计算溶液所需的质量、体积或浓度。
提供 ≥99% 纯度,适用于对基线干扰要求严格的色谱和分析工作流程。
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在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
KDM5-IN-1 is a potent, selective and orally bioavailable KDM5 inhibitor with an IC 50 of 15.1 nM.
In Vitro
KDM5-IN-1 is found to potently inhibit KDM5B and KDM5C isoforms (IC 50 of 4.7 and 65.5 nM, respectively). It is significantly less potent against other KDM enzymes (1A, 2B, 3B, 4C, 5A, 6A, 7B), inhibiting KDM4C the strongest with an IC 50 of 1.9 μM. KDM5-IN-1 still displays more than 100-fold selectivity for KDM4C vs. KDM5A. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
When dosed orally in mice at 50 mg/kg twice a day, KDM5-IN-1 shows an unbound maximal plasma concentration C max >15-fold over its cell EC 50 , thereby providing a robust chemical probe for studying KDM5 biological functions in vivo . MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Form:Solid
IC50& Target:IC50: 15.1 nM (KDM5),EC50: 0.34 μM (PC9 H3K4Me3)