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PYZD-4409

In stock
Catalog No.
B1244
E1 enzyme inhibitor
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$155.00
In stock
5mg
$140.00
Please inquiry
10mg
$231.00
In stock
50mg
$702.00
In stock
100mg
$1,014.00
Please inquiry

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

PYZD-4409 is a novel small molecule inhibitor of the ubiquitin-activating enzyme E1 with IC50 value of 20μM [1].

The ubiquitin-activating enzyme E1 is involved in the fist step of protein degradation. It uses ATP to adenylate and transfers the ubiquitin molecule to the next enzyme E2. It is demonstrated that the ubiquitination pathway is increased in the primary leukemia cells. Thus, inhibition of E1 can be a target of hematologic malignancies treatment. PYZD-4409 is screened out from a chemical library based on the pyrazolidine pharmacophore. The IC50 value(20μM) of it has been evaluated in a cell-free enzymatic assay. PYZD-4409 can also inhibit E1 in cultured K562 leukemia cells. PYZD-4409 causes cell death in leukemia, myeloma and solid tumor cell lines. In clonogenic growth assays, PYZD-4409 is found to reduce the growth of AML cells over normal hematopoietic cells. As an essential role of protein degradation, the inhibition of E1 resluts in the increased amounts of cyclin D3 and p53 [1].

References:
[1] G. Wei Xu, Mohsin Ali, Tabitha E. Wood et al. The ubiquitin-activating enzyme E1 as a therapeutic target for the treatment of leukemia and multiple myeloma. Blood. 2010, 115(11): 2251-2259.

Chemical Properties

Physical AppearanceBrown solid
StorageStore at -20°C
M.Wt351.67
Cas No.423148-78-1
FormulaC14H7ClFN3O5
SolubilitySoluble in DMSO
Chemical Name(4E)-1-(3-chloro-4-fluorophenyl)-4-[(5-nitrofuran-2-yl)methylidene]pyrazolidine-3,5-dione
SDFDownload SDF
Canonical SMILESC1=CC(=C(C=C1N2C(=O)C(=CC3=CC=C(O3)[N+](=O)[O-])C(=O)N2)Cl)F
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Biological Activity

Description PYZD-4409 is a small-molecule inhibitor of ubiquitin-activating enzyme (E1) with IC50 value of 20 μM.
Targets E1          
IC50 20 μM          

Quality Control

Quality Control & MSDS

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Chemical structure

PYZD-4409