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BioChemicals
VER-246608
tcsc0011787
VER-246608
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1mg
5mg
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100mg
$
271.00
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ORDERING INFORMATION
International
TAICLONE BIOTECH CORP.
order@taiclone.com
+886-2-2735-9682
+886-2-2735-9807
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Product Description
VER-246608 is a potent and ATP-competitive inhibitor of
pyruvate dehydrogenase kinase
(
PDK
) with
IC
50
s of 35 nM, 40 nM, 84 nM, and 91 nM for
PDK-1
,
PDK-3
,
PDK-2
, and
PDK-4
, respectively.
IC50 & Target: IC50: 35 nM (PDK-1), 40 nM (PDK-3), 84 nM (PDK-2), 91 nM (PDK-4)
[1]
In Vitro:
VER-246608 is a novel pan-isoform ATP competitive inhibitor of PDK. VER-246608 demonstrates similar potency across all four PDK isoforms in a DELFIA-based enzyme functional assay in the sub 100 nM range. In terms of cellular biomarker modulation, VER-246608 suppresses the phosphorylation of the Ser
293
residue of E1α (phosphorylated by all four PDK isozymes) with IC
50
values of 266 nM. Treatment of PC-3 cells with 9 μM and 27 μM VER-246608 results in a 21% and 42% reduction, respectively, in media L-lactate levels following a 1 h incubation. VER-246608 also decreases D-glucose consumption at the same concentrations that result in reduced L-lactate production. An approximately 50% reduction in spheroid volume is achieved at concentrations of 10 μM and above, suggesting an increase in VER-246608 potency compared to monolayer growth
[1]
.
Information
CAS No
1684386-71-7
Formula
C
28
H
23
ClF
2
N
4
O
4
Clinical Information
clinicalinformation
Pathway
Metabolic Enzyme/Protease
Target
PDHK
Specifications
Purity / Grade
>98%
Solubility
DMSO : 100 mg/mL (180.84 mM; Need ultrasonic)
Smiles
smiles
Misc Information
Observed Molecular Weight
552.96
related data
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