Art. -Nr.: HY-135954

PDK4-IN-1

3 Cited Publications

Kundenbewertung

Based on 3 publication(s) in Google Scholar

PDK4-IN-1 is an anthraquinone derivative and a potent and orally active pyruvate dehydrogenase kinase 4 (PDK4) inhibitor with an IC₅₀ value of 84 nM. PDK4-IN-1 potently represses cellular transformation and cellular proliferation and induces apoptosis. PDK4-IN-1 has antidiabetic, anticancer and anti-allergic activity.

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Reinheit: 99.34%
CAS. Nr.: 2310262-10-1
Formel: C₂₂H₁₉N₃O₂
Molecular Weight:357.41

Speicherung:

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)

PDK4-IN-1 Chemical Structure

CAS. Nr.: 2310262-10-1

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (3)
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

IC50: 84 nM (Pyruvate dehydrogenase kinase 4 (PDK4))^[1]

In Vitro

PDK4-IN-1 (Compound 8c; 50 μM; 0-72 hours; HCT116 and RKO cells) treatment significantly impedes the proliferation of human colon cancer cell lines, HCT116 and RKO. The colony formation efficiency in HCT116 and RKO cells Is significantly reduced after treatment of PDK4-IN-1^[1].
PDK4-IN-1 (Compound 8c; 10-50 μM; 24 hours; HCT116 and RKO cells) treatment dose-dependently increased apoptosis^[1].
PDK4-IN-1 (Compound 8c; 10 μM; 24 hours; HEK293T cells) treatment inhibits phosphorylation of Ser²³², Ser²⁹³, and Ser³⁰⁰ of PDHE1α^[1].
10 μM of PDK4-IN-1 (Compound 8c) significantly increases p-Akt in AML12 cells^[1].
PDK4-IN-1 (compound 8c)-induced phosphorylation of p53 on serine 15 is a dose-dependent response in both HCT116 and RKO cells. PDK4-IN-1 decreases the expression of BCL-xL and increases the expression of BAX. Cleavage of PARP1 and caspase 3 are increased by PDK4-IN-1^[1].

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

Cell Viability Assay^[1]

Cell Line:

HCT116 and RKO cells
Concentration:

50 μM
Incubation Time:

0 hour, 24 hours, 48 hours, 72hours
Result:

Significantly impeded the proliferation of human colon cancer cell lines, HCT116 and RKO.

Apoptosis Analysis^[1]

Cell Line:

HCT116 and RKO cells
Concentration:

10 μM, 25 μM, 50 μM
Incubation Time:

24 hours
Result:

Dose-dependently increased apoptosis.

Western Blot Analysis^[1]

Cell Line:

HEK293T human embryonic kidney cells
Concentration:

10 μM
Incubation Time:

24 hours
Result:

Inhibited phosphorylation of Ser²³², Ser²⁹³, and Ser³⁰⁰ of PDHE1α.

In Vivo

PDK4-IN-1 (Compound 8c; 100 mg/kg; oral administration; daily; for 1 week; C57BL/6J mice) treatment significantly improves glucose tolerance^[1].
Pre-incubation with PDK4-IN-1 (compound 8c) dose-dependently inhibits the release of β-hexosaminidase from IgE/antigen-activated BMMCs, showing that the absorbance values are 0.26, 0.20, and 0.126 in IgE/Ag, 10 μM, and 20 μM PDK4-IN-1-treated BMMCs^[1].
The pharmacokinetic (PK) profiles of PDK4-IN-1 (compound 8c) are evaluated in rat. PDK4-IN-1 shows good bioavailability (64%), long half-life (>7 h), and moderate clearance (CL of 0.69) in rats^[1].

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

Animal Model:

C57BL/6J mice (8-week old) fed with high-fat diet^[1]
Dosage:

100 mg/kg
Administration:

Oral administration; daily; for 1 week
Result:

Significantly improved glucose tolerance.

Chemical Information

CAS. Nr. 2310262-10-1
Appearance Solid
Molecular Weight 357.41
Formel C₂₂H₁₉N₃O₂
Color Light yellow to yellow
SMILES

O=C1C2=C(C=CC=C2)C(C3=CC=CC(C4=CN(C5CCNCC5)N=C4)=C13)=O
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

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)

Publications (3)

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Journal Impact Factor

Aging Cell

Cardiomyocyte Pdk4 response is associated with metabolic maladaptation in aging. [Abstract]

2023 Apr;22(4):e13800. PMID: 36797808
Biochem Pharmacol

Targeting PDK4 attenuates neointimal hyperplasia and regulates VSMC phenotypic switching, apoptosis, and autophagy. [Abstract]

2026 Feb 12:247:117805. PMID: 41687829
bioRxiv

2024 August 19.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (279.79 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.7979 mL

13.9895 mL

27.9791 mL

5 mM

0.5596 mL

2.7979 mL

5.5958 mL

10 mM

0.2798 mL

1.3990 mL

2.7979 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (281 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Lee D, et al. Discovery of Novel Pyruvate Dehydrogenase Kinase 4 Inhibitors for Potential Oral Treatment of Metabolic Diseases. J Med Chem. 2019 Jan 24;62(2):575-588. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.7979 mL	13.9895 mL	27.9791 mL	69.9477 mL
	5 mM	0.5596 mL	2.7979 mL	5.5958 mL	13.9895 mL
	10 mM	0.2798 mL	1.3990 mL	2.7979 mL	6.9948 mL
	15 mM	0.1865 mL	0.9326 mL	1.8653 mL	4.6632 mL
	20 mM	0.1399 mL	0.6995 mL	1.3990 mL	3.4974 mL
	25 mM	0.1119 mL	0.5596 mL	1.1192 mL	2.7979 mL
	30 mM	0.0933 mL	0.4663 mL	0.9326 mL	2.3316 mL
	40 mM	0.0699 mL	0.3497 mL	0.6995 mL	1.7487 mL
	50 mM	0.0560 mL	0.2798 mL	0.5596 mL	1.3990 mL
	60 mM	0.0466 mL	0.2332 mL	0.4663 mL	1.1658 mL
	80 mM	0.0350 mL	0.1749 mL	0.3497 mL	0.8743 mL
	100 mM	0.0280 mL	0.1399 mL	0.2798 mL	0.6995 mL

Keywords

PDK4-IN-1

3 Cited Publications

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PDK4-IN-1

Apoptosis Compound Library

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Anti-diabetic Compound Library

Glycolysis Compound Library

Orally Active Compound Library

Anti-Cancer Metabolism Compound Library

Mitochondria-Targeted Compound Library

Glucose Metabolism Compound Library

Heterocyclic Compound Library

Metabolic Enzyme Compound Library

TCA Cycle Compound Library

Cell Death Library

Bioactive Compound Library Max

Bioactive Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Lactic Acid Metabolic Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) PDK4-IN-1

Biologische Aktivität

Chemical Information

Publications (3)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

PDK4-IN-1

Apoptosis Compound Library

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Anti-diabetic Compound Library

Glycolysis Compound Library

Orally Active Compound Library

Anti-Cancer Metabolism Compound Library

Mitochondria-Targeted Compound Library

Glucose Metabolism Compound Library

Heterocyclic Compound Library

Metabolic Enzyme Compound Library

TCA Cycle Compound Library

Cell Death Library

Bioactive Compound Library Max

Bioactive Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Lactic Acid Metabolic Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) PDK4-IN-1

Biologische Aktivität

Chemical Information

Publications (3)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

PDK4-IN-1 Related Classifications

HY-135954 Related Classifications