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Chemical Structure : WP1130
CAS No.: 856243-80-6
Catalog No.: PC-43444Not For Human Use, Lab Use Only.
WP1130 (Degrasyn) is a small molecule that specifically and rapidly down-regulates both wild-type and mutant Bcr/Abl protein without affecting bcr/abl gene expression (IC50=1.8 uM), also inhibits deubiquitinases and blocks autophagy.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 25 mg | $188 | In stock | |
| 50 mg | $288 | In stock | |
| 100 mg | $458 | In stock | |
| 200 mg | Get quote | ||
| 1 g | Get quote |
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WP1130 (Degrasyn) is a small molecule that specifically and rapidly down-regulates both wild-type and mutant Bcr/Abl protein without affecting bcr/abl gene expression (IC50=1.8 uM), also inhibits deubiquitinases and blocks autophagy.
WP1130 reduces leukemic versus normal hematopoietic colony formation and strongly inhibits colony formation of cells derived from patients with T315I mutant Bcr/Abl-expressing CML in blast crisis.
WP1130 suppresses the growth of K562 heterotransplanted tumors as well as both wild-type Bcr/Abl and T315I mutant Bcr/Abl-expressing BaF/3 cells in vivo.
WP1130 acts as a partly selective DUB inhibitor, directly inhibiting DUB activity of USP9x, USP5, USP14, and UCH37, triggers aggresome formation and tumor cell apoptosis.
| M.Wt | 384.27 | |
| Formula | C19H18BrN3O | |
| Appearance | Solid | |
| Storage |
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| Solubility |
DMSO: ≥ 33 mg/mL |
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| Chemical Name/SMILES |
2-Propenamide, 3-(6-bromo-2-pyridinyl)-2-cyano-N-[(1S)-1-phenylbutyl]-, (2E)- |
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1. Bartholomeusz GA, et al. Blood. 2007 Apr 15;109(8):3470-8.
2. Bartholomeusz G, et al. Cancer Res. 2007 Apr 15;67(8):3912-8.
3. Kapuria V, et al. Cancer Res. 2010 Nov 15;70(22):9265-76.
4. Drießen S, et al. Autophagy. 2015;11(9):1458-70.
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