2. Metabolic Enzyme/Protease
  3. PDHK
  4. VER-246608

VER-246608 is a potent and ATP-competitive inhibitor of pyruvate dehydrogenase kinase (PDK) with IC50s of 35 nM, 40 nM, 84 nM, and 91 nM for PDK-1, PDK-3, PDK-2, and PDK-4, respectively.

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

VER-246608 Chemical Structure

VER-246608 Chemical Structure

CAS No. : 1684386-71-7

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10 mM * 1 mL in DMSO
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Customer Review

Based on 2 publication(s) in Google Scholar

VER-246608 Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

VER-246608 is a potent and ATP-competitive inhibitor of pyruvate dehydrogenase kinase (PDK) with IC50s 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]
Cellular Effect
Cell Line Type Value Description References
DU-145 GI50
> 50 μM
Compound: 6; VER-246608
Antiproliferative activity against p53 deficient human DU145 cells incubated for 72 hrs by CellTiter-Glo assay
Antiproliferative activity against p53 deficient human DU145 cells incubated for 72 hrs by CellTiter-Glo assay
[PMID: 31469962]
NCI-H1299 GI50
> 50 μM
Compound: 6; VER-246608
Antiproliferative activity against p53 deficient human H1299 cells incubated for 72 hrs by CellTiter-Glo assay
Antiproliferative activity against p53 deficient human H1299 cells incubated for 72 hrs by CellTiter-Glo assay
[PMID: 31469962]
PC-3 GI50
26.2 μM
Compound: 40
Antiproliferative activity against human PC3 cells after 96 hrs by sulphorhodamine B assay
Antiproliferative activity against human PC3 cells after 96 hrs by sulphorhodamine B assay
[PMID: 28199108]
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 Ser293 residue of E1α (phosphorylated by all four PDK isozymes) with IC50 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].

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

VER-246608 Related Antibodies
Molecular Weight

552.96

Formula

C28H23ClF2N4O4
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=CC=C(O)C=C1O)N(CC2=CC=C(CNC(C(F)F)=O)C=C2)C(C=C3)=CC=C3C4=NC(Cl)=NC=C4C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (180.84 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8084 mL 9.0422 mL 18.0845 mL
5 mM 0.3617 mL 1.8084 mL 3.6169 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (4.52 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (4.52 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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mg/kg

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(per animal)

g

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(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
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% 
+
%
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%
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References
Kinase Assay
[1]

DELFIA assay reagents (assay buffer, wash buffer, enhancement solution and anti-rabbit IgG-Eu-N1 secondary antibody) and plates are used. Test compounds are subjected to a 10 point tripling dilution in DMSO, diluted in MOPS buffer (60 mM MOPS pH7.2, 15 mM Magnesium acetate, 60 mM KCl) and added to the enzyme mix (10 nM PDK-1, 2 and 3 or 20 nM PDK-4, 300 nM E1, 0.1 mg/mL BSA, 1 mM DTT) in 96-well V-bottom plates. The reaction is initiated by the addition of ATP to a final concentration of 5 μM followed by a 1 h incubation at 30°C. The reaction is then stopped by the addition of STOP solution (50 mM Carbonate-Bicarbonate Buffer, pH 9.6), and then transferred to 96 well DEFLIA yellow plates. The plates are then sealed and incubated o/n at 4°C. Detection and quantification of p(Ser293)E1α levels is then achieved through incubation with anti-p(Ser293)E1α primary antibody followed by anti-rabbit secondary IgG-Eu-N1 antibody and addition of enhancement solution. The time-resolved fluorescent signal is then measured using a Victor2 plate reader. The data is fitted by non-linear regression using XLFIT4 within a custom ABASE (IDBS) protocol in order to determine IC50 values[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay
[1]

Compound cytotoxicity is determined using the Sulforhodamine B assay for cells cultured as a monolayer. For spheroid growth experiments, PC-3 cells are seeded (500 cells/well) into 96 well round bottom plates in RPMI-1640 media containing 2.5% (w/v) Matrigel. The resultant spheroids are treated with VER-246608 (2.5, 5, 10, 20, and 40 μM) 48 h post-seeding. Spheroid volumes are determined by obtaining diameter measurements from images taken on a Zeiss Axiovert 200 M inverted microscope using the axiovision software[1].

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

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.8084 mL 9.0422 mL 18.0845 mL 45.2112 mL
5 mM 0.3617 mL 1.8084 mL 3.6169 mL 9.0422 mL
10 mM 0.1808 mL 0.9042 mL 1.8084 mL 4.5211 mL
15 mM 0.1206 mL 0.6028 mL 1.2056 mL 3.0141 mL
20 mM 0.0904 mL 0.4521 mL 0.9042 mL 2.2606 mL
25 mM 0.0723 mL 0.3617 mL 0.7234 mL 1.8084 mL
30 mM 0.0603 mL 0.3014 mL 0.6028 mL 1.5070 mL
40 mM 0.0452 mL 0.2261 mL 0.4521 mL 1.1303 mL
50 mM 0.0362 mL 0.1808 mL 0.3617 mL 0.9042 mL
60 mM 0.0301 mL 0.1507 mL 0.3014 mL 0.7535 mL
80 mM 0.0226 mL 0.1130 mL 0.2261 mL 0.5651 mL
100 mM 0.0181 mL 0.0904 mL 0.1808 mL 0.4521 mL
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VER-246608 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

VER-2466081684386-71-7VER246608VER 246608PDHKPyruvate dehydrogenase kinasePDH kinaseInhibitorinhibitorinhibit

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