WP1130 (Degrasyn) | USP9X inhibitor, USP5 inhibitor

Chemical Structure : WP1130

CAS No.: 856243-80-6

WP1130 (Degrasyn, WP-1130)

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
5 mg	$58	In stock
10 mg	$88	In stock
25 mg	$138	In stock
50 mg	$218	In stock
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Biological Activity

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), inhibits deubiquitinases USP9x, USP5, USP14, and UCH37 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.

Physicochemical Properties

M.Wt	384.27
Formula	C19H18BrN3O
Appearance	Solid
CAS No.
Storage	Solide Powder -20 °C 12 Months; 4°C 6 Months	In Solvent -80 °C 6 Months; -20°C 6 Months
Shipping
Solubility	DMSO: ≥ 33 mg/mL
Chemical Name/SMILES	2-Propenamide, 3-(6-bromo-2-pyridinyl)-2-cyano-N-[(1S)-1-phenylbutyl]-, (2E)-

References

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.

WP1130 (Degrasyn, WP-1130)

Biological Activity

Physicochemical Properties

References

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