Products for Research Use Only
RegisterLogin

B-AP15

CAT: 0013-GTR19164089-01Size: 1 gDry Ice: NoHazardous: No
Product image 1
1 / 1
CAT#:0013-GTR19164089-01Size:1 g
Selected
24/48H Stock Items & 2 to 6 Weeks non Stock Items.
Quick Request Actions
Description
B-AP15 (NSC687852) is a specific inhibitor of the deubiquitinating enzymes UCHL5 and Usp14 of the 26S proteasome. It blocks the deubiquitinating activity of the 26S proteasome. (In Vitro) :Purified 19S proteasomes (5 nM) are treated with indicated concentrations of b-AP15 and DUB activity is determined by detectionof Ub-AMC cleavage. The IC50 value (2.1±0.411 μM) is determined from log concentration curves in Graph Pad Prism using non linear regression analysis. b-AP15 as a previously unidentified class of proteasome inhibitor that abrogates the deubiquitinating activity of the 19S regulatory particle. 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 ability of b-AP15 is determined to inhibit proteasome deubiquitinase activity using Ub-AMC as the substrate. An IC50 of 16.8±2.8 μM is observed. b-AP15 is a specific USP14 and UCHL5 inhibitor, which blocks growth and induces apoptosis in MM cells. (In Vivo) :b-AP15 (2.5 mg/kg) inhibits tumor growth in syngenic mice models with less frequent administration schedules. We administered b-AP15 to C57BL/6J mice with Lewis lung carcinomas (LLCs) using a 2-d-on, 2-d-off schedule and to BALB/c mice with orthotopic breast carcinoma (4T1) using a 1-d-on, 3-d-off schedule. b-AP15 significantly inhibited tumor growth in both models, with T/C=0.16 (P≤0.01) for the C57BL/6J mice and T/C=0.25 (P≤0.001) for the BALB/c mice. A reduction in the number of pulmonary metastases also is observed in the group of mice with 4T1 breast carcinomas treated with b-AP15.
CAS Number
1009817-63-3
Product Name Alternative
B-AP15 | USP14 Inhibitor III | UCHL5UCH37 Inhibitor II | NSC687852.
Purity
>98% (HPLC)
Solubility
DMSO: 48 mg/mL warmed (114.45 mM)
Smiles
O=C1/C (CN (C (C=C) =O) C/C1=C\C2=CC=C ([N+] ([O-]) =O) C=C2) =C/C3=CC=C ([N+] ([O-]) =O) C=C3
Molecular Formula
C22H17N3O6
Molecular Weight
419.39
Storage Conditions
Storage temperature: -20°C. Stability: ≥ 2 years
Notes
For research use only.
Other Product Names
(3E,5E) -1-acryloyl-3,5-bis (4-nitrobenzylidene) piperidin-4-one.

Related Products

CatalogName
GTR19319500Influenza B (B/Malaysia)
GTR19009424Asialog. GM2, B.b.
GTR19009421Asialog. GM1, B.b.
GTR19009419Monosialog. GM1, B.b.
GTR19009408Disialog. GD1b, B.b.
GTR19009429Trisialog. GT1b, B.b.
GTR19009427Trisialog. GT1a, B.b.
GTR19009413Monosialog. GM4, B.b.
GTR19009404Disialog. GD3, B.b.
GTR19009426Tetrasialog. GQ1b, B.b.

Alternative Products

CatalogName
406452b-AP15
MBS130804-01b-AP15(NSC687852)
27701-1B-AP15 (NSC-687852)
A4453-5.1NSC 687852 (b-AP15)
SG0020-5mgB-AP15 (DUB inhibitor)

Popular Products