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CAS No.: 1234480-50-2

XMD8-92 Catalog No. CSN16763

Synonyms: XMD8-92

XMD8-92 is an inhibitor of ERK5/BMK1. The Kd values for BMK1, DCAMKL2, PLK4 and TNK1 are 80 nM, 190 nM, 600 nM and 890 nM respectively.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 DCAMKL2

Kd:190nM PLK4

Kd:600nM BMK1/ERK5

Kd:80nM TNK1

Kd:890nM
描述BMK1 (Big MAP Kinase 1) is a member of the MAP kinase family. MAP kinases act as an integration point for multiple biochemical signals, and are involved in a wide variety of cellular processes such as proliferation, differentiation, transcription regulation and development. BMK1 is specifically activated by mitogen-activated protein kinase kinase 5 (MAP2K5/MEK5). It is involved in the downstream signaling processes of various receptor molecules including receptor type kinases, and G protein-coupled receptors. In response to extracelluar signals, this kinase translocates to cell nucleus, where it regulates gene expression by phosphorylating, and activating different transcription factors^[3]. XMD8-92 is a BMK1 inhibitor. The dissociation constant (Kd) of XMD8-92 towards BMK1 was 80 nM, and data of XMD8-92 against other kinases suggested selectivity of XMD8-92 to BMK1. In a kinase activity assay utilizing Hela cell lysates, the IC50 of XMD8-92 against BMK1 was 1.5 μM. Furthermore, growth factor-induced activation of cellular BMK1 was effectively blocked by 1 μM XMD8-92, detected by mobility retardation. Cell proliferation assay revealed that 5 μM XMD8-92 inhibited more than 50% PC3, Hela and LL/2 cell growth when incubated for 48h^[4]. 48h treatment of 25 μM XMD8-92 also inhibited cell proliferation of pancreatic tumor AsPC-1cells to the extent of more than 50%^[5]. In animal experiments, treatment of mice bearing Hela or LL/2 xenografts with XMD8-92 at the dose of 50 mg/kg twice daily 1 day, several days, or weeks after inoculation of the tumor cells all significantly inhibit the growth of the tumors^[4]. In an AsPC-1 xenograft model established in NOD/SCID mice, XMD8-92 administrated at the dose of 50 mg/kg i.p. daily for 15 days significantly inhibited tumor growth^[5].
作用机制XMD8-92 inhibits BMK1 via ATP site competition-binding. The selective binding and inhibition of XMD8-92 towards BMK1 was revealed by ATP-site competition binding assay and KiNativ method utilizing Hela cell lysates^[4].
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
human HeLa cells	-	Function assay	-	Inhibition of EGF-induced BMK1 autophosphorylation in human HeLa cells by SDS-PAGE analysis, IC50=0.24 μM	21412406

参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.1072 mL
- 10.5362 mL
- 21.0724 mL
- 5 mM
- 0.4214 mL
- 2.1072 mL
- 4.2145 mL
- 10 mM
- 0.2107 mL
- 1.0536 mL
- 2.1072 mL

技术信息

CAS号

1234480-50-2

储存条件

粉末: Keep in dark place,Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C26H30N6O3

运输

蓝冰

分子量

474.55

别名

XMD8-92

溶解度

DMSO	17.0 mg/mL (35.8 mM)
Water	insoluble

动物实验配方

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靶点	Description	IC50
DCAMKL2		Kd:190nM
PLK4		Kd:600nM
BMK1/ERK5		Kd:80nM
TNK1		Kd:890nM

XMD8-92 Catalog No. CSN16763

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