1. Cell Cycle/DNA Damage
  2. p97

DBeQ (Synonyms: JRF 12)

Cat. No.: HY-15945 Purity: 98.84%
Handling Instructions

DBeQ is a selective, potent, reversible, and ATP-competitive p97 inhibitor, with an IC50 value of 1.5 μM and 1.6 μM for p97(wt) and p97(C522A), respectively; DBeQ also inhibits Vps4 with an IC50 of 11.5 μM.

For research use only. We do not sell to patients.

DBeQ Chemical Structure

DBeQ Chemical Structure

CAS No. : 177355-84-9

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 79 In-stock
Estimated Time of Arrival: December 31
5 mg USD 72 In-stock
Estimated Time of Arrival: December 31
10 mg USD 108 In-stock
Estimated Time of Arrival: December 31
50 mg USD 480 In-stock
Estimated Time of Arrival: December 31
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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

DBeQ is a selective, potent, reversible, and ATP-competitive p97 inhibitor, with an IC50 value of 1.5 μM and 1.6 μM for p97(wt) and p97(C522A), respectively; DBeQ also inhibits Vps4 with an IC50 of 11.5 μM.

IC50 & Target

IC50: 1.5 μM (p97)[1], 11.5 μM (Vps4)[2]

In Vitro

DBeQ is a ATP-competitive p97 inhibitor, with an IC50 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 Ki of 3.2 ± 0.4 μM. DBeQ inhibits degradation of the p97-dependent substrate UbG76V-GFP, with IC50 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 GI50s 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 IC50 of 11.5 μM. Furthermore, DBeQ (30 μM) inhibits hyphal growth of the wild-type cell (strain YLZ0)[2].

Solvent & Solubility
In Vitro: 

DMSO : ≥ 47 mg/mL (138.06 mM)

*"≥" means soluble, but saturation unknown.

Preparing
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
*Please refer to the solubility information to select the appropriate solvent.
References
Cell Assay
[1]

Cells are seeded on a 384-well solid white plate (5,000 cells/well). Cells are transfected with luciferase siRNA or p97 siRNA (10 nM) for 48 h or treated with DBeQ for the indicated amount of time. Caspase-3/7 Glo, caspase-6 Glo, caspase-8 Glo, or caspase-9 Glo is added into each well and mixed by shaking at 500 rpm for 1 min. Luminescence signal is determined after incubation at room temperature for 1 h. Cellular viability is determined with CellTiter-Glo reagent. To determine the IC50 of cellular viability, cells are treated with MG132 or DBeQ at seven concentrations (threefold serial dilutions starting at 33 μM) for 48 h. IC50 values are calculated from fitting the percentage of luminescence signal normalized to DMSO treated cells)[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

340.42

Formula

C₂₂H₂₀N₄

CAS No.

177355-84-9

SMILES

C1(NCC2=CC=CC=C2)=NC(NCC3=CC=CC=C3)=C4C=CC=CC4=N1

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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This equation is commonly abbreviated as: C1V1 = C2V2

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× = ×
C1   V1   C2   V2

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Product Name:
DBeQ
Cat. No.:
HY-15945
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DBeQ

Cat. No.: HY-15945