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品質等級
化驗
≥98% (HPLC)
形狀
powder
顏色
white to beige
溶解度
DMSO: 2 mg/mL, clear (Warmed)
儲存溫度
-10 to -25°C
SMILES 字串
FC(OC1=CC=CC(C2=CN=C3C=CC(C4=CC=NC=C4)=NN32)=C1)(F)F
生化/生理作用
Compound C28 is an orally active, potent, ATP-competitive lemur tyrosine kinase 3 (LMTK3) inhibitor with additional inhibitory potency against only 4 other kinases among a panel of 140 (IC50 = 67 nM/LMTK3, 5 nM/CLK, 6 nM/DYRK1α, 48 nM/HIPK2, 41 nM/IRAK4). LMTK3 promotes proteasome-mediated LMTK3 degradation and decreases proliferation of cancer cultures (NCI-60 panel IC50 <10 μM) and displays antitumor efficacy in xenograft and transgenic breast cancer mouse models in vivo (10 mg/mL via dialy p.o.).
儲存類別代碼
11 - Combustible Solids
水污染物質分類(WGK)
WGK 3
閃點(°F)
Not applicable
閃點(°C)
Not applicable
LMTK3 inhibition affects microtubule stability
Molecular Cancer, 20(1), 53-53 (2021)
The Inhibitory Properties of a Novel, Selective LMTK3 Kinase Inhibitor
International Journal of Molecular Sciences, 24(1), 865-865 (2023)
Science advances, 6(46) (2020-11-15)
Elucidating signaling driven by lemur tyrosine kinase 3 (LMTK3) could help drug development. Here, we solve the crystal structure of LMTK3 kinase domain to 2.1Å resolution, determine its consensus motif and phosphoproteome, unveiling in vitro and in vivo LMTK3 substrates.
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