Home Ubiquitin DUB inhibitor b-AP15 For research use only.

b-AP15

Synonyms: NSC687852

b-AP15 (NSC687852) is a deubiquitinases inhibitor for 19S proteasomes activity of Ub-AMC cleavage with IC50 of 2.1 μM.

b-AP15 Chemical Structure

b-AP15 Chemical Structure

CAS: 1009817-63-3

Selleck's b-AP15 has been cited by 19 Publications

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Purity & Quality Control

Batch: Purity: 99.01%
99.01

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Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
P388 cells Cytotoxicity assay Cytotoxicity against murine P388 cells, IC50=0.05 μM 11170648
human HSC2 Cytotoxicity assay Cytotoxicity against human HSC2 by MTT method, CC50=0.094 μM 17499885
HL60 cells Cytotoxicity assay Cytotoxicity against human HL60 cells in presence of RPMI1640 containing 10% fetal bovine serum by trypan blue exclusion test, CC50=0.13 μM 17499885
Molt 4/C8 cells Cytotoxicity assay Cytotoxicity against human Molt 4/C8 cells, IC50=0.15 μM 11170648
CEM cells Cytotoxicity assay Cytotoxicity against human CEM cells, IC50=0.26 μM 19819135
L1210 cells Cytotoxicity assay Cytotoxicity against murine L1210 cells, IC50=0.42 μM 11170648
HSC4 cells Cytotoxicity assay Cytotoxicity against human HSC4 cells by MTT method, CC50=0.56 μM 17499885
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Biological Activity

Description b-AP15 (NSC687852) is a deubiquitinases inhibitor for 19S proteasomes activity of Ub-AMC cleavage with IC50 of 2.1 μM.
Features Not a general deubiquitinase inhibitor. Has minimal inhibition on recombinant and cytosolic nonproteasomal cysteine deubiquitinases.
Targets
USP14 [1] UCHL5 [1]
2.1 μM
In vitro
In vitro b-AP15 inhibits 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 results in a dose-dependent accumulation of the UbG76V-YFP reporter with IC50 of 0.8 μM, indicating impaired proteasome degradation. b-AP15 (1 μM) results in rapid accumulation of polyubiquitinated proteins in human colon carcinoma HCT-116 cells. b-AP15 (2.2 μM) increases the amounts of the cyclin-dependent kinases CDKN1A and CDKNIB and the tumor suppressor TP53 in a dose-dependent manner without altering the amounts of ornithine decarboxylase 1 (ODC1) in HCT-116 cells. b-AP15 (1 μM) results in G2/M phase cell-cycle arrest in HCT-116 cells, consistent with the accumulation of cell-cycle inhibitors. b-AP15 treatment increases the number of hypodiploid cells and is associated with increased amounts of apoptotic markers, including activated caspase-3, caspase-cleaved poly-ADP ribose polymerase (PARP) and cytokeratin-18 (CK18). b-AP15 is more toxic to HCT-116 cells as compared to immortalized epithelial cells (hTERT-RPE1) or peripheral blood mononuclear cells. b-AP15 inhibits deubiquitinating activity using a variety of substrates, including Ub-AMC, Ub-GFP22, ubiquitinated p53-binding protein homolog (HDM2), and K48- and K63-linked ubiquitin tetramer chains. [1] b-AP15 is an inhibitor of the UPS that induced cell death via induction of the lysosomal apoptosis pathway in a cathepsin-D dependent manner. b-AP15 elicits characteristic UPS defects including the accumulation of ubiquitin conjugates and cell cycle inhibitors such as p21, p27 and the tumor suppressor p53. b-AP15 inhibits the deubiquitinase activity of both cysteine DUBs, with USP14 being slightly more sensitive than UCHL5. b-AP15 induces apoptosis in cells over-expressing the anti-apoptotic Bcl-2 protein and in cells lacking the p53 gene. [2] b-AP15 (1 μM) inhibits ATP-induced IL-1β release from LPS-primed peritoneal macrophages. b-AP15 (1 μM) reduces the levels of cell death induced by nigericin treatment in THP-1 cells. b-AP15 (1 μM) significantly reduces the numbers of ASC specks formed after nigericin treatment in LPS-primed THP-1 cells. [3]
In Vivo
In vivo b-AP15 (5 mg/kg) shows significant antitumor activity in severe combined immunodeficiency (SCID) mice with FaDu squamous carcinoma xenografts. b-AP15 (5 mg/kg) significantly delays tumor onset in mice with HCT-116 colon carcinoma xenografts. [1]
Animal Research Animal Models mice with HCT-116 colon carcinoma xenografts
Dosages 5 mg/kg
Administration intraperitoneal injection

Chemical lnformation & Solubility

Molecular Weight 419.39 Formula

C22H17N3O6
CAS No. 1009817-63-3 SDF Download b-AP15 SDF
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
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 48 mg/mL ( (114.45 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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