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Compound class: Synthetic organic
|Data from WO2010149944 indicates that ISA-2011B (eq. Analogue 1) causes apoptotic cell death in PC-3 cells (human prostate cells) with an EC50 of 36µM . The compound downregulates the expression of PIP5K1A  and is active in vitro and in in vivo xenografted mice. Kinase profile screening of ISA-2011B across 460 kinases (covering >80% of the human catalytic protein kinome) identified several high affinity targets including PIP5K1A, MAP/microtubule affinity-regulating kinase 1 and 4 (MARK1 and MARK4)  and BR serine/threonine kinase 2 (BRSK2) .
We have tagged PIP5K1A as the primary molecular target of ISA-2011B based on the target validation experiments reported by Semenas et al (2014) .
|Selectivity at enzymes|
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