CHIR-99021
| 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;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;水溶性CHIR-99021;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;GSK-3 Inhibitor XVI;3-Pyridinecarbonitrile, 6-[[2-[[4-(2,4-dichlorophenyl)-5-(5-methyl-1H-imidazol-2-yl)-2-pyrimidinyl]amino]ethyl]amino];CT 99021(CHIR 99021);6-[2-[4-(2,4-Dichlorophenyl)-5-(4-Methyl-1H-iMidazol-2-yl)pyriMidin-2-ylaMino]ethylaMino]pyridine-3-;CHIR 99021(CT 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;Antineoplastic;Anti-cancer&immunity;PI3K/Akt/mTOR;Inhibitors;Akt;mTOR;PI3K;生化试剂;试剂盒-细胞分析试剂盒;小分子 |
| Mol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。 |
| InChIKey | AQGNHMOJWBZFQQ-UHFFFAOYSA-N |
| CAS 数据库 | 252917-06-9 |
| Target | Value |
|
GSK-3β
(Cell-free assay) | 6.7 nM |
|
GSK-3α
(Cell-free assay) | 10 nM |
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.
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.
安全信息
| 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 |