Product Name :
PYZD-4409 — Ubiquitin-activating Enzyme (E1) Inhibitor

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.

CAS:
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+

Purity:
≥98% (or refer to the Certificate of Analysis)

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.

Additional information:
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.{{Busulfan} site|{Busulfan} Cell Cycle/DNA Damage|{Busulfan} Purity & Documentation|{Busulfan} In Vivo|{Busulfan} manufacturer|{Busulfan} Cancer} |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.{{Ripretinib} site|{Ripretinib} Apoptosis|{Ripretinib} Technical Information|{Ripretinib} In stock|{Ripretinib} supplier|{Ripretinib} Autophagy} |Shelf Life: ≥12 months if stored properly.PMID:23376608 |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.|Documents||

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