WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 406452
CAS#: 1009817-63-3
Description: b-AP15 is a novel inhibitor of proteasome deubiquitination. b-AP15 displays antitumor activity in several preclinical, solid tumor models. b-AP15 triggers time- and dose-dependent apoptosis of the human multiple myeloma (MM) cell lines RPMI8226 and U266, as determined by phosphatidylserine exposure. 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. b-AP15 may have potential for treatment of multiple myeloma patients.
MedKoo Cat#: 406452
Name: b-AP15
CAS#: 1009817-63-3
Chemical Formula: C22H17N3O6
Exact Mass: 419.11174
Molecular Weight: 419.39
Elemental Analysis: C, 63.01; H, 4.09; N, 10.02; O, 22.89
b-AP15, purity > 98%, is in stock. The same day shipping out after order is received.
Synonym: b-AP15; b-AP15; b-AP-15; USP14 Inhibitor III; UCHL5UCH37 Inhibitor II; NSC687852.
IUPAC/Chemical Name: (3E,5E)-1-acryloyl-3,5-bis(4-nitrobenzylidene)piperidin-4-one.
InChi Key: GFARQYQBWJLZMW-JYFOCSDGSA-N
InChi Code: 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+
SMILES Code: 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
The following data is based on the product molecular weight 419.39 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
1: Tian Z, D'Arcy P, Wang X, Ray A, Tai YT, Hu Y, Carrasco RD, Richardson P, Linder S, Chauhan D, Anderson KC. A novel small molecule inhibitor of deubiquitylating enzyme USP14 and UCHL5 induces apoptosis in multiple myeloma and overcomes bortezomib resistance. Blood. 2014 Jan 30;123(5):706-16. doi: 10.1182/blood-2013-05-500033. Epub 2013 Dec 6. PubMed PMID: 24319254.
2: Feng X, Holmlund T, Zheng C, Fadeel B. Proapoptotic effects of the novel proteasome inhibitor b-AP15 on multiple myeloma cells and natural killer cells. Exp Hematol. 2013 Nov 27. pii: S0301-472X(13)00871-0. doi: 10.1016/j.exphem.2013.11.010. [Epub ahead of print] PubMed PMID: 24291587.
3: Brnjic S, Mazurkiewicz M, Fryknäs M, Sun C, Zhang X, Larsson R, D'Arcy P, Linder S. Induction of Tumor Cell Apoptosis by a Proteasome Deubiquitinase Inhibitor Is Associated with Oxidative Stress. Antioxid Redox Signal. 2013 Oct 17. [Epub ahead of print] PubMed PMID: 24011031.
4: Sarhan D, Wennerberg E, D'Arcy P, Gurajada D, Linder S, Lundqvist A. A novel inhibitor of proteasome deubiquitinating activity renders tumor cells sensitive to TRAIL-mediated apoptosis by natural killer cells and T cells. Cancer Immunol Immunother. 2013 Aug;62(8):1359-68. doi: 10.1007/s00262-013-1439-1. Epub 2013 May 21. PubMed PMID: 23689729.
5: D'Arcy P, Linder S. Proteasome deubiquitinases as novel targets for cancer therapy. Int J Biochem Cell Biol. 2012 Nov;44(11):1729-38. doi: 10.1016/j.biocel.2012.07.011. Epub 2012 Jul 20. Review. PubMed PMID: 22819849.
6: D'Arcy P, Brnjic S, Olofsson MH, Fryknäs M, Lindsten K, De Cesare M, Perego P, Sadeghi B, Hassan M, Larsson R, Linder S. Inhibition of proteasome deubiquitinating activity as a new cancer therapy. Nat Med. 2011 Nov 6;17(12):1636-40. doi: 10.1038/nm.2536. PubMed PMID: 22057347.
