IKK2抑制剂（LY2409881）

中文名称:

IKK2抑制剂（LY2409881）

中文同义词:

IKK2抑制剂(LY2409881);2-[5-氯-2-[[3-(4-甲基-1-哌嗪基)丙基]氨基]-4-嘧啶基]-N-环丙基-苯并[B]噻吩-4-甲酰胺三盐酸盐;LY2409881三盐酸盐

英文名称:

LY2409881 trihydrochloride

英文同义词:

LY2409881 trihydrochloride;LY2409881;2-(5-chloro-2-(3-(4-methylpiperazin-1-yl)propylamino)pyrimidin-4-yl)-N-cyclopropylbenzo[b]thiophene-4-carboxamide trihydrochloride;2-[5-Chloro-2-[[3-(4-methyl-1-piperazinyl)propyl]amino]-4-pyrimidinyl]-N-cyclopropylbenzo[b]thiophene-4-carboxamide trihydrochloride;LY2409881 triHCl;LY2409881 3HCl;CS-1620;LY-2409881 HCl

CAS号:

946518-60-1

分子式:

C24H30Cl2N6OS

分子量:

521.51

EINECS号:

相关类别:

小分子抑制剂;小分子抑制剂，天然产物;细胞生物学试剂;Inhibitors

Mol文件:

946518-60-1.mol

生物活性

LY2409881 是一种有效的选择性 IKK2 抑制剂，IC50 为 30 nM，选择性比IKK1和其他常见激酶高10倍多。

体外研究

LY2409881 inhibits constitutively activated NF-ƘB, and causes concentration- and time-dependent growth inhibition and apoptosis in diffuse large B-cell lymphoma (DLBCL) cells. In the ovarian cancer cell line SKOV3, LY2409881 demonstrates moderate cytotoxicity. LY2409881 is synergistic with doxorubicin and cyclophosphamide in SUDHL2 cell in inhibiting the cell growth, but not in LY1 cell. In both SUDHL2 and LY1 cells, LY2409881 is synergistic with the histone deacetylase (HDAC) inhibitor romidepsin in inhibiting the cell growth.

体内研究

In SCID-beige xenograft mouse model, LY2409881 (50, 100, and 200 mg/kg, i.p.) significantly inhibits the tumor growth.