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ML-00253764 is a brain penetrant nonpeptidic melanocortin receptor 4 (MC4R) antagonist with a Ki/IC50 of 0.16 µM/0.103 µM, respectively.
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AZD1208 is a potent, selective, ATP-competitive, and orally active pan-Pim kinase inhibitor. AZD1208 inhibits acute myeloid leukaemia.
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SB-332235 is a potent, orally active nonpeptide CXCR2 antagonist. SB-332235 inhibits acute and chronic models of arthritis in the rabbit.
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LYN-1604, a potent ULK1 activator, induces cell death involved in ATF3, RAD21, and caspase3, accompanied by autophagy and apoptosis.
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MS049 is a potent, selective dual inhibitor of PRMT4 and PRMT6. MS049 reduces levels of Med12me2a and H3R2me2a in HEK293 cells.
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L-Moses is the first potent, selective, and cell-active PCAF Brd inhibitor. L-Moses disrupts PCAF-Brd histone H3.3 interaction.
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Miransertib is an orally active, selective and allosteric Akt inhibitor. Miransertib is also a potent the AKT1-E17K mutant protein inhibitor.
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BMS-354825 is a dual Src and Abl kinase inhibitor. Antitumor activity. Orally active in the chronic myelogenous leukemia.
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APS-2-79 is a MEK inhibitor. Stabilization of the KSR inactive state. An effective strategy to target other pseudokinases.
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Retro-2 is an inhibitor of retrograde protein trafficking at the endosome-trans-Golgi network interface. Retro-2 induces cell autophagy
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