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Chemical Structure : XMD8-92
CAS No.: 1234480-50-2
Catalog No.: 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.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 10 mg | $78 | In stock | |
| 25 mg | $128 | In stock | |
| 50 mg | $218 | In stock | |
| 100 mg | $358 | In stock | |
| 250 mg | Get quote |
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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).
| M.Wt | 474.57 | |
| Formula | C26H30N6O3 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| 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 |
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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.
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