Birabresib (OTX015, MK 8628) is a potent BET bromodomain inhibitor with EC50 ranging from 10 to 19 nM for BRD2, BRD3, and BRD4 in cell-free assays. Birabresib inhibits the expression of Nuclear receptor binding SET domain protein 3 (NSD3) target genes.
More Information Supplier PageAdipoRon (SC-396658) is a novel, and orally bioavailable adiponectin receptor agonist with KD of 1.8 and 3.1 μM for AdipoR1 and AdipoR2, respectively.
More Information Supplier PageLY2119620 is a specific, and allosteric agonist of human M2 and M4 muscarinic acetylcholine receptors.
More Information Supplier PageLY2119620 is a specific, and allosteric agonist of human M2 and M4 muscarinic acetylcholine receptors.
More Information Supplier PageGNE-0877 (DNL201) is a highly potent and selective leucine-rich repeat kinase 2 (LRRK2) inhibitor with Ki of 0.7 nM.
More Information Supplier PageGNE-9605 is a highly potent and selective leucine-rich repeat kinase 2 (LRRK2) inhibitor with Ki and IC50 of 2 nM and 19 nM, respectively.
More Information Supplier PageUNC2250 is a potent and selective Mer inhibitor with IC50 of 1.7 nM, about 160- and 60-fold selectivity over the closely related kinases Axl/Tyro3.
More Information Supplier PageURMC-099 is an orally bioavailable, brain penetrant mixed lineage kinase (MLK) inhibitor with IC50 of 19 nM, 42 nM, 14 nM, and 150 nM, for MLK1, MLK2, MLK3, and DLK, respectively, and also inhibits LRRK2 activity with IC50 of 11 nM. URMC-099 also inhibits ABL1 with IC50 of 6.8 nM. URMC-099 induces autophagy.
More Information Supplier PageJSH-23 is an inhibitor of NF-κB transcriptional activity, which inhibits LPS-stimulated nuclear factor (NF)-κB transcriptional activity in RAW 264.7 cells with an IC50 value of 7.1 μM, and interferes with LPS-induced NF-κB nuclear translocation without affecting IκB degradation.
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