[CAS NO. 177355-84-9] DBeQ
PRODUCTS SPECIFICATIONS [177355-84-9]
DESCRIPTION [177355-84-9]
Overview
| MDL | MFCD03691820 |
|---|---|
| Molecular Weight | 340.42 |
| Molecular Formula | C22H20N4 |
| SMILES | C1(NCC2=CC=CC=C2)=NC(NCC3=CC=CC=C3)=C4C=CC=CC4=N1 |
1 Publications Citing Use of MCE
Summary
DBeQ is a selective, potent, reversible, and ATP-competitive p97 inhibitor, with an IC 50 value of 1.5 μM and 1.6 μM for p97(wt) and p97(C522A), respectively; DBeQ also inhibits Vps4 with an IC 50 of 11.5 μM.
In Vitro
DBeQ is a ATP-competitive p97 inhibitor, with an IC 50 value of 1.5 μM and 1.6 μM for p97(wt) and p97(C522A), respectively. DBeQ inhibits p97 competitively with respect to ATP, with a K i of 3.2 ± 0.4 μM. DBeQ inhibits degradation of the p97-dependent substrate UbG76V-GFP, with IC 50 value of 2.6 μM. DBeQ (10 μM) also significantly suppresses degradation of TCRα-GFP, induces CHOP but does not increase p21 level. Moreover, DBeQ inhibits the viability of MRC-5, Hek293, HeLa and RPMI8226 cells, with GI 50 s of 6.6 ± 2.9, 4 ± 0.6, 3.1 ± 0.5 and 1.2 ± 0.3, respectively [1] . DBeQ potently inhibits the AAA ATPase p97 by specifically binding to the ATPase site of its D2 domain (p97D2). DBeQ also inhibits Vps4, with an IC 50 of 11.5 μM. Furthermore, DBeQ (30 μM) inhibits hyphal growth of the wild-type cell (strain YLZ0) [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 35.71 mg/mL ( 104.90 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.9375 mL | 14.6877 mL | 29.3755 mL |
| 5 mM | 0.5875 mL | 2.9375 mL | 5.8751 mL |
| 10 mM | 0.2938 mL | 1.4688 mL | 2.9375 mL |
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Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.5 mg/mL (7.34 mM); Clear solution
References
- [1] Chou TF, et al.Reversible inhibitor of p97, DBeQ, impairs both ubiquitin-dependent and autophagic protein clearance pathways. Proc Natl Acad Sci U S A. 2011 Mar 22;108(12):4834-9.
- [2] Zhang Y, et al. The AAA ATPase Vps4 Plays Important Roles in Candida albicans Hyphal Formation and is Inhibited by DBeQ. Mycopathologia. 2016 Jun;181(5-6):329-39.