DBeQ Chemical Properties

Melting point:

149 °C

Boiling point:

573.1±52.0 °C(Predicted)

Density 

1.259±0.06 g/cm3(Predicted)

storage temp. 

room temp

solubility 

DMSO: ≥20mg/mL

form 

powder

pka

7.78±0.30(Predicted)

color 

white to beige

Stability:

Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 2 months.

InChIKey

QAIMUUJJAJBPCL-UHFFFAOYSA-N

CAS DataBase Reference

177355-84-9

Safety Information

Hazard Codes 

Xn

Risk Statements 

22-36

Safety Statements 

26

WGK Germany 

3

HS Code 

2933.59.8000

DBeQ Usage And Synthesis

Description

DBeQ (177355-84-9) is a potent, selective and reversible inhibitor of the AAA-ATPase p97 (ATPase associated with diverse cellular activities). Ki=3.2 μM. DBeQ blocks ubiquitin-dependent protein clearance pathways. Cell permeable.

Uses

The ATPase p97 is an ubiquitin-selective chaperone known to play a critical role in the degradation of misfolded membrane and secretory proteins and has been linked to various cellular processes that require unfolding and disassembly of protein complexes. DBeQ is a selective, reversible, and ATP-competitive inhibitor of the ATPase p97 (Ki = 3.2 μM; IC50 = 1.5 μM). It does not exhibit activity when tested against a panel 170 protein kinases at concentrations as high as 15 μM. At 10 μM it blocks endoplasmic reticulum-associated degradation, impairing the autophagy pathway and promoting the activation of caspase-3 and -7 in cancer cells.[Cayman Chemical]

Uses

HeLa cells were treated with DBeQ and the effects on in vivo ubiquitination and protein dislocation were studied by live cell imaging.

Biochem/physiol Actions

DBeQ is a potent and specific inhibitor of ATPase p97, an integral component of the ubiquitin-fusion degradation (UFD) pathway. DBeQ inhibits the degradation of ubiquitinated proteins, the endoplasmic reticulum-associated degradation pathway, and autophagosome maturation. The compound also potently inhibits cellular proliferation and induces caspase 3/7 activity and apoptosis.

storage

Store at +4°C

References

1) Chou et al. (2011), Reversible inhibitor of p97, DBeQ, impairs both ubiquitin-dependent and autophagic protein clearance pathways; Proc. Natl. Acad. Sci. USA, 108 4834

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