catenin pharmacological agonist in the cell-conditioned medium to perform chromatin immunoprecipitation (ChIP) studies in HT22 neurons.

IUPAC Name：6-N-[2-[[4-(2,4-dichlorophenyl)-5-imidazol-1-ylpyrimidin-2-yl]amino]ethyl]-3-nitropyridine-2,6-diamine

INCHI：InChI=1S/C20H17Cl2N9O2/c21-12-1-2-13(14(22)9-12)18-16(30-8-7-24-11-30)10-27-20(29-18)26-6-5-25-17-4-3-15(31(32)33)19(23)28-17/h1-4,7-11H,5-6H2,(H3,23,25,28)(H,26,27,29)

InChi Key：MDZCSIDIPDZWKL-UHFFFAOYSA-N

Canonical SMILES：C1=CC(=C(C=C1Cl)Cl)C2=NC(=NC=C2N3C=CN=C3)NCCNC4=NC(=C(C=C4)[N+](=O)[O-])N

Isomeric SMILES：C1=CC(=C(C=C1Cl)Cl)C2=NC(=NC=C2N3C=CN=C3)NCCNC4=NC(=C(C=C4)[N+](=O)[O-])N

WGK Germany：3

PubChem CID：53396311

CAS Registry No.：252935-94-7

ChEMBL Ligand：CHEMBL3185148

Reactome Reaction：R-HSA-9687724

Reactome Drug：R-ALL-9687681

溶解性：溶于DMSO, 最高浓度 (mg/mL) 9.73, 最高浓度(mM) 20 温和加热

产品包装