(R)-OR-S1 is a potent inhibitor of histone methyltransferases EZH1 and EZH2, exhibiting selective dual activity against both enzymes. This reagent has demonstrated the capacity to induce cell differentiation and apoptosis in acute myeloid leukemia (AML) cells, suggesting its potential application in targeted therapy. Notably, (R)-OR-S1 does not lead to significant myelosuppression, allowing for normal hematopoiesis to persist post-treatment, especially when combined with cytarabine. These properties highlight (R)-OR-S1’s promise as a clinically tolerable option for patients undergoing PRC2-targeted treatment in AML.
(R)-OR-S1 is a potent inhibitor of histone methyltransferases EZH1 and EZH2, exhibiting selective dual activity against both enzymes. This reagent has demonstrated the capacity to induce cell differentiation and apoptosis in acute myeloid leukemia (AML) cells, suggesting its potential application in targeted therapy. Notably, (R)-OR-S1 does not lead to significant myelosuppression, allowing for normal hematopoiesis to persist post-treatment, especially when combined with cytarabine. These properties highlight (R)-OR-S1’s promise as a clinically tolerable option for patients undergoing PRC2-targeted treatment in AML.
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