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Sep. 18, 2021

M3258: An Orally Available, Selective, and Reversible Inhibitor of LMP7

M3258

sel. reversible cov. immunoproteosome inh. oral efficacy (1 mpk) in xeno., Ph. I in MM from SBDD Mol. Cancer Ther., May 27, 2021 Merck KGaA, Darmstadt, DE

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Drug Hunter Team

The Merck LMP7 inhibitor, M3258 , is an orally available, selective, and reversible inhibitor of the immunoproteasome proteolytic subunit, LMP7. In contrast to the constitutive proteasome, the immunoproteasome is predominantly expressed in hematolymphoid cells such as in multiple myeloma cells. Pan-proteasome inhibitors (pan-PIs) such as [...]

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