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DBeQ

Cat. No. M2614
DBeQ Structure
Synonym:

JRF 12

Size Price Availability Quantity
5mg USD 55  USD55 In stock
10mg USD 90  USD90 In stock
25mg USD 200  USD200 In stock
50mg USD 360  USD360 In stock
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Quality Control & Documentation
Biological Activity

DBeQ is a selective, potent, reversible, and ATP-competitive p97 inhibitor with IC50 of 1.5 μM. DBeQ blocks UbG76V-GFP, ODD-Luc and Luc-ODC degradation with IC50 of 2.6 μM, 56 μM and 45 μM in HeLa cells. DBeQ (9 μM) reduces the initial gradient of neutralization as a function of antibody concentration. DBeQ decreases both basal and nutrient-stimulated phosphorylation of MTOR targets similar to the effects of rapamycin in U20S cells.

Chemical Information
Molecular Weight 340.42
Formula C22H20N4
CAS Number 177355-84-9
Solubility (25°C) DMSO: ≥ 50 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Ching JK, et al. Autophagy. Rapamycin-induced autophagy aggravates pathology and weakness in a mouse model of VCP-associated myopathy.

[2] Hauler F, et al. Proc Natl Acad Sci U S A. AAA ATPase p97/VCP is essential for TRIM21-mediated virus neutralization.

[3] Chou TF, et al. Autophagy. Development of p97 AAA ATPase inhibitors.

[4] Chou TF, et al. Proc Natl Acad Sci U S A. Reversible inhibitor of p97, DBeQ, impairs both ubiquitin-dependent and autophagic protein clearance pathways.

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NMS-873

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  Catalog
Abmole Inhibitor Catalog




Keywords: DBeQ, JRF 12 supplier, p97, inhibitors, activators


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