Description
| Molecular Weight: | 419.39 |
| Formula: | C22H17N3O6 |
| Purity: | ≥98% |
| CAS#: | 1009817-63-3 |
| Solubility: | DMSO up to 100 mM |
| Chemical Name: | (3E,5E)-1-acryloyl-3,5-bis(4-nitrobenzylidene)piperidin-4-one |
| Storage: | Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year. |
Biological Activity:
b-AP15 (NSC686852) is a potent and selective deubiquitinases inhibitor for 19S proteasomes activity of Ub-AMC cleavage with IC50 of 2.1 μM. It inhibits the activity of two 19S regulatory-particle-associated deubiquitinases, UCHL5 and USP14, resulting in accumulation of polyubiquitin. It has minimal inhibition of UCHL-1, UCHL-3, USP2, USP7, USP, BAP1 and proteasome activity. b-AP15 induces apoptosis by cathepsin D-dependent caspase-cleavage (IC50 ~0.5 μM) and displays antitumor activity in vivo.
How to Use:
In vitro: b-AP15 was used at 10 µM final concentration in various in vitro assays.
In vivo: b-AP15 was dosed to mice with HCT-116 colon carcinoma xenografts by intraperitoneal injection at 5 mg/Kg. formulation is Cremophor EL and polyethylene glycol 400 (1:1).
Reference:
- 1. Berndtsson M, et al. Induction of the lysosomal apoptosis pathway by inhibitors of the ubiquitin-proteasome system. (2009) Int J Cancer. 124(6):1463-9.
- 2. D'Arcy P, et al. Inhibition of proteasome deubiquitinating activity as a new cancer therapy. (2011) Nat Med. 17(12):1636-40.
Products are for research use only. Not for human use.
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