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PYZD-4409

Catalog No. T16699 CAS 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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PYZD-4409, CAS 423148-78-1

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Purity: 98%

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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.
Targets&IC50	ubiquitin-activating enzyme UBA1:20 μM
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].

Molecular Weight	351.67
Formula	C14H7ClFN3O5
CAS No.	423148-78-1

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 35 mg/mL (99.53 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. Xu GW, et al. The ubiquitin-activating enzyme E1 as a therapeutic target for the treatment of leukemia and multiple myeloma. Blood. 2010 Mar 18;115(11):2251-9.

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Keywords

PYZD-4409 423148-78-1 泛素化其他 Others E1/E2/E3 Enzyme Inhibitor PYZD 4409 E3 ligating enzyme E2 conjugating enzyme inhibit Ubiquitin activating enzyme E1 activating enzyme Ubiquitin ligase Ubiquitin conjugating enzyme PYZD4409 inhibitor

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