DBeQ

Modify Date: 2024-01-02 11:19:07

DBeQ Structure
DBeQ structure
Common Name DBeQ
CAS Number 177355-84-9 Molecular Weight 340.421
Density 1.3±0.1 g/cm3 Boiling Point 573.1±52.0 °C at 760 mmHg
Molecular Formula C22H20N4 Melting Point 149 °C
MSDS Chinese USA Flash Point 300.4±30.7 °C

 Use of DBeQ


DBeQ is a selective, potent, reversible, and ATP-competitive p97 inhibitor, with an IC50 value of 1.5 μM and 1.6 μM for p97(wt) and p97(C522A), respectively; DBeQ also inhibits Vps4 with an IC50 of 11.5 μM.

 Names

Name N,N'-Dibenzyl-2,4-quinazolinediamine
Synonym More Synonyms

 DBeQ Biological Activity

Description DBeQ is a selective, potent, reversible, and ATP-competitive p97 inhibitor, with an IC50 value of 1.5 μM and 1.6 μM for p97(wt) and p97(C522A), respectively; DBeQ also inhibits Vps4 with an IC50 of 11.5 μM.
Related Catalog
Target

IC50: 1.5 μM (p97)[1], 11.5 μM (Vps4)[2]

In Vitro DBeQ is a ATP-competitive p97 inhibitor, with an IC50 value of 1.5 μM and 1.6 μM for p97(wt) and p97(C522A), respectively. DBeQ inhibits p97 competitively with respect to ATP, with a Ki of 3.2 ± 0.4 μM. DBeQ inhibits degradation of the p97-dependent substrate UbG76V-GFP, with IC50 value of 2.6 μM. DBeQ (10 μM) also significantly suppresses degradation of TCRα-GFP, induces CHOP but does not increase p21 level. Moreover, DBeQ inhibits the viability of MRC-5, Hek293, HeLa and RPMI8226 cells, with GI50s of 6.6 ± 2.9, 4 ± 0.6, 3.1 ± 0.5 and 1.2 ± 0.3, respectively[1]. DBeQ potently inhibits the AAA ATPase p97 by specifically binding to the ATPase site of its D2 domain (p97D2). DBeQ also inhibits Vps4, with an IC50 of 11.5 μM. Furthermore, DBeQ (30 μM) inhibits hyphal growth of the wild-type cell (strain YLZ0)[2].
Cell Assay 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 h 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 h. Cellular viability is determined with CellTiter-Glo reagent. 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 h. IC50 values are calculated from fitting the percentage of luminescence signal normalized to DMSO treated cells)[1].
References

[1]. Chou TF, et al.Reversible inhibitor of p97, DBeQ, impairs both ubiquitin-dependent and autophagic protein clearance pathways. Proc Natl Acad Sci U S A. 2011 Mar 22;108(12):4834-9.

[2]. Zhang Y, et al. The AAA ATPase Vps4 Plays Important Roles in Candida albicans Hyphal Formation and is Inhibited by DBeQ. Mycopathologia. 2016 Jun;181(5-6):329-39.

 Chemical & Physical Properties

Density 1.3±0.1 g/cm3
Boiling Point 573.1±52.0 °C at 760 mmHg
Melting Point 149 °C
Molecular Formula C22H20N4
Molecular Weight 340.421
Flash Point 300.4±30.7 °C
Exact Mass 340.168793
PSA 56.30000
LogP 4.34
Appearance of Characters white to beige
Vapour Pressure 0.0±1.6 mmHg at 25°C
Index of Refraction 1.735
Storage condition room temp
Water Solubility DMSO: ≥20mg/mL

 Safety Information

Hazard Codes Xn
Risk Phrases 22-36
Safety Phrases 26

 Synonyms

2,4-dibenzylaminoquinazoline
N,N'-Dibenzyl-2,4-quinazolinediamine
2,4-Quinazolinediamine, N,N-bis(phenylmethyl)-
DBeQ
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