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217878 WP1130 (Degrasyn) CAS:

Specifications
Grade
Highly Purified
Molecular Formula
C19H18BrN3O
Molecular Weight
384.3
EU Commodity Code
38220090
Shipping Temp
Blue Ice
Storage Temp
-20°C

A cell-permeable tyrphostin compound that acts as a partially selective deubiquitinase (DUB) inhibitor and suppresses JAK-Stat signaling pathway. Reported to cause accumulation of polyubiquitinated p53, JAK2 and Bcr-Abl, and reduce c-Myc and MCL-1 protein levels in several tumor cells and downregulate Stat3 and NF-kB activities (IC50 < 1uM in MCL cells) leading to tumor cell apoptosis (IC50 ~1.2uM in Z138 cells). Suggested to modify active site cysteine of DUB and inhibit USP5, UCH-L1, USP9x, USP14, and UCH37 activities (≥80% inhibition at 5uM) without affecting 20S proteasome. Reported to exert stronger antiproliferative and antitumor properties than STAT3 Inhibitor III, WP1066 in xenograft mouse models of CML and melanoma.

Formula
C19H18BrN3O
Solubility
DMSO
Molecular Weight
384.3
Storage and Stability
Lyophilized powder may be stored at -20°C. Stable for 12 months at -20°C. Reconstitute with sterile buffer or dH2O. Aliquot to avoid repeated freezing and thawing. Store at -20°C. For maximum recovery of product, centrifuge the original vial after thawing and prior to removing the cap. Further dilutions can be made in assay buffer.
Purity
~97% (HPLC)
Concentration
Not determined
Form
Supplied as a light yellow solid.
Important Note
This product as supplied is intended for research use only, not for use in human, therapeutic or diagnostic applications without the expressed written authorization of United States Biological.
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