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B-AP15

Catalog No. T1932 CAS 1009817-63-3

Synonyms: NSC 687852

B-AP15 (NSC-687852)(NSC-687852) is a selective inhibitor of the deubiquitinating enzymes Usp14 and UCHL5 of the 26S proteasome. It blocks the deubiquitinating activity of the 26S proteasome.

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B-AP15, CAS 1009817-63-3

Pack Size	Availability	Price/USD
5 mg	In stock	$ 32.00
10 mg	In stock	$ 52.00
25 mg	In stock	$ 89.00
50 mg	In stock	$ 133.00
100 mg	In stock	$ 225.00
200 mg	In stock	$ 397.00
500 mg	In stock	$ 676.00
1 mL * 10 mM (in DMSO)	In stock	$ 44.00

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Purity: 98%

Purity: 95.25%

Purity: 95.07%

Purity: 91.43%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	B-AP15 (NSC-687852)(NSC-687852) is a selective inhibitor of the deubiquitinating enzymes Usp14 and UCHL5 of the 26S proteasome. It blocks the deubiquitinating activity of the 26S proteasome.
Targets&IC50	UCHL5:2.1 μM
In vitro	In mice with HCT-116 colon carcinoma xenografts, B-AP15 (5 mg/kg) significantly delayed tumor onset. Additionally, in severely immunodeficient mice bearing squamous cell carcinoma xenografts, B-AP15 (5 mg/kg) demonstrated notable antitumor activity.
In vivo	As a UPS (Ubiquitin-Proteasome System) inhibitor, B-AP15 induces cell death by triggering the cathepsin-D-dependent lysosomal apoptotic pathway. Compared to peripheral blood mononuclear cells or immortalized epithelial cells (hTERT-RPE1), B-AP15 exhibits greater cytotoxicity towards HCT-116 cells. It dose-dependently accumulates the UbG76V-YFP receptor (IC50: 0.8 μM), indicating impaired proteasomal degradation. When applied to human colon cancer HCT-116 cells, B-AP15 (1 μM) rapidly accumulates polyubiquitinated proteins. At a concentration of 1 μM, B-AP15 inhibits the release of IL-1β induced by ATP from lipopolysaccharide-induced peritoneal macrophages. In THP-1 cells, 1 μM B-AP15 reduces the level of cell death induced by nigericin and significantly decreases the formation of ASC specks in lipopolysaccharide-induced THP-1 cells treated with nigericin. Additionally, B-AP15 (1 μM) causes a G2/M phase cell cycle arrest and accumulation of cell cycle inhibitors in HCT-116 cells. At 2.2 μM, B-AP15 dose-dependently increases the levels of the cyclin-dependent kinase inhibitors CDKN1A and CDKN1B, and the tumor suppressor gene TP53, without affecting the levels of ornithine decarboxylase 1.
Kinase Assay	For deubiquitinase inhibition assays, 19S regulatory particle (5 nM), 26S (5 nM) UCH-L1 (5 nM), UCH-L3 (0.3 nM), USP2CD (5 nM) USP7CD (5 nM) USP8CD (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].
Cell Research	b-AP15 is dissolved in DMSO and stored, and then diluted with appropriate medium before use[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].

Synonyms	NSC 687852
Molecular Weight	419.39
Formula	C22H17N3O6
CAS No.	1009817-63-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 41.9 mg/mL (100 mM)

References and Literature

1. D'Arcy P, et al. Nat Med. 2011, 17(12):1636-40. 2. D'Arcy P, et al. Int J Biochem Cell Biol. 2012, 44(11):1729-38. 3. Lopez-Castejon G, et al. J Biol Chem, 2013, 288(4), 2721-2733.

Citations

1. Wu W, Xu H, Liao C, et al. Blockade of USP14 potentiates type I interferon signaling and radiation-induced antitumor immunity via preventing IRF3 deubiquitination. Cellular Oncology. 2022: 1-15 2. Yue X, Liu T, Wang X, et al.Pharmacological inhibition of BAP1 recruits HERC2 to competitively dissociate BRCA1–BARD1, suppresses DNA repair and sensitizes CRC to radiotherapy.Acta Pharmaceutica Sinica B.2023

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Bioactive Compound Library HIF-1 Signaling Pathway Compound Library Apoptosis Compound Library Cell Cycle Compound Library Covalent Inhibitor Library Ubiquitination Compound Library Anti-Aging Compound Library Anti-Cancer Compound Library Cysteine Covalent Library

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Keywords

B-AP15 1009817-63-3 Apoptosis Cell Cycle/Checkpoint DNA Damage/DNA Repair Ubiquitination DUB Deubiquitinase Inhibitor BAP15 inhibit NSC-687852 DUBs B AP15 NSC 687852 b-AP15 B-AP-15 NSC687852 inhibitor

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