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CHIR-99021 |
| CAS No.: |
252917-06-9 |
| 分子式： |
C22H18Cl2N8 |
| 分子量： |
465.34 |
| 备注： |
中文名称CHIR-99021中文同义词6-[2-[4-(2,4-二氯苯基)-5-(4-甲基-1H-咪唑-2-基)嘧啶-2-基氨基]乙基氨基]吡啶-3-甲腈1G;水溶性CHIR-99021;6-[[2-[[4-(2,4-二氯苯基)-5-(5-甲基-1H-咪唑-2-基)-2-嘧啶]氨基]乙基]氨基]-3-吡啶甲腈;抑制剂CHIR-99021;6-[2-[4-(2,4-二氯苯基)-5-(4-甲基-1H-咪唑-2-基)嘧啶-2-基氨基]乙基氨基]吡啶-3-甲腈;6-[2-[[4-(2,4-二氯苯基)-5-(5-甲基-1H-咪唑-2-基)嘧啶-2-基]氨基]乙氨基]吡啶-3-腈;GSK-3Α/Β抑制剂(CHIR-99021);6-[2-[4-(2,4-二氯苯基)-5-(4-甲基-1H-咪唑2基)嘧啶2-YLAMINO]乙基氨基]吡啶-3-腈英文名称CHIR-99021英文同义词6-[2-[4-(2,4-Dichlorophenyl)-5-(4-methyl-1H-imidazol-2-yl)pyrimidin-2-ylamino]ethylamino]pyridine-3-carbonitrile;6-{2-[4-(2,4-Dichloro-phenyl)-5-(4-methyl-1H-imidazol-2-yl)-pyrimidin-2-ylamino]-ethylamino}-nicotinonitrile;CHIR-99021;CT99021;GSK-3InhibitorXVI;3-Pyridinecarbonitrile,6-[[2-[[4-(2,4-dichlorophenyl)-5-(5-methyl-1H-imidazol-2-yl)-2-pyrimidinyl]amino]ethyl]amino];CT99021;CHIR99021;CHIR99021;CT-99021;CT99021(CHIR99021)CAS号252917-06-9分子式C22H18Cl2N8分子量465.34EINECS号809-015-4相关类别抗肿瘤及免疫抑制剂;小分子抑制剂，天然产物;小分子抑制剂;信号转导通路激酶抑制剂;细胞生物学试剂;生化试剂;试剂盒-细胞分析试剂盒;小分子;Inhibitors;Antineoplastic;Anti-cancer&immunity;PI3K/Akt/mTOR;Akt;mTOR;PI3KMol文件252917-06-9.mol结构式CHIR-99021性质沸点784.1±70.0°C(Predicted)密度1.48储存条件-20°C溶解度DMSO：可溶，2mg/mL，澄清（加热）酸度系数(pKa)11.92±0.10(Predicted)形态粉末颜色白色至浅棕色稳定性DMSO中的溶液可在-20°下稳定储存3个月。InChIKeyAQGNHMOJWBZFQQ-UHFFFAOYSA-NCAS数Chemicalbook据库252917-06-9CHIR-99021用途与合成方法产品描述CHIR99021是一种氨基嘧啶衍生物，其抑制GSK3α和GSK3β的IC50值分别为10和6.7nM。生物活性CHIR-99021(CT99021)是一种GSK-3α和GSK-3β抑制剂，IC50分别为10nMand6.7nM。CHIR99201对CDKs没有交叉反应性，对GSK-3β的选择性是对CDKs选择性的350倍。CHIR-99021可作为Wnt/β-catenin的激活剂并诱导自噬。靶点TargetValueGSK-3β(Cell-freeassay)6.7nMGSK-3α(Cell-freeassay)10nM体外研究CHIR-99021inhibitshumanGSK-3βwithKivaluesof9.8nM.CHIR-99021isasmallorganicmoleculethatinhibitsGSK3αandGSK3βbycompetingfortheirATP-bindingsites.InvitrokinaseassaysrevealthatCHIR-99021specificallyinhibitsGSK3β(IC50=~5nM)andGSK3α(IC50=~10nM),withlittleeffectonotherkinases.InthepresenceofCHIR-99021theviabilityoftheES-D3cellsisreducedby24.7%at2.5μM,56.3%at5μM,61.9%at7.5μMand69.2%at10μMCHIR-99021withanIC50of4.9μM.体内研究InZDFrats,asingleoraldoseofCHIR-99021(16mg/kgor48mg/kg)rapidlylowersplasmaglucose,withamaximalreductionofnearly150mg/dl3-4hafteradministration.CHIR99021(2mg/kg)givenonce,4hbeforeirradiation,significantlyimprovessurvivalafter14.5Gyabdominalirradiation(ABI).CHIR99021treatmentsignificantlyblockscryptapoptosisandaccumulationofp-H2AX+cells,andimprovescryptregenerationandvillusheight.CHIR99021treatmentincreasesLgr5+cellsurvivalbyblockingapoptosis,andeffectivelypreventsthereductionofOlfm4,Lgr5andCD44asearlyas4h. |
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