| 规格或纯度 | >97% |
|---|---|
| 英文名称 | KH CB19 |
| 英文别名 | Ethyl 3-(2-Amino-1-cyanoethenyl)-6,7-dichloro-1-methylindole-2-carboxylate |
| 储存温度 | -20°C储存 |
| 运输条件 | 超低温冰袋运输 |
| 产品介绍 |
KH CB19是CDC2样激酶（CLK）1和4的有效和选择性抑制剂。KHCB19在促炎性条件下通过CLKs抑制富含丝氨酸/精氨酸的蛋白质磷酸化。 KH CB19 is a potent and selective inhibitor of CDC2-like kinase (CLK) 1 and 4. KH CB19 suppresses serine/arginine-rich protein phosphorylation by CLKs under proinflammatory conditions. |
| IC50 | CLK1: IC??= 20 nM |
|---|
| IUPAC Name | ethyl 3-[(E)-2-amino-1-cyanoethenyl]-6,7-dichloro-1-methylindole-2-carboxylate |
|---|---|
| INCHI | InChI=1S/C15H13Cl2N3O2/c1-3-22-15(21)14-11(8(6-18)7-19)9-4-5-10(16)12(17)13(9)20(14)2/h4-6H,3,18H2,1-2H3/b8-6- |
| InChi Key | CXJCGSPAPOTTSF-VURMDHGXSA-N |
| Canonical SMILES | CCOC(=O)C1=C(C2=C(N1C)C(=C(C=C2)Cl)Cl)C(=CN)C#N |
| PubChem CID | 44237094 |
| 分子量 | 338.19 |
| ChEMBL Ligand | CHEMBL1236620 |
|---|---|
| DrugBank Ligand | DB08691 |
| PubChem CID | 44237094 |
| CAS Registry No. | 1354037-26-5 |
| RCSB PDB Ligand | V25 |
| 溶解性 | Soluble in DMSO (40 mM). |
|---|---|
| 密度 | ~1.4 g/cm3(Predicted) |
| 折光率 | n20D1.62 (Predicted) |
| 沸点 | ~604.1° C at 760 mmHg (Predicted) |
| Ligand ID | 8055 |
|---|---|
| 名称 | KH-CB19 |
| 别名 | KH CB19 |
| 类别 | Synthetic organic |
| 学名 | ethyl 3-[(E)-2-amino-1-cyanoethenyl]-6,7-dichloro-1-methylindole-2-carboxylate |
| 生物活性评价 |
Off-targets include CLK3 and dual-specificity tyrosine-(Y)-phosphorylation regulated kinase 1A (DYRK1A) |
| 评价 |
KH-CB19 is an inhibitor of dual specificity CDC-like kinase 1 (CLK1) |
| 1. A-González N, Castrillo A. (2011) Liver X receptors as regulators of macrophage inflammatory and metabolic pathways.. Biochim Biophys Acta, 1812 (8): (982-94). [PMID:21193033] |
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