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| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| C650922-5mg |
5mg |
期货 ![]() |
| |
| C650922-10mg |
10mg |
期货 ![]() |
| |
| C650922-25mg |
25mg |
期货 ![]() |
|
| 别名 | CLK1-输入-1 |
|---|---|
| 规格或纯度 | ≥99% |
| 英文名称 | CLK1-IN-1 |
| 生化机理 | CLK1-IN-1 是一种强效的 Cdc2 样激酶 1(CLK1)选择性抑制剂,其 IC 50 为 2 nM。 |
| 储存温度 | -20°C储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 抑制剂 |
| 产品介绍 |
CLK1-IN-1 is a potent and selective of Cdc2-like kinase 1 ( CLK1 ) inhibitor, with an IC 50 of 2 nM. In Vitro CLK1 is the most potently inhibited kinase (IC 50 : 2 nM). In addition to CLK1, only two kinases have an IC 50 value less than 100 nM, namely CLK2 (IC 50 : 31 nM) and CLK4 (IC 50 : 8 nM), DYRK1A is the strongest off-target. The ability of CLK1-IN-1 to induce autophagy in BNL CL.2 and SKOV-3 (human ovarian cancer cell line) cells is also examined. The effects of CLK1-IN-1 on yellow LC3 puncta also displays obvious dose dependency, and a dose of 10 μM shows the best performance. In addition, in CLK1-IN-1-treated cells, the number of red LC3 puncta (mRFP signals only35) increases compared with that of DMSO-treated cells, indicating the formation of autolysosomes. Importantly, CLK1-IN-1 stimulats the degradation of SQSTM1/p62 and increases the ratio of red LC3 puncta to yellow LC3 puncta, both of which indicate an induction of autophagic flux by CLK1-IN-1. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo APAP exposure results in severe liver injury, and treatment with CLK1-IN-1 (ip, 30 mg/kg) imparts a significant hepatoprotective effect. The results show that treatment with CLK1-IN-1 decreases serum ALT and AST levels significantly such that both marker enzymes return to normal levels . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid IC50& Target:CLK1 2 nM (IC 50 ) |
| 纯度 | ≥99% |
| 作用机制 | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | 参考文献 |
|---|
| 分子类型 | 小分子 |
|---|---|
| IIUPAC Name | 5-[1-[(1S)-1-(4-fluorophenyl)ethyl]triazolo[4,5-c]quinolin-8-yl]-1,3-benzoxazole |
| INCHI | 1S/C24H16FN5O/c1-14(15-2-6-18(25)7-3-15)30-24-19-10-16(4-8-20(19)26-12-22(24)28-29-30)17-5-9-23-21(11-17)27-13-31-23/h2-14H,1H3/t14-/m0/s1 |
| InChi Key | BHKVSOQUPYXVRZ-AWEZNQCLSA-N |
| Smiles | CC(C1=CC=C(C=C1)F)N2C3=C4C=C(C=CC4=NC=C3N=N2)C5=CC6=C(C=C5)OC=N6 |
| Isomeric SMILES | C[C@@H](C1=CC=C(C=C1)F)N2C3=C4C=C(C=CC4=NC=C3N=N2)C5=CC6=C(C=C5)OC=N6 |
| PubChem CID | 129318964 |
| 分子量 | 409.42 |
| 溶解性 | DMSO : 25 mg/mL (61.06 mM; Need ultrasonic) |
|---|