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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.
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.
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | $32 | In Stock | |
| 5 mg | $73 | In Stock | |
| 10 mg | $123 | In Stock | |
| 25 mg | $228 | In Stock | |
| 50 mg | $372 | In Stock | |
| 100 mg | $538 | In Stock | |
| 500 mg | $1,150 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $80 | In Stock |
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Purity:98.00%
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All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.Product Introduction
Bioactivity
Chemical Properties
| 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; administered every other day 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 & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||
| Solubility Information | DMSO: 6 mg/mL (17.06 mM), Sonication is recommended.  | ||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||
DMSO
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(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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