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DBEQ

Catalog No. T1969 CAS 177355-84-9

Synonyms: JRF 12

DBEQ (JRF 12) is a selective, potent, reversible, and ATP-competitive p97 inhibitor.

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DBEQ, CAS 177355-84-9

Pack Size	Availability	Price/USD
5 mg	In stock	$ 53.00
10 mg	In stock	$ 96.00
25 mg	In stock	$ 190.00
50 mg	In stock	$ 342.00
100 mg	In stock	$ 432.00
200 mg	In stock	$ 639.00
500 mg	In stock	$ 987.00
1 mL * 10 mM (in DMSO)	In stock	$ 54.00

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Purity: 99.94%

Purity: 99.16%

Purity: 98.89%

Purity: 98.16%

Purity: 98%

Biological Description

Chemical Properties

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Description	DBEQ (JRF 12) is a selective, potent, reversible, and ATP-competitive p97 inhibitor.
Targets&IC50	p97:1.5 μM
In vivo	At a concentration of 10 μM, DBeQ effectively inhibits the degradation of viruses and antibodies, without affecting the degradation of IgG Fc. It rapidly facilitates the activation of caspases-3 and -7 in HeLa cells, demonstrating a more potent activation of the intrinsic caspase-9 apoptosis pathway compared to the extrinsic caspase-8 pathway, while Staurosporine (STS) similarly activates both pathways. Additionally, 10 μM DBeQ blocks the degradation of TCRα-GFP in HEK293 cells. In HEK293 cells, DBeQ dose-dependently induces CHOP within 3 hours without increasing p21 levels. It diminishes the phosphorylation of basal and nutrient-stimulated mTOR targets in U2OS cells, similar to the effects of Rapamycin. At 15 μM, DBeQ induces a significant accumulation of LC3-II in the nuclei, membrane concentrations, and cytoplasm of HeLa cells. Furthermore, DBeQ inhibits the degradation of UbG76V-GFP, ODD-Luc, and Luc-ODC in HeLa cells, with IC50 values of 2.6 μM, 56 μM, and 45 μM, respectively.
Kinase Assay	Manual ATPase Assay: Assay Buffer [20 μL of 2.5× concentration, where 1× = 50 mM Tris (pH 7.4), 20 mM MgCl2, 1 mM EDTA, and 0.5 mM tris(2-carboxyethyl)phosphine (TCEP)] is dispensed into each well of a 96-well plate. Puri?ed p97 (25 μL of 50 μM) is diluted in 975 μL of 1× Assay Buffer, and 10 μL is dispensed in each well. DBeQ (10 μL) or 5% DMSO (10 μL) is then added to each well, and the plate is incubated at room temperature for 10 min. The ATPase assay is carried out by adding to each well 10 μL of 500 μM ATP (pH 7.5), incubating at room temperature for 60 min, and then adding 50 μL Kinase Glo Plus reagent, followed by a ?nal 10-min incubation at room temperature in the dark. Luminescence is read on an Analyst AD. DBeQ is assayed at a range of concentrations (0, 0.048, 0.24, 1.2, 6, and 30 μM) in triplicate.
Cell Research	Cells are seeded on a 384-well solid white plate (5,000 cells/well). Cells are transfected with luciferase siRNA or p97 siRNA (10 nM) for 48 hours or treated with DBeQ for the indicated amount of time. Caspase-3/7 Glo, caspase-6 Glo, caspase-8 Glo, or caspase-9 Glo is added into each well and mixed by shaking at 500 rpm for 1 min. Luminescence signal is determined after incubation at room temperature for 1 hour. Cellular viability is determined with CellTiter-Glo reagen. To determine the IC50 of cellular viability, cells are treated with MG132 or DBeQ at seven concentrations (threefold serial dilutions starting at 33 μM) for 48 hours. IC50 values are calculated from ?tting the percentage of luminescence signal normalized to DMSO treated cells).(Only for Reference)

Synonyms	JRF 12
Molecular Weight	340.42
Formula	C22H20N4
CAS No.	177355-84-9

Storage

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

Solubility Information

DMSO: 34 mg/mL (100 mM)

References and Literature

1. Chou TF, et al. Proc Natl Acad Sci U S A, 2011, 108(12), 4834-4839. 2. Chou TF, et al. Autophagy, 2011, 7(9), 1091-1092. 3. Hauler F, et al. Proc Natl Acad Sci U S A, 2012, 109(48), 19733-19738. 4. Ching JK, et al. Autophagy, 2013, 9(5), 799-800.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Bioactive Compounds Library Max Bioactive Compound Library Target-Focused Phenotypic Screening Library HIF-1 Signaling Pathway Compound Library Anti-Aging Compound Library NO PAINS Compound Library Autophagy Compound Library Apoptosis Compound Library Ubiquitination Compound Library

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

DBEQ 177355-84-9 Apoptosis Autophagy Ubiquitination p97 Inhibitor VCP JRF12 JRF 12 inhibit JRF-12 Cdc48 inhibitor

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.