Description
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.
Product information
CAS Number: 423148-78-1
Molecular Weight: 351.67
Formula: C14H7ClFN3O5
Chemical Name: 1-(3-Chloro-4-fluorophenyl)-4-[(5-nitro-2-furanyl)methylene]-3,5-pyrazolidinedione
Smiles: [O-][N+](=O)C1=CC=C(C=C2C(=O)NN(C3=CC(Cl)=C(F)C=C3)C2=O)O1
InChiKey: MSYMKEYWUWVZQY-RMKNXTFCSA-N
InChi: InChI=1S/C14H7ClFN3O5/c15-10-5-7(1-3-11(10)16)18-14(21)9(13(20)17-18)6-8-2-4-12(24-8)19(22)23/h1-6H,(H,17,20)/b9-6+
Technical Data
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: ≥12 months 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
In Vitro:
PYZD-4409 was used at 10-30 µM final concentration in various in vitro assays.
In Vivo:
PYZD-4409 was dosed intraperitoneally to the mouse model of leukemia (MDAY-D2 murine leukemia cells) at 10 mg/kg once per day.
References:
- 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.
Products are for research use only. Not for human use.
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