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PYZD-4409  ≥98%

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包装规格：5mg 10mg 50mg 100mg in glass bottle
溶解性：溶于DMSO(≥35mg/mL)
产品描述：一种ubiquitin-activating enzyme UBA1 的特异性抑制剂，其 IC50 值为 20 μM。PYZD-4409 能诱导恶性细胞死亡，并优先抑制原发性急性髓性白血病细胞的生长。 PYZD-4409 is an inhibitor of ubiquitin-activating enzyme UBA1 (E1). PYZD-4409 induced cell death in malignant cells and preferentially inhibited the clonogenic growth of primary acute myeloid leukemia cells compared with normal hematopoietic cells. Mechanistically, genetic or chemical inhibition of E1 increased expression of E1 stress markers. Moreover, BI-1 overexpression blocked cell death after E1 inhibition, suggesting ER stress is functionally important for cell death after E1 inhibition. Finally, in a mouse model of leukemia, intraperitoneal administration of PYZD - 4409 decreased tumor weight and volume compared with control without untoward toxicity.
保存条件：-20℃

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