| SKU | Size | Availability | Price | Qty |
|---|---|---|---|---|
| N420305-1ml | 1ml | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $181.90 |
Inhibitor of UCHL5 and USP14
| Synonyms | b-AP15|1009817-63-3|(3E,5E)-1-Acryloyl-3,5-bis(4-nitrobenzylidene)piperidin-4-one|NSC687852|NSC 687852|4-Piperidinone, 3,5-bis[(4-nitrophenyl)methylene]-1-(1-oxo-2-propen-1-yl)-, (3E,5E)-|NSC-687852|(3E,5E)-3,5-bis[(4-nitrophenyl)methylidene]-1-(prop-2-en |
|---|---|
| Specifications & Purity | 10mM in DMSO |
| Storage Temp | Store at -80°C |
| Shipped In | Dry ice |
| Product Description | A cell-permeable bis-nitrobenzylidene-piperidinone that inhibits 19S deubiquitinase (DUB) activity (IC50 = 2.1 µM against Ub-AMC hydrolysis) in a reversible manner by directly targeting UCH37/UCH-L5 and USP14, while exhibiting little or no activity toward BAP1, UCH-L1, UCH-L3, USP2, USP7, USP8 (IC50 >100 µM), or POH1/PRN11. Dual UCH37 and USP14 inhibition by a-AP15 results in increased bulk cellular protein ubiquitination level and a blockage of protein proteasomal degradation (Effective conc. ≥770 nM in HCT-116 cells), exactly opposite to the effects seen with USP14 inhibition alone by IU1 (Cat. No. 662210). Effectively suppresses the growth of various tumors in mice (2.5 to 5 mg/kg, i.p. or s.c.) in vivo. |
| IUPAC Name | (3E,5E)-3,5-bis[(4-nitrophenyl)methylidene]-1-prop-2-enoylpiperidin-4-one |
|---|---|
| INCHI | InChI=1S/C22H17N3O6/c1-2-21(26)23-13-17(11-15-3-7-19(8-4-15)24(28)29)22(27)18(14-23)12-16-5-9-20(10-6-16)25(30)31/h2-12H,1,13-14H2/b17-11+,18-12+ |
| InChi Key | GFARQYQBWJLZMW-JYFOCSDGSA-N |
| Canonical SMILES | C=CC(=O)N1CC(=CC2=CC=C(C=C2)[N+](=O)[O-])C(=O)C(=CC3=CC=C(C=C3)[N+](=O)[O-])C1 |
| Isomeric SMILES | C=CC(=O)N1C/C(=C\C2=CC=C(C=C2)[N+](=O)[O-])/C(=O)/C(=C/C3=CC=C(C=C3)[N+](=O)[O-])/C1 |
| PubChem CID | 5351435 |
| Molecular Weight | 419.39 |
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| Pictogram(s) | GHS07 |
|---|---|
| Signal | Warning |
| Hazard Statements | H302:Harmful if swallowed |
| Precautionary Statements | P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses if present and easy to do - continue rinsing. P280:Wear protective gloves/protective clothing/eye protection/face protection. |
