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.
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 |
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.
[3] Chou TF, et al. Autophagy. Development of p97 AAA ATPase inhibitors.
Related p97 Products |
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CB-5339
CB-5339 is a potent p97 inhibitor with an IC50 <30 nM (WO2015109285A1, compound FF07). |
CB-5083
CB-5083 is a first-in-class, potent and selective, orally bioavailable inhibitor of the p97 AAA ATPase/VCP. CB-5083 selectively inhibits p97 through its D2 site with the IC50 of 11 nM. |
NMS-873
NMS-873 is an allosteric and specific p97 inhibitor with IC50 of 30 nM. |
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