2. Metabolic Enzyme/Protease Cell Cycle/DNA Damage
  3. PDHK HSP
  4. PDK-IN-1

PDK-IN-1 (compound 7o) is a pyruvate dehydrogenase kinase (PDK) inhibitor. PDK-IN-1 shows IC50 values of 0.03 and 0.1 μM for PDK1 and HSP90, respectively. PDK-IN-1 targets PDH/PDK axis thus reducing efficiently the tumor mass.

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

PDK-IN-1 Chemical Structure

PDK-IN-1 Chemical Structure

CAS No. : 2897696-10-3

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Based on 1 publication(s) in Google Scholar

PDK-IN-1 Related Antibodies

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Description

PDK-IN-1 (compound 7o) is a pyruvate dehydrogenase kinase (PDK) inhibitor. PDK-IN-1 shows IC50 values of 0.03 and 0.1 μM for PDK1 and HSP90, respectively. PDK-IN-1 targets PDH/PDK axis thus reducing efficiently the tumor mass[1].

IC50 & Target

IC50: 0.03 ± 0.005 μM (PDK1); 0.1 μM (HSP90)[1]
In Vitro

PDK-IN-1 (compound 7o) shows 2D cytotoxic activity against PSN-1 and BxPC-3 pancreatic cell lines, with IC50 values of 0.1 ± 0.04 and 1.0 ± 0.2 μM, respectively. PDK-IN-1 also shows 3D cytotoxic activity, with IC50 values of 3.3 ± 0.2 and 11.9 ± 1.1 μM, respectively[1].

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

PDK-IN-1 Related Antibodies
In Vivo

PDK-IN-1 (compound 7o) is slightly more effective than cisplatin (HY-17394) in reducing the tumor mass[1].
PDK-IN-1 intensely reduces PDH phosphorylation in Lewis Lung Carcinoma (LLC)-bearing mice[1].

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

Animal Model: LLC-bearing C57BL mice[1]
Dosage: 20 mg/kg
Administration: IP, daily, days 7-14
Result: Reduced more tumor mass than cisplatin (HY-17394) (tumor inhibition by 86 and 84% for compound 7o and cisplatin, respectively). Induced a body weight loss much lower than that induced by cisplatin (HY-17394) and gemcitabine (HY-17026).
Molecular Weight

450.29

Formula

C20H16BrN7O
CAS No.
Appearance

Solid

Color

Off-white to yellow

SMILES

BrC1=CC(C(C2=C(C3=CNC4=C3C=C(OC)C=C4)N=NC(N)=N2)=CN5C)=C5N=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (55.52 mM; ultrasonic and warming and heat to 60°C; 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 2.2208 mL 11.1040 mL 22.2079 mL
5 mM 0.4442 mL 2.2208 mL 4.4416 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, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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  • Dilution Calculator

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

Mass
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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Concentration (final)

C2

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Volume (final)

V2

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 (5.55 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(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:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
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).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

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

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, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.2208 mL 11.1040 mL 22.2079 mL 55.5198 mL
5 mM 0.4442 mL 2.2208 mL 4.4416 mL 11.1040 mL
10 mM 0.2221 mL 1.1104 mL 2.2208 mL 5.5520 mL
15 mM 0.1481 mL 0.7403 mL 1.4805 mL 3.7013 mL
20 mM 0.1110 mL 0.5552 mL 1.1104 mL 2.7760 mL
25 mM 0.0888 mL 0.4442 mL 0.8883 mL 2.2208 mL
30 mM 0.0740 mL 0.3701 mL 0.7403 mL 1.8507 mL
40 mM 0.0555 mL 0.2776 mL 0.5552 mL 1.3880 mL
50 mM 0.0444 mL 0.2221 mL 0.4442 mL 1.1104 mL
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PDK-IN-1 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:

PDK-IN-12897696-10-3PDHKHSPPyruvate dehydrogenase kinasePDH kinaseHeat shock proteinsPSN-1 cancer cellsBxPC-3Lewis Lung CarcinomaInhibitorinhibitorinhibit

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