(E)-1-(3-chloro-4-fluorophenyl)-4-((5-nitrofuran-2-yl)Methylene)pyrazolidine-3,5-dione
- Product Name
- (E)-1-(3-chloro-4-fluorophenyl)-4-((5-nitrofuran-2-yl)Methylene)pyrazolidine-3,5-dione
- CAS No.
- 423148-78-1
- Chemical Name
- (E)-1-(3-chloro-4-fluorophenyl)-4-((5-nitrofuran-2-yl)Methylene)pyrazolidine-3,5-dione
- Synonyms
- PYZD 4409;PYZD4409;PYZD 4409;PYZD-4409 >=98% (HPLC);PYZD-4409, 10 mM in DMSO;1-(3-Chloro-4-fluorophenyl)-4-[(5-nitro-2-furanyl)methylene]-3,5-pyrazolidinedione;3,5-Pyrazolidinedione, 1-(3-chloro-4-fluorophenyl)-4-[(5-nitro-2-furanyl)methylene]-;(E)-1-(3-chloro-4-fluorophenyl)-4-((5-nitrofuran-2-yl)Methylene)pyrazolidine-3,5-dione;Inhibitor,PYZD 4409,E3 ligating enzyme,E2 conjugating enzyme,PYZD-4409,inhibit,E1/E2/E3 Enzyme,Ubiquitin activating enzyme,E1 activating enzyme,Ubiquitin ligase,Ubiquitin conjugating enzyme,PYZD4409;(E)-1-(3-chloro-4-fluorophenyl)-4-((5-nitrofuran-2-yl)Methylene)pyrazolidine-3,5-dione 3,5-Pyrazolidinedione, 1-(3-chloro-4-fluorophenyl)-4-[(5-nitro-2-furanyl)methylene]-
- CBNumber
- CB82609290
- Molecular Formula
- C14H7ClFN3O5
- Formula Weight
- 351.67
- MOL File
- 423148-78-1.mol
(E)-1-(3-chloro-4-fluorophenyl)-4-((5-nitrofuran-2-yl)Methylene)pyrazolidine-3,5-dione Property
- Density
- 1.662±0.06 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- Soluble in DMSO
- form
- solid
- pka
- 7.12±0.20(Predicted)
- color
- Brown
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Danger
- Hazard statements
-
H301Toxic if swalloed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P302+P352IF ON SKIN: wash with plenty of soap and water.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- SML1188
- Product name
- PYZD-4409
- Purity
- ≥98% (HPLC)
- Packaging
- 5mg
- Price
- $103
- Updated
- 2025/07/31
- Product number
- 4994
- Product name
- PYZD4409
- Purity
- ≥98%(HPLC)
- Packaging
- 10
- Price
- $216
- Updated
- 2021/12/16
- Product number
- 4994
- Product name
- PYZD4409
- Purity
- ≥98%(HPLC)
- Packaging
- 50
- Price
- $906
- Updated
- 2021/12/16
- Product number
- 256376
- Product name
- PYZD 4409
- Packaging
- 10mg
- Price
- $480
- Updated
- 2021/12/16
- Product number
- CS-1725
- Product name
- PYZD-4409
- Purity
- >98.0%
- Packaging
- 50mg
- Price
- $540
- Updated
- 2021/12/16
(E)-1-(3-chloro-4-fluorophenyl)-4-((5-nitrofuran-2-yl)Methylene)pyrazolidine-3,5-dione Chemical Properties,Usage,Production
Uses
PYZD-4409 is a specific inhibitor of the ubiquitin-activating enzyme UBA1 with an IC50 of 20 μM (cell-free enzymatic assay). PYZD-4409 induces cell death in malignant cells and preferentially inhibits the clonogenic growth of primary acute myeloid leukemia cells[1].
Biological Activity
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].
in vivo
PYZD-4409 (10 mg/kg; intraperitoneal injection; daily on alternate days; for 16 days; male severe combined immunodeficient mice) decreases tumor weight and volume without untoward toxicity[1].
| Animal Model: | Male severe combined immunodeficient (SCID) mice with MDAY-D2 murine leukemia cells[1] |
| Dosage: | 10 mg/kg |
| Administration: | Intraperitoneal injection; daily on alternate days; for 16 days |
| Result: | Delayed tumor growth and decreased tumor weight without untoward toxicity. |
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.
(E)-1-(3-chloro-4-fluorophenyl)-4-((5-nitrofuran-2-yl)Methylene)pyrazolidine-3,5-dione Preparation Products And Raw materials
Raw materials
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