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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 |
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| P005091
P005091 (P5091) is a potent and selective inhibitor of ubiquitin-specific protease (USP) 7 with IC50 of 4.2 μM. |
| P22077
P22077 is a selective inhibitor of ubiquitin-specific protease (USP) 7 with EC50 of 8.6 μM. P 22077 also inhibits USP47 with an EC50 of 8.74 μM. |
| PR-619
PR-619 is a broad-spectrum reversible DUB (deubiquitinating enzyme) inhibitor of USP2, USP4, USP5, USP7 and USP8 with an EC50 of 3-9 μM. PR-619 also induces endoplasmic reticulum stress and endoplasmic reticulum stress-associated apoptosis. |
| LDN-57444
LDN-57444 is a reversible, competitive proteasome inhibitor for Uch-L1 with IC50 of 0.88 μM, 28-fold selectivity over isoform Uch-L3. |
| TCID
TCID is a DUB inhibitor for ubiquitin C-terminal hydrolase L3 with IC50 of 0.6 μM, 125-fold selective to L1. |
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