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Trilaciclib is a CDK4/6 inhibitor with IC50s of 1 nM/4 nM for CDK4/6, respectively. Use for chemotherapy-induced myelosuppression in vivo.
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Lenalidomide, a CRBN ligand, is an orally active immunomodulator that effective treatment for myelodysplastic syndrome and multiple myeloma.
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PHT-7.3 is a selective inhibitor of Cnk1 pleckstrin homology (PH) domain. PHT 7.3 blocks the growth of mutant KRAS cells and tumors.
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2021-05-27Butaprost is a selective prostaglandin E receptor (EP2) agonist. Butaprost can effectively mitigate kidney fibrogenesis in various fibrosis models.
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FTI-277 is a farnesyl transferase inhibitor, selectively blocks oncogenic Ras signaling. It inhibits hepatitis delta virus infection.
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Lonafarnib is a potent and orally active farnesyl transferase inhibitor, and it inhibits the activities of H-ras, K-ras and N-ras.
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DT-061 is an Orally Active PP2A Activator. PP2A inhibition is a druggable MEK inhibitor resistance mechanism.
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GSK973, a selective, orally bioavailable inhibitor of the BD2s of the BET family, shows good potency against BRD2 BD2, BRD3 BD2 and BRDT BD2.
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BI-3406 is a selective, orally bioavailable SOS1 inhibitor that binds to the catalytic domain of SOS1, preventing the interaction with KRAS.
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PROTAC MDM2 degrader MD-222 is highly potent and effective in inducing degradation of MDM2 and in activating wild-type p53 in cells.
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