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Datasheet of DBeQ

Description:.
DBeQ(JRF-12) is a selective, potent, reversible, and ATP-competitive p97 inhibitor with IC50 of 1.5 M.
in vitro: DBeQ blocks UbG76V-GFP, ODD-Luc and Luc-ODC degradation with IC50 of 2.6 M, 56 M and 45 M in HeLa
cells. DBeQ is at least 50-fold less potent toward N-ethylmaleimidesensitive factor (NSF) and 26S proteasome. DBeQ inhibits
p97 competitively with respect to ATP, with Ki of 3.2 M, suggesting that it binds to the active site of the D2 domain. DBeQ (10
M) potently blocks degradation of TCR-GFP in HEK293 cells. DBeQ induces CHOP within 3 hours in a
concentration-dependent manner but does not increase p21 level in HEK293 cells. DBeQ (15 M) induces a strong accumulation
of LC3-II in the nucleus plus membrane-enriched and cytosolic fractions in Hela cells. DBeQ acts by blocking autophagic
degradation of LC3-II instead of inducing autophagy in HeLa cells. DBeQ (10 M) rapidly promotes activation of the
executioner caspases-3 and -7 in HeLa cells. DBeQ activates the intrinsic caspase-9 apoptotic pathway more than the extrinsic
caspase-8 pathway, whereas STS activates both pathways to a similar extent. DBeQ is fivefold more active against multiple
myeloma (RPMI8226) cells than normal human fetal lung fibroblasts (MRC5), with HeLa and Hek293 cells showing
intermediate sensitivities[1]. DBeQ exhibits 20-fold selectivity for stabilizing p97-dependent vs. independent UPS reporter
substrates in HeLa cells. DBeQ impairs degradation of substrates within the ERAD and autophagy pathways [2]. DBeQ (12 M)
inhibits intracellular neutralization in a dose-dependent manner in HeLa cells. DBeQ (10 M), which completely inhibits
degradation of virus and antibody in the fate-of-capsid experiment, fails to prevent degradation of IgG Fc. DBeQ (9 M) 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
Catalog

DC7602

Purity of current batch:

>98%

Molecular Weight (MW)

340.42

Molecular Formula

C22H20N4

CAS No.

177355-84-9

Solubility (25C)

DMSO

Storage

Store at -20C (desiccating conditions).

Handling:
Providing storage is as stated on the product vial and the vial is kept tightly sealed, the product can be stored for up to 24 months.
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in
advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20C. Generally, these will be useable
for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room
temperature for at least 1 hour.