EB1

Modify Date: 2024-01-26 01:31:26

EB1 Structure
EB1 structure
Common Name EB1
CAS Number 42951-68-8 Molecular Weight 286.33100
Density N/A Boiling Point N/A
Molecular Formula C18H14N4 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of EB1


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].

 Names

Name 3-amino-4,6-diphenyl-1H-pyrazolo<3,4-b>pyridine
Synonym More Synonyms

 EB1 Biological Activity

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

[1]. Bou-Petit E, et al. Overcoming Paradoxical Kinase Priming by a Novel MNK1 Inhibitor. J Med Chem. 2022 Apr 28;65(8):6070-6087.  

[2]. Aboukhatwa SM, et al. Nicotinonitrile-derived apoptotic inducers: Design, synthesis, X-ray crystal structure and Pim kinase inhibition. Bioorg Chem. 2022 Dec;129:106126.  

 Chemical & Physical Properties

Molecular Formula C18H14N4
Molecular Weight 286.33100
Exact Mass 286.12200
PSA 67.59000
LogP 4.45530

 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
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