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化驗
≥98% (HPLC)
形狀
powder
顏色
white to beige
溶解度
DMSO: 2 mg/mL, clear
儲存溫度
−20°C
SMILES 字串
O=C(N1CCC(CC1)C2=C3C(C=C(C=N3)N4CCN(CC4)C)=NC=N2)C5=CC=C(C=C5N)OC(F)(F)F
生化/生理作用
BAY-885 is an ATP site-targeting, potent and selective ERK5 (BMK1, MAPK7) inhibitor (IC50 = 35 nM with 250 μM ATP; % inhibition at 1 μM = 62/rat Fer, 58/human EphB3, 43/human EphA5, =20/355 kinases) with no BRD4 affinity (20 μM), nor inhibitory potency toward hERG (10 μM) and CYP enzymes (20 μM; CYP1A2, CYP2C8, CYP2C9, CYP2D6, CYP3A4). BAY-885 potently inhibits 100 ng/mL EGF-induced, ERK5-dependent MEF2 activity (IC50 = 120 nM; SN12C-MEF2-luc reporter assay).
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
Journal of medicinal chemistry, 62(2), 928-940 (2018-12-20)
The availability of a chemical probe to study the role of a specific domain of a protein in a concentration- and time-dependent manner is of high value. Herein, we report the identification of a highly potent and selective ERK5 inhibitor
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