PYZD-4409

SKU: orb1307822

Description

PYZD-4409

Research Area

Protein Biochemistry

Key Properties

• CAS Number: 423148-78-1
• MW: 351.67
• Purity: 99.71%
• Formula: C₁₄H₇ClFN₃O₅
• SMILES: [O-][N+](=O)c1ccc(\C=C2\C(=O)NN(C2=O)c2ccc(F)c(Cl)c2)o1
• Target: E1/E2/E3 Enzyme
• Solubility: DMSO:6 mg/mL (17.06 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (2.84 mM)

Bioactivity

• Target IC50:
  Ubiquitin-activating enzyme UBA1:20 μM
• In Vivo:
  PYZD-4409 (10 mg/kg; intraperitoneal injection; administered every Other day for 16 dayss; Male severe combined immunodeficient mice) reduces tumor weight and volum.
• In Vitro:
  PYZD-4409 is preferentially cytotoxic to malignant cells over normal hematopoietic cells. PYZD-4409 increases levels of phospho-JNK and phospho-p38 mitogen-activated protein kinase, which have also been linked to ER stress an the unfolded protein response. PYZD-4409 50 μM; 4 hours; K562 leukemia cells) treatment block the E1-dependent conjugation of ubiquitin to the E2 enzyme cdc34. PYZD-4409 (0-25 μM; 24 hours; K562 leukemia cells) significantly increases both mRNA and protein levels of Grp78 and Hsp70. PYZD-4409 (10-40 μM; 72 hours; myeloma, leukemia, and solid tumor cell lines, Primary mL cells and normal hematopoietic cells) induces cell death with an LD50 less than 10 μM in 5 of 8 leukemia and myeloma cell lines. Solid tumor cell lines were less sensitive with an LD50 of approximately 15 to 20 μM.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Disclaimer: For research use only

Alternative Names

inhibit, Inhibitor, E3Enzyme, E3 ligating enzyme, E2Enzyme, E3 Enzyme, E1 activating enzyme, E1/E2/E3 Enzyme, E1 Enzyme, E2 Enzyme, E1Enzyme, E2 conjugating enzyme, Ubiquitin ligase, ubiquitin-activating enzyme UBA1, Ubiquitin conjugating enzyme, Ubiquitin activating enzyme, UBA1, PYZD4409, PYZD-4409, PYZD 4409

Compound Identifiers

PubChem CID

60111983