产品详情
简单介绍：
PYZD-4409,Ubiquitin-activatingEnzyme(E1)Inhibitor
详情介绍：
Product Information
| Molecular Weight: | 351.67 |
| Formula: | C14H7ClFN3O5 |
| Purity: | ≥98% |
| CAS#: | 423148-78-1 |
| Solubility: | DMSO up to 100 mM |
| Chemical Name: | 1-(3-Chloro-4-fluorophenyl)-4-[(5-nitro-2-furanyl)methylene]-3,5-pyrazolidinedione |
| Storage: | Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year. |
Biological Activity:
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.
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.
Reference:
- 1.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.
相关文章
