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PYZD-4409

PYZD-4409
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PYZD-4409

Catalog No. T16699Cas No. 423148-78-1
PYZD-4409 is a selective UBA1 inhibitor with an IC50 of 20 μM. PYZD-4409 induces cell death in malignant cells and is preferentially cytotoxic to malignant cells over normal hematopoietic cells.
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Pack SizePrice/USDAvailabilityQuantity
1 mg$32In Stock
5 mg$73In Stock
10 mg$123In Stock
25 mg$228In Stock
50 mg$372In Stock
100 mg$538In Stock
500 mg$1,150In Stock
1 mL x 10 mM (in DMSO)$80In Stock
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Product Introduction

Bioactivity
Description
PYZD-4409 is a selective UBA1 inhibitor with an IC50 of 20 μM. PYZD-4409 induces cell death in malignant cells and is preferentially cytotoxic to malignant cells over normal hematopoietic cells.
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 and the unfolded protein response. PYZD-4409 (50 μM; 4 hours; K562 leukemia cells) treatment blocks 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 AML 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 [1].
In vivo
PYZD-4409 (10 mg/kg; intraperitoneal injection; daily on alternate days; for 16 days; male severe combined immunodeficient mice) reduces tumor weight and volume[1].
Chemical Properties
Molecular Weight351.67
FormulaC14H7ClFN3O5
Cas No.423148-78-1
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year
Solubility Information
DMSO: 35 mg/mL (99.53 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.8436 mL14.2179 mL28.4357 mL142.1787 mL
5 mM0.5687 mL2.8436 mL5.6871 mL28.4357 mL
10 mM0.2844 mL1.4218 mL2.8436 mL14.2179 mL
20 mM0.1422 mL0.7109 mL1.4218 mL7.1089 mL
50 mM0.0569 mL0.2844 mL0.5687 mL2.8436 mL

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