b-AP15
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    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.


Price and Availability

Size
Price

10mg
USD 150
100mg
USD 450
1g
USD 1250
Size
Price

25mg
USD 250
200mg
USD 550
2g
USD 1950
Size
Price

50mg
USD 350
500mg
USD 750
5g
USD 3650

b-AP15, purity > 98%, is in stock. The same day shipping out after order is received. Note: the estimated shipping out time for order > 2g may be 2 weeks.


Chemical Structure

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Theoretical Analysis

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


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


Technical Data

Appearance:
Yellow solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Certificate of Analysis:

Safety Data Sheet (MSDS):

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO, not in water

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Harmonized System Code:
293490


Additional Information

  
 
 
 


References

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.