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Product Name: | DBeQ | Synonyms: | DBeQ;2,4-QuinazolinediaMine, N2,N4-bis(phenylMethyl)-;2,4-QuinazolinediaMine, N,N'-bis(phenylMethyl)-;JRF 12;N,N'-Dibenzylquinazoline-2,4-diamine;N2,N4-Dibenzylquinazoline-2,4-diamine;JRF;N,N'-Dibenzylquinazoline-2,4-diamine DBeQ | CAS: | 177355-84-9 | MF: | C22H20N4 | MW: | 340.42 | EINECS: | | Product Categories: | API;Inhibitors | Mol File: | 177355-84-9.mol | |
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. | InChIKey | QAIMUUJJAJBPCL-UHFFFAOYSA-N | CAS DataBase Reference | 177355-84-9 |
Hazard Codes | Xn | Risk Statements | 22-36 | Safety Statements | 26 | WGK Germany | 3 | HS Code | 2933.59.8000 |
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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