DBeQ
Synonym(s):JRF 12;N2,N4-dibenzylquinazoline-2,4-diamine
- CAS NO.:177355-84-9
- Empirical Formula: C22H20N4
- Molecular Weight: 340.42
- MDL number: MFCD03691820
- SAFETY DATA SHEET (SDS)
- Update Date: 2023-06-30 15:45:59
What is DBeQ?
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.
The Uses of DBeQ
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]
The Uses of DBeQ
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
Properties of DBeQ
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 |
pka | 7.78±0.30(Predicted) |
form | powder |
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. |
CAS DataBase Reference | 177355-84-9 |
Safety information for DBeQ
Signal word | Warning |
Pictogram(s) |
Exclamation Mark Irritant GHS07 |
GHS Hazard Statements |
H302:Acute toxicity,oral H319:Serious eye damage/eye irritation |
Precautionary Statement Codes |
P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing. |
Computed Descriptors for DBeQ
InChIKey | QAIMUUJJAJBPCL-UHFFFAOYSA-N |
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