GLPBio

DBeQ

Catalog No.: GC10824Purity:>99.50%Synonyms: N,N'Dibenzylquinazoline2,4diamine, JRF 12
DBeQ ist ein selektiver, potenter, reversibler und ATP-kompetitiver p97-Inhibitor mit einem IC50-Wert von 1,5 μM und 1,6 μM fÜr p97(wt) bzw. p97(C522A); DBeQ hemmt auch Vps4 mit einem IC50 von 11,5 μM.

Die Produkte sind ausschließlich für Forschungszwecke bestimmt. Nicht zur Anwendung am Menschen. Wir verkaufen nicht an Patienten.


DBeQ
Cas No.: 177355-84-9
10mM (in 1mL DMSO)In Stock
$47.00
1
10mgIn Stock
$70.00
1
50mgIn Stock
$238.00
1

Zitate (Citations)

Für dieses Produkt sind derzeit keine Zitate verfügbar. Nachfolgend finden Sie ausgewählte Publikationen, die GlpBio-Produkte zitieren.
  • Nature cover
    Nature
    641, 529–536 (2025)
  • Nature cover
    Nature
    628, 630–638 (2024)
  • Nature cover
    Nature
    632, 686–694 (2024)
  • Nature cover
    Nature
    618, 1017–1023 (2023)
  • Nature cover
    Nature
    610, 366–372 (2022)
  • Cell cover
    Cell
    187(9):2288-2304 (2024)
  • Cell cover
    Cell
    183(7):1867-1883 (2020)
  • Science cover
    Science
    388(6745) (2025)
  • Science cover
    Science
    387(6739) (2025)
  • Science cover
    Science
    387(6734) (2025)
  • Cell Research cover
    Cell Research
    35, 97–116 (2025)
  • Cell Research cover
    Cell Research
    34, 683–706 (2024)
  • Cell Research cover
    Cell Research
    33, 273–287 (2023)
  • Cell Research cover
    Cell Research
    33, 546–561 (2023)
  • Cell Research cover
    Cell Research
    33, 904–922 (2023)
  • Cell Research cover
    Cell Research
    31, 1291–1307 (2021)

Beschreibung (Description)

DBeQ is a selective and reversible inhibitor of p97 ATPase (IC50 = 1.5 μM) which induces caspase-3 and caspase-7 rapidly.
p97 knows also as VCP ( Cdc48 in yeast) is a hexameric ATPase of the AAA family which disassembles SNARE proteins after membrane fusion.[1] It is involved in a fusion of homotypic membranes, protein degradation, and activation of membrane-bound transcription factors.[2] p97 is one of the most abundant proteins in the eukaryotic cytosol and its segregase function has been linked to a large number of biological processes including endoplasmic reticulum-associated degradation(ERAD), mitochondrial associated degradation, ubiquitin fusion degradation, homotypic membrane fusion, cell cycle regulation, autophagy and transcription factor regulation.[3]
DBeQ can block the degradation of endoplasmic reticulum-associated degradation (ERAD) reporters and also block autophagosome maturation,all of which are proven to be important in cancer therapy.[4,5] DBeQ is ATP-sensitive and selectively target D1and D2 domain with ODD-Luc IC50 56 μM, Luc-ODC IC50 45 μM,UbG76VGFP IC50 2.3 μM, much less affected by the presence of p47 than the other quinazolines.[6,7]
References:
1.  Zhang, X. et al. "Structure of the AAA ATPase p97". Molecular cell 2000, 6 (6): 1473–84.
2.  Madsen, L. et al. "New ATPase regulators--p97 goes to the PUB.". Int J Biochem Cell Biol 2009, 41 (12): 2380–8.
3.  Eli Chapman. et al. “Inhibitors of the AAA+ Chaperone p97”. Molecules 2015, 20(2), 3027-3049.
4.  Liu, Y. Et al. “VCP/p97,down-regulated by microRNA-129-5p, could regulate the progression of hepatocellular carcinoma”. PLoS One 2012, 7, e35800.
5.  Laguë, M.N. et al. “Proteomic profiling of a mouse model for ovarian granulosa cell tumor identifies VCP as a highly sensitive serum tumor marker in several human cancers.” PLoS One 2012, 7, e42470.
6.  Fang, C.J. et al. “Evaluating p97 inhibitor analogues for their domain selectivity and potency against the p97–p47 complex.” Chem. Med. Chem. 2014.
7.  Chou, T.F. et al. “Specific inhibition of p97/VCP ATPase and kinetic analysis demonstrated interaction between D1 and D2 ATPase domains.” J. Mol. Biol. 2014, 426, 2886–2899.

Protokoll (Protocol)

Cell experiment [1]:

Cell lines

HeLa cells, HEK293 cells

Preparation method

The solubility of this compound in DMSO is > 16.0 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

5 h

Applications

In HeLa cells, DBeQ blocked UbG76V-GFP, ODD-Luc and Luc-ODC degradation with IC50 of 2.6 μM, 56 μM and 45 μM. DBeQ (10 μM) potently blocked degradation of TCRα-GFP in HEK293 cells. DBeQ dose-dependently induced CHOP within 3 hours. DBeQ (15 μM) induced a strong accumulation of LC3-II in the nucleus plus membrane-enriched and cytosolic fractions in Hela cells. DBeQ functioned by blocking autophagic degradation of LC3-II instead of inducing autophagy in HeLa cells. DBeQ (10 μM) rapidly promoted activation of the “executioner” caspases-3 and -7 in HeLa cells. DBeQ was five-fold more active against multiple myeloma (RPMI8226) cells than normal human fetal lung fibroblasts (MRC5), with HeLa and Hek293 cells showing intermediate sensitivities.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Chou T F, Brown S J, Minond D, et al. Reversible inhibitor of p97, DBeQ, impairs both ubiquitin-dependent and autophagic protein clearance pathways[J]. Proceedings of the National Academy of Sciences, 2011, 108(12): 4834-4839.

Produktdokumente (Product Documents)

Purity:>99.50%Appearance:A solid

Chemische Eigenschaften (Chemical Properties)

CAS-Nr.
177355-84-9
Synonyme
N,N'Dibenzylquinazoline2,4diamine, JRF 12
Chemischer Name
2-N,4-N-dibenzylquinazoline-2,4-diamine
SMILES
C1=CC=C(C=C1)CNC2=NC(=NC3=CC=CC=C32)NCC4=CC=CC=C4
Summenformel
C22H20N4
Molekulargewicht
340.42
Löslichkeit
≥ 16mg/mL in DMSO
Lagerung
Store at -20°C
Allgemeine Hinweise
Wählen Sie anhand der Löslichkeitsdaten des Produkts ein geeignetes Lösungsmittel. Aliquotieren Sie die Stammlösung nach der Herstellung, um wiederholte Gefrier-Auftau-Zyklen zu vermeiden.
Verwenden Sie Stammlösungen bei Lagerung bei -80°C innerhalb von 6 Monaten bzw. bei -20°C innerhalb von 1 Monat.
Zur Verbesserung der Löslichkeit das Röhrchen auf 37°C erwärmen und für eine angemessene Dauer beschallen.
Versandbedingungen
Evaluierungsmuster werden mit Kühlakkus versandt. Andere verfügbare Größen werden bei Raumtemperatur oder auf Anfrage mit Kühlakkus versandt.

Rechner (Calculators)Molarität / Verdünnung / Molekulargewicht / Einheitenumrechnung / In-vivo-Formulierung / Löslichkeit

g/mol

Reviews

Review for DBeQ

Rating: 5
  • 5 Star100%
  • 4 Star0%
  • 3 Star0%
  • 2 Star0%
  • 1 Star0%