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b-AP15 CAS: 1009817-63-3

Category: Inhibitors
Product Name: b-AP15
Cat No: I000111
CAS No: 1009817-63-3
Synonyms: (3E,5E)-3,5-bis[(4-nitrophenyl)methylidene]-1-prop-2-enoylpiperidin-4-one
Molecular Formula: C22H17N3O6
Molecular Weight: 419.4
SMILES: O=C(C=C)N(C/C(C/1=O)=C\C2=CC=C([N+]([O-])=O)C=C2)CC1=C/C3=CC=C([N+]([O-])=O)C=C3
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+
InChIKey: GFARQYQBWJLZMW-JYFOCSDGSA-N
Solubility: DMSO: ≥ 44 mg/mL
Target: Apoptosis Inducers
Storage: Store at 4°C
CAS 1009817-63-3,b-AP15
  • 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.
IC50 value:
Target: UCHL5/Usp14
in vitro: b-AP15 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 was insensitive to TP53 status and overexpression of the apoptosis inhibitor BCL2 [1]. b-AP15 triggers time- and dose-dependent apoptosis of the human multiple myeloma (MM) cell lines RPMI8226 and U266, as determined by phosphatidylserine exposure. Apoptosis was dependent on caspase activation and was partially dependent on cathepsin D. Furthermore, b-AP15 triggered processing of pro-caspase-3 and cleavage of poly (ADP-ribose) polymerase in MM cells. b-AP15 also induced caspase-independent apoptosis in primary human natural killer cells [2]. in addition to inhibition of deubiquitinases, b-AP15 inhibits the selenoprotein thioredoxin reductase (TrxR) [3].
in vivo: Treatment with b-AP15 inhibited tumor progression in four different in vivo solid tumor models and inhibited organ infiltration in an acute myeloid leukemia model [1]. b-AP15 is well tolerated, inhibits tumor growth, and prolongs survival. Combining b-AP15 with suberoylanilide hydroxamic acid, lenalidomide, or dexamethasone induces synergistic anti-MM activity in distinct human MM xenograft models [4].

  • Spec

Appearance:Yellow solid powder
Purity: > 98%

  • References


1:Synthesis and evaluation of derivatives of the proteasome deubiquitinase inhibitor b-AP15. Wang X, D'Arcy P, Caulfield TR, Paulus A, Chitta K, Mohanty C, Gullbo J, Chanan-Khan A, Linder S.Chem Biol Drug Des. 2015 Nov;86(5):1036-48. doi: 10.1111/cbdd.12571. Epub 2015 May 27. PMID: 25854145 Free PMC Article
2:Inhibitory effect of b-AP15 on the 20S proteasome. Huang L, Jung K, Chen CH.Biomolecules. 2014 Oct 14;4(4):931-9. doi: 10.3390/biom4040931. PMID: 25317846 Free PMC Article
3:The 19S Deubiquitinase inhibitor b-AP15 is enriched in cells and elicits rapid commitment to cell death. Wang X, Stafford W, Mazurkiewicz M, Fryknäs M, Brjnic S, Zhang X, Gullbo J, Larsson R, Arnér ES, D'Arcy P, Linder S.Mol Pharmacol. 2014 Jun;85(6):932-45. doi: 10.1124/mol.113.091322. Epub 2014 Apr 8. PMID: 24714215 Free Article
4:Proapoptotic effects of the novel proteasome inhibitor b-AP15 on multiple myeloma cells and natural killer cells. Feng X, Holmlund T, Zheng C, Fadeel B.Exp Hematol. 2014 Mar;42(3):172-82. doi: 10.1016/j.exphem.2013.11.010. Epub 2013 Nov 27. PMID: 24291587


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