XMD8-92 | ERK5 inhibitor | Probechem Biochemicals

Chemical Structure : XMD8-92

CAS No.: 1234480-50-2

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XMD8-92 (XMD 8-92)

货号: PC-22834Not For Human Use, Lab Use Only.

XMD8-92 a specific small-molecule inhibitor of Big mitogen-activated protein kinase 1 (BMK1, ERK5) with Kd of 80 nM, IC50 of 1.5 uM in cell-free assays.

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10 mg	￥780	In stock
25 mg	￥1280	In stock
50 mg	￥2180	In stock
100 mg	￥3580	In stock
250 mg		Get quote

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生物&药学活性

XMD8-92 a specific small-molecule inhibitor of Big mitogen-activated protein kinase 1 (BMK1, ERK5) with Kd of 80 nM, IC50 of 1.5 uM in cell-free assays.
XMD8-92 weakly inhibits TNK1 (IC50 = 10 μM) and ACK1 (aka TNK2, IC50 = 18 μM), does not inhibit MEK5, TNK1 and PLK4.
XMD8-92 (1 uM) effectively blocks growth factor-induced activation of cellular BMK1, but not the structurally similar ERK1/2 in HeLa cells.
XMD8-92 dramatically reduced the BMK1-dependent transactivating activity of MEF2C, a known substrate for BMK1.
XMD8-92 shows anti-tumor effect by blocking tumor cell proliferation and tumor-associated angiogenesis, through promyelocytic leukemia protein (PML).

物理化学性质&存储条件

分子量	474.57
分子式	C26H30N6O3
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	2-((2-Ethoxy-4-(4-hydroxypiperidin-1-yl)phenyl)amino)-5,11-dimethyl-5,11-dihydro-6H-benzo[e]pyrimido[5,4-b][1,4]diazepin-6-one

参考文献

1. Yang Q, et al. Cancer Cell. 2010 Sep 14;18(3):258-67.

2. Yang Q, et al. Clin Cancer Res. 2011 Jun 1;17(11):3527-32.

XMD8-92 (XMD 8-92)

生物&药学活性

物理化学性质&存储条件

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XMD8-92 (XMD 8-92)

生物&药学活性

物理化学性质&存储条件

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