Art. -Nr.: HY-13989

Copy Link Print Information

b-AP15

(Synonyms: NSC 687852)

13 Cited Publications

Kundenbewertung

Based on 13 publication(s) in Google Scholar

b-AP15 is a specific inhibitor of the deubiquitinating enzymes UCHL5 and Usp14.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Reinheit: 98.05%
CAS. Nr.: 1009817-63-3
Formel: C₂₂H₁₇N₃O₆
Molecular Weight:419.39

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years

* The compound is unstable in solutions, freshly prepared is recommended.

b-AP15 Chemical Structure

CAS. Nr.: 1009817-63-3

Größe

Preis

Verfügbarkeit

Menge

Amount: USD 0.00

* Bitte wählen Sie Menge, bevor Sie Artikel hinzufügen.

Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (13)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

b-AP15 is a specific inhibitor of the deubiquitinating enzymes UCHL5 and Usp14.

IC₅₀ & Target

UCHL5/Usp14^[1]

Alle Deubiquitinase Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
CCRF-CEM	IC₅₀	0.26 μM Compound: 2e	Cytotoxicity against CEM T-lymphocytes. Cytotoxicity against CEM T-lymphocytes.	[PMID: 11170648]
CCRF-CEM	IC₅₀	0.26 μM Compound: 2e	Cytotoxicity against human CEM cells Cytotoxicity against human CEM cells	[PMID: 19819135]
CCRF-CEM	IC₅₀	0.28 μM Compound: 417	Antiproliferative activity against human CEM cells assessed as cell growth inhibition Antiproliferative activity against human CEM cells assessed as cell growth inhibition	[PMID: 32172081]
HCT-116	EC₅₀	1.05 μM Compound: b-AP15	Cytotoxicity in human HCT116 cells assessed as reduction in cell viability incubated for 72 hrs by FMCA analysis Cytotoxicity in human HCT116 cells assessed as reduction in cell viability incubated for 72 hrs by FMCA analysis	[PMID: 31682427]
HL-60	CC₅₀	0.13 μM Compound: 2c	Cytotoxicity against human HL60 cells in presence of RPMI1640 containing 10% fetal bovine serum by trypan blue exclusion test Cytotoxicity against human HL60 cells in presence of RPMI1640 containing 10% fetal bovine serum by trypan blue exclusion test	[PMID: 17499885]
HSC-2	CC₅₀	0.094 μM Compound: 2c	Cytotoxicity against human HSC2 by MTT method Cytotoxicity against human HSC2 by MTT method	[PMID: 17499885]
HSC-4	CC₅₀	0.56 μM Compound: 2c	Cytotoxicity against human HSC4 cells by MTT method Cytotoxicity against human HSC4 cells by MTT method	[PMID: 17499885]
L1210	IC₅₀	0.28 μM Compound: 417	Antiproliferative activity against mouse L1210 cells assessed as cell growth inhibition Antiproliferative activity against mouse L1210 cells assessed as cell growth inhibition	[PMID: 32172081]
L1210	IC₅₀	0.42 μM Compound: 2e	Cytotoxicity against murine L1210 cells. Cytotoxicity against murine L1210 cells.	[PMID: 11170648]
L1210	IC₅₀	0.42 μM Compound: 2e	Cytotoxicity against mouse L1210 cells Cytotoxicity against mouse L1210 cells	[PMID: 19819135]
L1210	IC₅₀	2.77 μM Compound: 2e	Inhibitory effect on the biosyntheses of DNA in murine L1210 cells. Inhibitory effect on the biosyntheses of DNA in murine L1210 cells.	[PMID: 11170648]
L1210	IC₅₀	3.21 μM Compound: 2e	Inhibitory effect on the biosyntheses of protein in murine L1210 cells. Inhibitory effect on the biosyntheses of protein in murine L1210 cells.	[PMID: 11170648]
L1210	IC₅₀	5.73 μM Compound: 2e	Inhibitory effect on the biosyntheses of RNA in murine L1210 cells. Inhibitory effect on the biosyntheses of RNA in murine L1210 cells.	[PMID: 11170648]
MOLT-4	IC₅₀	0.15 μM Compound: 2e	Cytotoxicity against human Molt4/C8 cells Cytotoxicity against human Molt4/C8 cells	[PMID: 19819135]
P388	IC₅₀	0.05 μM Compound: 2e	Cytotoxicity against murine P388 cells. Cytotoxicity against murine P388 cells.	[PMID: 11170648]
P388	IC₅₀	0.28 μM Compound: 417	Antiproliferative activity against mouse P388 cells assessed as cell growth inhibition Antiproliferative activity against mouse P388 cells assessed as cell growth inhibition	[PMID: 32172081]

In Vitro

Purified 19S proteasomes (5 nM) are treated with indicated concentrations of b-AP15 and DUB activity is determined by detectionof Ub-AMC cleavage. The IC₅₀ value (2.1±0.411 μM) is determined from log concentration curves in Graph Pad Prism using non linear regression analysis. b-AP15 as a previously unidentified class of proteasome inhibitor that 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 is insensitive to TP53 status and overexpression of the apoptosis inhibitor BCL2^[1]. The ability of b-AP15 is determined to inhibit proteasome deubiquitinase activity using Ub-AMC as the substrate. An IC₅₀ of 16.8±2.8 μM is observed^[2]. b-AP15 is a specific USP14 and UCHL5 inhibitor, which blocks growth and induces apoptosis in MM cells^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

b-AP15 (2.5 mg/kg) inhibits tumor growth in syngenic mice models with less frequent administration schedules. We administered b-AP15 to C57BL/6J mice with Lewis lung carcinomas (LLCs) using a 2-d-on, 2-d-off schedule and to BALB/c mice with orthotopic breast carcinoma (4T1) using a 1-d-on, 3-d-off schedule. b-AP15 significantly inhibited tumor growth in both models, with T/C=0.16 (P≤0.01) for the C57BL/6J mice and T/C=0.25 (P≤0.001) for the BALB/c mice. A reduction in the number of pulmonary metastases also is observed in the group of mice with 4T1 breast carcinomas treated with b-AP15^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS. Nr. 1009817-63-3
Appearance Solid
Molecular Weight 419.39
Formel C₂₂H₁₇N₃O₆
Color Light yellow to yellow
SMILES

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
Synonyms

NSC 687852
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years

* The compound is unstable in solutions, freshly prepared is recommended.

Publications (13)

All WBCell Proliferation/Viability AssayCell Imaging/StainingFlow Cytometry

Sort by:

Journal Impact Factor

Redox Biol

USP20 governs tyrosine kinase inhibitors resistance through ferroptosis evasion by targeting GPX4 in cancers. [Abstract]

2026 May:92:104086. PMID: 41844497

b-AP15 purchased from MedChemExpress. Usage Cited in: Redox Biol. 2026 May:92:104086. [Abstract]

Immunoblot analysis of target proteins in sorafenib-resistant 769-P and A549 cells following 24 h treatment with specific deubiquitinase inhibitors. ML-323: 10 μM, GSK2643943A: 10 μM, XL177A: 10 μM, Spautin-1: 10 μM, IU1: 10 μM, AZ1: 10 μM, MF-094: 10 μM, LDN-57444: 10 μM, TCID: 10 μM, PR-619: 10 μM, BAY11-7082: 10 μM, EOAI3402143: 2.5 μM, ML364: 10 μM, b-AP15: 0.5 μM.
Apoptosis

Deubiquitylatinase inhibitor b-AP15 induces c-Myc-Noxa-mediated apoptosis in esophageal squamous cell carcinoma. [Abstract]

2019 Oct;24(9-10):826-836. PMID: 31342239
EMBO J

USP8 promotes cancer progression and extracellular vesicle-mediated CD8+ T cell exhaustion by deubiquitinating the TGF-β receptor TβRII. [Abstract]

2022 Aug 16;41(16):e108791. PMID: 35811497
Cancer Gene Ther

b-AP15 enhances TRAIL-induced cell death in HNSCC via the induction of ROS/JNK/DR5 signalling. [Abstract]

2026 May 2. PMID: 42069980

b-AP15 purchased from MedChemExpress. Usage Cited in: Cancer Gene Ther. 2026 May 2. [Abstract]

CCK8 cell viability analysis of HNSCC cell lines treated with increasing doses of b-AP15 and/or TRAIL for 48 h. Values below the combination are Combination Indices (CI) as described in the text.

b-AP15 purchased from MedChemExpress. Usage Cited in: Cancer Gene Ther. 2026 May 2. [Abstract]

Colony formation assay of HNSCC cell lines treated with b-AP15 (250 nM) and/or TRAIL (50 ng/mL) for 24 h. Representative images are shown with quantification below.

b-AP15 purchased from MedChemExpress. Usage Cited in: Cancer Gene Ther. 2026 May 2. [Abstract]

Annexin V analysis of HNSCC cell lines after treated with b-AP15 (250 nM) and/or TRAIL (50 ng/mL) for 24 and 48 h.

b-AP15 purchased from MedChemExpress. Usage Cited in: Cancer Gene Ther. 2026 May 2. [Abstract]

Representative western blot of the expression of DR4/TRAILR1 and DR5/TRAILR2 in HNSCC cell lines treated with increasing doses of b-AP15 for 24 h. GAPDH was used as a loading control.

b-AP15 purchased from MedChemExpress. Usage Cited in: Cancer Gene Ther. 2026 May 2. [Abstract]

Flow cytometry analysis of DR4/TRAILR1 and DR5/TRAILR2 expression in HNSCC cell lines treated with increasing doses of b-AP15 for 24 h.

b-AP15 purchased from MedChemExpress. Usage Cited in: Cancer Gene Ther. 2026 May 2. [Abstract]

Flow cytometry analysis ROS in HNSCC cell lines treated with increasing doses of b-AP15 (0-1000 nM) for 24 h. The fluorescent probe DCFH-DA was added to cells for the detection of ROS.
Eur J Pharmacol

Doxorubicin-mediated retardation of aggresome formation enhances Carfilzomib-induced cell death synergistically by augmenting ER stress and proapoptotic signaling. [Abstract]

2025 Dec 5:1008:178303. PMID: 41183585
Sci Rep

Enhancing proteasome activity by NMDAR antagonists explains their therapeutic effect in neurodegenerative and mental diseases. [Abstract]

2025 Jan 13;15(1):1165. PMID: 39805913
FASEB J

Cullin 2-RBX1 E3 ligase and USP2 regulate antithrombin ubiquitination and stability. [Abstract]

2021 Aug;35(8):e21800. PMID: 34324733
PLoS Negl Trop Dis

Identification of anti-flaviviral drugs with mosquitocidal and anti-Zika virus activity in Aedes aegypti. [Abstract]

2019 Aug 20;13(8):e0007681. PMID: 31430351
Chem Asian J

Selective Protein Degradation through Tetrazine Ligation of Genetically Incorporated Unnatural Amino Acids. [Abstract]

2024 Sep 2:e202400824. PMID: 39221720
Biochem Biophys Res Commun

The CDK4/6-UCHL5-BRD4 axis confers resistance to BET inhibitors in MLL-rearranged leukemia cells by suppressing BRD4 protein degradation. [Abstract]

2022 Jan 15:588:147-153. PMID: 34954522
Cell Physiol Biochem

The Deubiquitinating Enzyme USP14 Regulates Leukemic Chemotherapy Drugs-Induced Cell Apoptosis by Suppressing Ubiquitination of Aurora Kinase B. [Abstract]

2017;42(3):965-973. PMID: 28662510
bioRxiv

2025 May 14.
bioRxiv

2024 August 21.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 20 mg/mL (47.69 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.3844 mL

11.9221 mL

23.8442 mL

5 mM

0.4769 mL

2.3844 mL

4.7688 mL

10 mM

0.2384 mL

1.1922 mL

2.3844 mL

Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: 2.08 mg/mL (4.96 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protokoll

Kinase Assay^[1]

For deubiquitinase inhibition assays, 19S regulatory particle (5 nM), 26S (5 nM) UCH-L1 (5 nM), UCH-L3 (0.3 nM), USP2_CD (5 nM) USP7_CD (5 nM) USP8_CD (5 nM) or BAP1 (5 nM) is incubated with DMSO or b-AP15 and monitored the cleavage of ubiquitin-AMC (1,000 nM) using a Wallac VICTOR Multilabel counter or a Tecan Infinite M1000 equipped with 380 nm excitation and 460 nm emission filters^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay^[2]

Cell viability is monitored by either the fluorometric microculture cytotoxicity assay or the MTT assay. For the MTT assay, cells are seeded into 96-well flat-bottomed plates overnight and exposed to drugs, using DMSO as the control. At the end of incubations, 10 µl of a stock solution of 5 mg/mL MTT is added into each well, and the plates are incubated 4 hours at 37°C. Formazan crystals are dissolved with 100 µL 10% SDS/10 mM HCl solution overnight at 37°C. Absorbance is measured using an enzyme-linked immunosorbent assay (ELISA) plate reader at 590 nm^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration^[1]

Mice^[1]
For the squamous carcinoma model, 1×10⁶ FaDu cells are subcutaneously injected into the right rear flank of female SCID mice. Tumor growth is measured by the formula length×width²×0.44. When tumors have grown to a size of approximately 200 mm³ (defined as day 0), mice are randomized to receive either vehicle (n=10) or b-AP15 (n=15) at 5 mg per kg of body weight by daily subcutaneous injection. For the colon carcinoma model, we subcutaneously injected 2.5×10⁶ HCT-116 colon carcinoma cells overexpressing Bcl2 into the right flank of female nude mice. We treated mice with 5 mg of b-AP15 per kg of body weight by intraperitoneal injection. For the lung carcinoma model, we subcutaneously injected 2×10⁵ LLC cells into the right rear flank of female C57/B6 mice. When tumors had grown to a size of approximately 50 mm³ (defined as day 0), we randomized mice to receive either vehicle (n=4) or b-AP15 (n=4) at 5 mg per kg of body weight intraperitoneally, with a treatment cycle consisting of 2 d of treatment followed by 2 d of rest (2 d on, 2 d off) for 2 weeks.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (281 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. D'Arcy P, et al. Inhibition of proteasome deubiquitinating activity as a new cancer therapy. Nat Med. 2011 Nov 6;17(12):1636-40. [Content Brief]

[2]. Wang X, et al. The 19S Deubiquitinase Inhibitor b-AP15 is Enriched in Cells and Elicits Rapid Commitment to Cell Death. Mol Pharmacol. 2014 Jun;85(6):932-45. [Content Brief]

[3]. Tian Z, et al. 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. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.3844 mL	11.9221 mL	23.8442 mL	59.6104 mL
	5 mM	0.4769 mL	2.3844 mL	4.7688 mL	11.9221 mL
	10 mM	0.2384 mL	1.1922 mL	2.3844 mL	5.9610 mL
	15 mM	0.1590 mL	0.7948 mL	1.5896 mL	3.9740 mL
	20 mM	0.1192 mL	0.5961 mL	1.1922 mL	2.9805 mL
	25 mM	0.0954 mL	0.4769 mL	0.9538 mL	2.3844 mL
	30 mM	0.0795 mL	0.3974 mL	0.7948 mL	1.9870 mL
	40 mM	0.0596 mL	0.2981 mL	0.5961 mL	1.4903 mL

Keywords

b-AP15

13 Cited Publications

100 mg Angebot einholen

Subscribe to the

MedChemExpress

Newsletter

Produktname:
Art. -Nr.:
Menge:
MCE Japan Authorized Agent:

Produktname:
CAS. Nr.:
Species:
Reinheit:
Menge:

b-AP15

Peptidomimetic Library

Publications Citing Use of MedChemExpress (MCE) b-AP15

Alle Deubiquitinase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (13)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

b-AP15

Peptidomimetic Library

Publications Citing Use of MedChemExpress (MCE) b-AP15

Alle Deubiquitinase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (13)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

b-AP15 Related Classifications

HY-13989 Related Classifications