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PYZD-4409, Ubiquitin-activating Enzyme (E1) Inhibitor

PYZD-4409, Ubiquitin-activating Enzyme (E1) Inhibitor

$139.00
A novel potent, selective and cell permeable inhibitor of ubiquitin-activating enzyme (E1).
Catalog No. Unit Price Qty
M60213-2s 2 mg solid $139.00

Details

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. 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. 

Description

Details

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. 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. 

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