42951-68-8
42951-68-8 structure
- Name: EB1
- Chemical Name: 3-amino-4,6-diphenyl-1H-pyrazolo<3,4-b>pyridine
- CAS Number: 42951-68-8
- Molecular Formula: C18H14N4
- Molecular Weight: 286.33100
- Catalog: Signaling Pathways Apoptosis Apoptosis
- Create Date: 2018-06-25 17:02:14
- Modify Date: 2024-01-26 01:31:26
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EB1 is the inhibitor of kinases MNK with IC50s of 0.69 μM (MNK1) and 9.4 μM (MNK2). EB1 selectively inhibits the growth of cancer cells, but not normal cells. EB1 also increases cell apoptosis and suppresses eIF4E phosphorylation[1][2].
| Name | 3-amino-4,6-diphenyl-1H-pyrazolo<3,4-b>pyridine |
|---|---|
| Synonyms |
3-amino-4,6-diphenylpyrazolo<3,4-b>pyridine
4,6-Diphenyl-1H-pyrazolo[3,4-b]pyridin-3-ylamine 4,6-diphenyl-1H-pyrazolo[3,4-b]pyridin-3-ylamine |
| Description | EB1 is the inhibitor of kinases MNK with IC50s of 0.69 μM (MNK1) and 9.4 μM (MNK2). EB1 selectively inhibits the growth of cancer cells, but not normal cells. EB1 also increases cell apoptosis and suppresses eIF4E phosphorylation[1][2]. |
|---|---|
| Related Catalog | |
| Target |
MNK1:0.69 μM (IC50) MNK2:9.4 μM (IC50) eIF4E |
| In Vitro | EB1（1.3-40 μM；24 小时）剂量依赖性地抑制 eIF4E 的磷酸化[1]。 EB1（2.5-40 μM；72 小时）对肿瘤细胞显示出剂量依赖性细胞毒性，并诱导细胞凋亡[1]。 EB1（5 μM、10 μM 和 20 μM；24 小时）直接作用于 MNK 激酶，而不会干扰激活上游信号，例如 p38 的激活 (p-p38) 及其下游效应子 HSP27 的磷酸化[1]。 EB1 (compound 14) 抑制癌细胞 HepG2 和 MCF-7 的 IC50 分别为 0.74 μM 和 5.18 μM[2]。 Western Blot Analysis[1] Cell Line: MDA-MB-231, MDA-MB-468, MCF7, and IMR90 cells Concentration: 1.3 μM, 2.5 μM, 5 μM, 10 μM, 20 μM, 40 μM Incubation Time: 24 hours Result: Blocked the phosphorylation of eIF4E in a dose-dependent manner. Apoptosis Analysis[1] Cell Line: MDA-MB-231, MDA-MB-468, MCF7, and IMR90 cells Concentration: 2.5 μM, 5 μM, 10 μM, 20 μM, 40 μM Incubation Time: 72 hours Result: Increased the percentage of apoptosis cells among tumor cells. |
| References |
| Molecular Formula | C18H14N4 |
|---|---|
| Molecular Weight | 286.33100 |
| Exact Mass | 286.12200 |
| PSA | 67.59000 |
| LogP | 4.45530 |