中文名 | CHIR-99021 |
英文名 | CHIR-99021 |
别名 | 水溶性CHIR-99021 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 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 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 |
英文别名 | CT99021 CT-99021 CHIR99021 CHIR-99021 CHIR 99021 GSK-3 Inhibitor XVI CT 99021(CHIR 99021) 6-{2-[4-(2,4-Dichloro-phenyl)-5-(4-methyl-1H-imidazol-2-yl)-pyrimidin-2-ylamino]-ethylamino}-nicotinonitrile 6-[2-[4-(2,4-Dichlorophenyl)-5-(4-methyl-1H-imidazol-2-yl)pyrimidin-2-ylamino]ethylamino]pyridine-3-carbonitrile 3-Pyridinecarbonitrile, 6-[[2-[[4-(2,4-dichlorophenyl)-5-(5-methyl-1H-imidazol-2-yl)-2-pyrimidinyl]amino]ethyl]amino] |
CAS | 252917-06-9 |
EINECS | 809-015-4 |
化学式 | C22H18Cl2N8 |
分子量 | 465.34 |
InChIKey | AQGNHMOJWBZFQQ-UHFFFAOYSA-N |
密度 | 1.48 |
沸点 | 784.1±70.0 °C(Predicted) |
溶解度 | DMSO: 溶解2mg/mL,澄清 (温热) |
酸度系数 | 11.92±0.10(Predicted) |
存储条件 | -20°C |
稳定性 | 从提供的购买之日起稳定2年。在DMSO中的溶液可以在-20 ° 储存长达3个月。 |
外观 | 粉末 |
颜色 | white to light brown |
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 - 有毒物品 |
风险术语 | R25 - 吞食有毒。 R36/37/38 - 刺激眼睛、呼吸系统和皮肤。 |
安全术语 | S26 - 不慎与眼睛接触后,请立即用大量清水冲洗并征求医生意见。 S36/37/39 - 穿戴适当的防护服、手套和护目镜或面具。 S45 - 若发生事故或感不适,立即就医(可能的话,出示其标签)。 |
危险品运输编号 | UN 2811 6.1 / PGIII |
WGK Germany | 3 |
海关编号 | 29335990 |
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