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b-AP15 is a deubiquitinases inhibitor for 19S proteasomes activity of Ub-AMC cleavage with IC50 of 2.1 μM. b-AP15 inhibited the activity of two 19S regulatory-particle-associated deubiquitinases, ubiquitin C-terminal hydrolase 5 (UCHL5) and ubiquitin-specific peptidase 14 (USP14), resulting in accumulation of polyubiquitin. b-AP15 induced tumor cell apoptosis that is insensitive to TP53 status and overexpression of the apoptosis inhibitor BCL2.
*The compound is unstable in solutions, freshly prepared is recommended
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Source | Eur J Pharmacol (2018). Figure 1. b-AP15 |
| Method | MTT assay | |
| Cell Lines | HepG2 cells and Hep3B cells | |
| Concentrations | 1.0 μM | |
| Incubation Time | 12, 24, and 48 h | |
| Results | Compared with DMSO control, b-AP15 administration significantly reduced cell viability in dose- and time-dependent manners |
| Molecular Weight | 419.39 |
| Formula | C22H17N3O6 |
| CAS Number | 1009817-63-3 |
| Solubility (25°C) | DMSO 20 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Deubiquitinase Products |
|---|
| CMPD-39
CMPD-39 is a selective USP30 inhibitor with an IC50 of 0.02 μM. CMPD-39 increases protein ubiquitination and accelerates mitophagy. |
| FT709
FT709 is a potent and selective USP9X inhibitor, an IC50 of 82 nM. |
| XL177A
XL177A is a highly potent and selective irreversible USP7 inhibitor with an IC50 of 0.34 nM. |
| LDN-91946
LDN-91946 is a potent, selective and uncompetitive ubiquitin C-terminal hydrolase-L1 (UCH-L1) inhibitor with a Ki app of 2.8 μM. |
| USP5-IN-1
USP5-IN-1, a potent deubiquitinase USP5 inhibitor, binds to the USP5 ZnF-UBD with a KD of 2.8 μM. |
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