Molecular Weight(MW): 384.27
Degrasyn (WP1130) is a selective deubiquitinase (DUB: USP5, UCH-L1, USP9x, USP14, and UCH37) inhibitor and also suppresses Bcr/Abl, also a JAK2 transducer (without affecting 20S proteasome) and activator of transcription (STAT).
Cited by 10 Publications
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HEK-293 cells expressing Strep-CLASPIN were first arrested in S-phase with HU or in mitosis with nocodazole. Cycloheximide was then added to prevent further protein synthesis in the presence or absence of the USP9X inhibitor WP1130 and samples were harvested at the indicated times. A sample from the same cell line uninduced (U) was loaded as control.
Cancer Res, 2016, 76(8):2384-93. Degrasyn (WP1130) purchased from Selleck.
SF188, U251 and T98G glioblastoma cells were treated for 24 h with increasing concentrations of WP1130 under serum starvation. Whole-cell extracts were examined by Western blot for Usp9X, Bag3, Mcl-1, Bcl-2, Bcl-xL, XIAP and Survivin. Actin served as a loading control.
Oncotarget, 2016, 7(11):12791-805. Degrasyn (WP1130) purchased from Selleck.
The inhibitors of DUBs and UBE1 inhibited HSV-2 replication. HEC-1-A cells were either infected or not infected in the presence of WP1130 (2 ug/ml) or PYR-41 (20 ug/ml). Levels of ubiquitin conjugates, IκB-α, and gD were determined 24 h p.i.
J Virol 2013 87(15), 8675-86. Degrasyn (WP1130) purchased from Selleck.
USP9X activity regulates Mcl-1 expression. (b) A549 cells were plated in 10 cm tissue culture dishes and upon reaching 70% confluency were treated with 10 μg/ml CHX for 6 h or exposed to a combination of 7.5 μM WP1130 for 2, 4 and 6 h and 10 μg/ml CHX for 6 h. Mcl-1 and USP9X signals were then determined by western blotting. Proteins were quantified using UN-SCAN-IT. Those intensities of the signals of USP-9X and Mcl-1 are relative to Actin.
BMC Cancer 2012 12, 541. Degrasyn (WP1130) purchased from Selleck.
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Choose Selective Bcr-Abl Inhibitors
|Description||Degrasyn (WP1130) is a selective deubiquitinase (DUB: USP5, UCH-L1, USP9x, USP14, and UCH37) inhibitor and also suppresses Bcr/Abl, also a JAK2 transducer (without affecting 20S proteasome) and activator of transcription (STAT).|
|Features||WP1130 has an advantage over imatinib mesylate in that its activity is not inhibited by a variety of Abl kinase mutations, including T315I.|
In addition to inducing rapid down-regulation of Bcr/Abl without affecting Bcr or c-Abl, WP1130 also regulates the stability of Jak2 and c-Myc without affecting other kinases (HER1, HER2, c-Kit, FAK, ERK1, ERK2, Akt, Btk, Src and Src-related kinases) or transcription factors (wild-type p53, STAT1, STAT3, STAT5, c-Jun, NF-κB, and Max). Unlike adaphostin and Trisenox, WP1130 induces down-regulation of Bcr/Abl within 60 minutes. WP1130 is more effective in inducing apoptosis of myeloid and lymphoid tumor cells with IC50 of ~0.5-2.5 μM compared with normal CD34+ hematopoietic precursors, dermal fibroblasts, or endothelial cells with IC50 of ~5-10 μM. WP1130 (5 μM) specifically and rapidly down-regulates both wild-type and T315I mutant Bcr/Abl protein without affecting bcr/abl gene expression or engaging the proteasomal degradation pathway in chronic myelogenous leukemia (CML) cells, accompanied by induction of apoptosis. WP1130 is more effective in reducing leukemic cell colony formation compared with normal progenitor cells, and effective against primary leukemic cells harboring the T315I mutation.  WP1130 induces rapid proteasomal-dependent degradation of c-Myc protein in MM-1 multiple myeloma and other tumor cell lines, correlated with tumor growth inhibition.  Unlike AG490, WP1130 acts as a partly selective deubiquitinase (DUB) inhibitor to induce a rapid and marked accumulation of polyubiquitinated (K48/K63-linked) proteins into juxtanuclear aggresomes without affecting proteasome activity. WP1130 (5 μM) directly inhibits DUB activity of USP9x, USP5, USP14, UCH-L1, and UCH37, but not UCH-L3, resulting in downregulation of antiapoptotic and upregulation of proapoptotic proteins, such as MCL-1 and p53. 
|In vivo||Administration of WP1130 inhibits the growth of K562 tumors as well as both wildtype Bcr/Abl and T315I mutant Bcr/Abl-expressing BaF/3 cells transplanted into nude mice.  Consistent with the down-regulation of c-Myc, WP1130 displays potent inhibitory activity against A375 melanoma tumors established in nude mice. |
|In vitro||DMSO||77 mg/mL (200.37 mM)|
|Ethanol||18 mg/mL (46.84 mM)|
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