LFM-A13(Z)
| CAS号 | 244240-24-2 | 货号 | BCP12817 |
| 中文名 | LFM-A13(Z) | ||
| 英文名 | LFM-A13(Z) | ||
| 中文别名 | |||
| 英文别名 | LFMA13;LFM A13;(Z)-2-Cyano-N-(2,5-dibromophenyl)-3-hydroxybut-2-enamide; | ||
| 分子式 | C11H8Br2N2O2 | 分子量 | 360 |
| 生物活性 | in vitro: LFM-A13 inhibited recombinant BTK expressed in a baculovirus expression vector system with an IC50 value of 2.5 microM. Even at concentrations as high as 100 micrograms/ml (approximately 278 microM), this novel inhibitor did not affect the enzymatic activity of other protein tyrosine kinases, including JAK1, JAK3, HCK, epidermal growth factor receptor kinase, and insulin receptor kinase. Inhibition of Btk activity by LFM-A13 leads to enhancement of PKCtheta; activity, whereas nonselective inhibition of PKC activity by bisindolylmaleimide I leads to reduction in Btk activity. in vivo: LFM-A13 suppressed migration and differentiation of osteoclast precursors as well as bone-resorbing activity of mature osteoclasts. In primary myeloma-bearing SCID-rab mice, LFM-A13 inhibited osteoclast activity, prevented myeloma-induced bone resorption and moderately suppressed myeloma growth. | ||
| 信号通路 | Angiogenesis/Protein Tyrosine Kinase Cell Cycle/DNA Damage Jak/Stat Pathway Wnt/Stem Cell Epigenetics | ||
| 靶 点 | JAK BTK PLK | ||
结构式
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