YM 298198 Hydrochloride is a non-competitive antagonist with high affinity and selectivity for mGlu1 receptors (Ki = 19 nM). YM 298198 Hydrochloride is inactive at other mGlu receptor subtypes (mGlu2-7), ionotropic receptors and glutamate transporters (IC50 > 10 μM). It inhibits glutamate-induced IP production more potently than CPCCOEt (IC50 values are 16 nM and 6.3 μM respectively).
YM-202074 is a high affinity, selective metabotropic glutamate receptor type 1 (mGlu1) antagonist. YM-202074 binds an allosteric site of the rat mGlu1 receptor with a Ki of 4.8 nM. It inhibits mGlu1-mediated inositol phosphates production (IC50 = 8.6 nM in rat cerebellar granule cells).
DCYM21 is an inhibitor of menin-MLL interaction. DCYM21 demonstrates potent and selective blockage of proliferation and induces both cell cycle arrest and differentiation of leukemia cells harboring MLL translocations.