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
中文名称:
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
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:
6-[2-[4-(2,4-Dichlorophenyl)-5-(4-methyl-1H-imidazol-2-yl)pyrimidin-2-ylamino]ethylamino]pyridine-3-carbonitrile
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-3 Inhibitor XVI;3-Pyridinecarbonitrile, 6-[[2-[[4-(2,4-dichlorophenyl)-5-(5-methyl-1H-imidazol-2-yl)-2-pyrimidinyl]amino]ethyl]amino];CT99021;CHIR99021;CHIR 99021;CT-99021;CT 99021(CHIR 99021)
CAS号:
252917-06-9
分子式:
C22H18Cl2N8
分子量:
465.34
EINECS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;Inhibitors;Antineoplastic;Anti-cancerimmunity;PI3K/Akt/mTOR;Akt;mTOR;PI3K
Mol文件:
252917-06-9.mol
沸点
784.1±70.0 °C(Predicted)
密度
1.48
储存条件
-20°C
溶解度
DMSO: soluble2mg/mL, clear (warmed)
酸度系数(pKa)
11.92±0.10(Predicted)
形态
powder
颜色
white to light brown
InChIKey
AQGNHMOJWBZFQQ-UHFFFAOYSA-N
CAS 数据库
252917-06-9
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6.7 nM。
生物活性
CHIR-99021 (CT99021)是一种GSK-3α和GSK-3β抑制剂， IC50分别为10 nM and 6.7 nM。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
Target Value
GSK-3β
(Cell-free assay) 6.7 nM
GSK-3α
(Cell-free assay) 10 nM
Target
Value
GSK-3β
(Cell-free assay)
6.7 nM
GSK-3α
(Cell-free assay)
10 nM
体外研究
CHIR-99021 inhibits human GSK-3β with K i values of 9.8 nM. CHIR-99021 is a small organic molecule that inhibits GSK3α and GSK3β by competing for their ATP-binding sites.In vitro kinase assays reveal that CHIR-99021 specifically inhibits GSK3β (IC 50 =~5 nM) and GSK3α (IC 50 =~10 nM), with little effect on other kinases. In the presence of CHIR-99021 the viability of the ES-D3 cells is reduced by 24.7% at 2.5 μM, 56.3% at 5 μM, 61.9% at 7.5 μM and 69.2% at 10 μM CHIR-99021 with an IC 50 of 4.9 μM.
体内研究
In ZDF rats, a single oral dose of CHIR-99021 (16 mg/kg or 48 mg/kg) rapidly lowers plasma glucose, with a maximal reduction of nearly 150 mg/dl 3-4 h after administration. CHIR99021 (2 mg/kg) given once, 4 h before irradiation, significantly improves survival after 14.5 Gy abdominal irradiation (ABI). CHIR99021 treatment significantly blocks crypt apoptosis and accumulation of p-H2AX + cells, and improves crypt regeneration and villus height. CHIR99021 treatment increases Lgr5 + cell survival by blocking apoptosis, and effectively prevents the reduction of Olfm4, Lgr5 and CD44 as early as 4 h.
危险品标志
T
危险类别码
25-36/37/38
安全说明
26-36/37/39-45
危险品运输编号
UN 2811 6.1 / PGIII
WGK Germany
3
海关编码
29335990
