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Chemical Structure| 856243-80-6 Chemical Structure| 856243-80-6

Structure of Degrasyn
CAS No.: 856243-80-6

Chemical Structure| 856243-80-6

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WP1130 is a selective small molecular deubiquitinase (USP5, UCH-L1, USP9x, USP14, and UCH37) inhibitor and a Bcr/Abl destruction pathway activator with an IC50 of 1.8 μM for K562 cells.

Synonyms: Wp1130

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Product Details of Degrasyn

CAS No. :856243-80-6
Formula : C19H18BrN3O
M.W : 384.27
SMILES Code : O=C(N[C@H](C1=CC=CC=C1)CCC)/C(C#N)=C/C2=NC(Br)=CC=C2
Synonyms :
Wp1130
MDL No. :MFCD18839228
InChI Key :LIDOPKHSVQTSJY-VMEIHUARSA-N
Pubchem ID :11222830

Safety of Degrasyn

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of Degrasyn

RTK

Isoform Comparison

Biological Activity

Target
  • Bcr-Abl

    Bcr-Abl, IC50:1.8 μM

  • DUB

In Vitro:

Cell Line
Concentration Treated Time Description References
VCaP cells 5 μM 24 hours WP1130 treatment significantly reduced ERG protein levels PMC3964108
HeLa cells 5 μM 4 hours WP1130 treatment caused a rapid increase in ubiquitinated ERG levels PMC3964108
KYSE-150 cells 2.5 µM 24 hours Degrasyn significantly reduced the proliferative capacity of KYSE-150 cells and combined with X-ray treatment significantly enhanced the sensitivity of radioresistant cells. PMC11699344
TE-12 cells 2.5 µM 24 hours Degrasyn significantly reduced the proliferative capacity of TE-12 cells and combined with X-ray treatment significantly enhanced the sensitivity of radioresistant cells. PMC11699344
LP1 cells 0.5 μM 24 hours Evaluating the effect of mebendazole on μM cell apoptosis, mebendazole significantly increased the cleavage of PARP and caspase-3 PMC7468578
RPMI-8226 cells 0.5 μM 24 hours Evaluating the effect of mebendazole on μM cell apoptosis, mebendazole significantly increased the cleavage of PARP and caspase-3 PMC7468578
U266 cells 0.5 μM 24 hours Evaluating the effect of mebendazole on μM cell apoptosis, mebendazole had a lesser effect on apoptosis in U266 cells PMC7468578
Mino MCL cells 0-5 μM 24 hours Degrasyn down-regulated constitutive pSTAT3 expression in Mino MCL cells in a dose-and time-dependent manner. PMC5483974
Z-138 BV-MCL cells 1 μM 48 hours The combination of degrasyn and bortezomib significantly inhibited cell growth and induced apoptosis in Z-138 BV-MCL cells. PMC5483974
RAW 264.7 murine macrophages 5 µM 30 minutes To investigate the effect of WP1130 on MNV-1 infection, results showed that WP1130 significantly reduced viral titers. PMC3390402
Bone marrow-derived macrophages (BMDMs) 5 µM 30 minutes To investigate the effect of WP1130 on MNV-1 infection, results showed that WP1130 significantly reduced viral titers. PMC3390402
HG23 cells (Norwalk virus replicon) 5 µM 24 hours To investigate the effect of WP1130 on Norwalk virus replication, results showed that WP1130 significantly inhibited viral replication. PMC3390402

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
nude mice VCaP xenograft model intraperitoneal injection 300 mg/kg Single dose, sacrificed 24 hours post-treatment WP1130 significantly inhibited the growth of VCaP tumors and reduced ERG protein levels PMC3964108
BALB/c nude mice KYSE-150R cell transplantation model Intraperitoneal injection 25 mg·kg−1·d−1 Once daily for 15 days Degrasyn combined with X-ray treatment significantly inhibited tumor growth in KYSE-150R cell-transplanted mice with no detectable toxicity. PMC11699344
Nude mice Human MM cell xenograft model Oral 30 mg/kg 12 hours and 2 hours before Evaluating the effect of mebendazole on MM xenograft tumor growth, mebendazole significantly inhibited tumor growth without toxicity PMC7468578
SCID mice MCL xeno-transplant model intraperitoneally (IP) 20mg/kg Daily for 4 weeks The combination of degrasyn and bortezomib significantly inhibited MCL tumor growth and prolonged survival in SCID mice. PMC5483974
Balb/c mice MNV-1 infection model Oral gavage 50 or 100 mg/kg body weight Once daily for 20 days To investigate the effect of WP1130 on MNV-1 infection in mice, results showed that WP1130 significantly reduced viral titers in the jejunum/duodenum, the most proximal part of the gastrointestinal tract. PMC3390402

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.60mL

0.52mL

0.26mL

13.01mL

2.60mL

1.30mL

26.02mL

5.20mL

2.60mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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