PYZD-4409 is a novel potent, selective and cell permeable inhibitor of ubiquitin-activating enzyme (E1). It induces cell death in hematologic malignant cell lines and primary patient samples preferentially over normal hematopoietic cells. PYZD-4409 blocks degradation of the short-lived proteins p53 and cyclin D3. It inhibits NF-κB activation and induces cell death associated with ER stress. It also displays antitumor effects in a mouse model of leukemia by intraperitoneal administration of the drug.
CAS Number: 423148-78-1
Molecular Weight: 351.67
Chemical Name: 1-(3-Chloro-4-fluorophenyl)-4-[(5-nitro-2-furanyl)methylene]-3,5-pyrazolidinedione
Appearance: Solid Power.
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO up to 100 mM
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥360 days if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined.
HS Tariff Code: 382200
How to use
PYZD-4409 was used at 10-30 µM final concentration in various in vitro assays.
PYZD-4409 was dosed intraperitoneally to the mouse model of leukemia (MDAY-D2 murine leukemia cells) at 10 mg/kg once per day.
- Xu GW, et al. The ubiquitin-activating enzyme E1 as a therapeutic target for the treatment of leukemia and multiple myeloma. (2010) Blood. 115(11):2251-9.
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