681685

WP1130

A cell-permeable tyrphostin compound that acts as a partially selective deubiquitinase (DUB) inhibitor and suppresses JAK-Stat signaling pathway.

• Synonym(s): WP1130, Degrasyn
• Empirical Formula (Hill Notation): C₁₉H₁₈BrN₃O
• CAS Number: 856243-80-6
• Molecular Weight: 384.27
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• Quality Level: 100
• assay: ≥97% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: light yellow
• solubility: DMSO: 100 mg/mL
• shipped in: ambient
• storage temp.: 2-8°C

Description

General description

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-κB activities (IC₅₀<1 M in MCL cells) leading to tumor cell apoptosis (IC₅₀ ~1.2 M in Z138 cells). Suggested to modify active site cysteine of DUB and inhibit USP5, UCH-L1, USP9x, USP14, and UCH37 activities (≥80% inhibition at 5 M) 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.

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-κB activities (IC₅₀<1 µM in MCL cells) leading to tumor cell apoptosis (IC₅₀ ~1.2 µM in Z138 cells). Suggested to modify active site cysteine of DUB and inhibit USP5, UCH-L1, USP9x, USP14, and UCH37 activities (≥80% inhibition at 5 µM) without affecting 20S proteasome. Reported to exert stronger antiproliferative and antitumor properties than STAT3 Inhibitor III, WP1066 (Cat. No. 573097) in xenograft mouse models of CML and melanoma.

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Other Notes

Kapuria, V., et al. 2010. Cancer Res.70, 9265.
Pham, L.V., et al. 2010. Mol. Cancer Ther.9, 2026.
Bartholomeusz, G.A, et al. 2007. Cancer Res.67, 3912.

Bartholomeusz, G.A, et al. 2007. Blood109, 3470.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 2
• flash_point_f: Not applicable
• flash_point_c: Not applicable