Art. -Nr.: HY-179371

LIQ1

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LIQ1, a flavonoid derivative, is a potent Pyruvate kinase M2 (PKM2) allosteric inhibitor (IC₅₀ = 0.39 μM; K_d = 4.5 μM) targeting Arg43 within the polyarginine pocket. LIQ1 exhibits efficacy in a mouse model of LPS (HY-D1056)-induced endotoxemia, preventing the nuclear translocation of PKM2 and inhibiting its binding to HIF-1α, thereby suppressing IL-1β transcription. LIQ1 can be used for the research of endotoxemia^[1].

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Reinheit: 97.40%
CAS. Nr.: 2606032-80-6
Formel: C₁₆H₁₂O₅
Molecular Weight:284.26

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

LIQ1 Chemical Structure

CAS. Nr.: 2606032-80-6

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

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

PKM2

0.39 μM (IC₅₀)

PKM2

4.5 μM (Kd)

Alle Interleukin Related Isoform-spezifische Produkte anzeigen :

In Vitro

LIQ1 (100 μM; 2 h) significantly enhances the thermal stability of PKM2 within the tem-perature range of 40-52 °C, increasing its melting temperature (T_m) by 3.4 °C^[1].
LIQ1 significantly reduces the inhibitory effect on PKM2 R43A (IC₅₀ = 4.10 μM; K_d = 11.1 μM) compared to wild-type PKM2 (IC₅₀ = 0.98 μM; K_d = 3.2 μM), indicating that R43 is a critical residue mediating the allosteric inhibition of PKM2^[1].

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

In Vivo

LIQ1 (1, 2, and 5 mg/kg; i.p.; administered at 0, 12, 24, and 36 h after LPS injection) significantly improves survival and reduces inflammation and organ injury in LPS-induced endotoxemia in mice^[1].
LIQ1 (20 mg/kg; i.p.; single dose or daily for 14 days) shows negligible acute toxicity and no hepatorenal toxicity in mice, supporting its favorable safety profile^[1].

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

Animal Model:

Male BALB/c mice (6-8 weeks old) intraperitoneally injected with LPS (13 mg/kg)^[1]
Dosage:

1, 2, 5 mg/kg
Administration:

i.p.; administered at 0, 12, 24, and 36 h after LPS injection
Result:

Increased the 7-day survival rate from 40% (1 mg/kg) to 80% (5 mg/kg).
Exhibited a dose-dependent reduction in serum IL-1β levels.
Mitigated the injuries induced by LPS, such as microvilli loss, villus atrophy, deformation, and necrosis.
Alleviated the LPS-induced pathological lesions in the lung and heart tissues at the dose of 5 mg/kg.
Suppressed LPS-induced ATP accumulation.
Significantly inhibited the nuclear translocation of PKM2 in the small intestine, lung, and heart tissues.
Prevented PKM2-HIF-1α complex formation, ultimately leading to reduced IL-1β transcription in mice.

Animal Model:

Male BALB/c mice (6-8 weeks old)^[1]
Dosage:

20 mg/kg
Administration:

i.p.; single dose
Result:

Showed no significant decrease in body weight over 14 days.
Revealed no changes in motor activity, grooming and rubbing behaviors.

Animal Model:

Male BALB/c mice (6-8 weeks old)^[1]
Dosage:

20 mg/kg
Administration:

i.p.; daily for 14 days
Result:

Revealed a significant increase in alkaline phosphatase (ALP) levels.
Showed no statistically significant changes in other liver enzymes, including AST, ALT, GGT, total protein (TP), albumin (ALB), and globulin (GLO).
Showed no significant effects on kidney function parameters, including urea, creatinine (CREA), uric acid (UA), and estimated glomerular filtration rate (eGFR).

Chemical Information

CAS. Nr. 2606032-80-6
Appearance Solid
Molecular Weight 284.26
Formel C₁₆H₁₂O₅
Color White to off-white
SMILES

O=C(C1=CC=CC=C1C2CC(C3=CC=C(C=C3O2)O)=O)O
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 33.33 mg/mL (117.25 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

3.5179 mL

17.5895 mL

35.1791 mL

5 mM

0.7036 mL

3.5179 mL

7.0358 mL

10 mM

0.3518 mL

1.7590 mL

3.5179 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. 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)}

In Vivo:

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

Stock Solution Working Solution

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 (8.79 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (8.79 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

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

Solubility: ≥ 2.5 mg/mL (8.79 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:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 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]. Wang X, et al. Discovery of liquiritigenin derivatives as PKM2 allosteric inhibitors via targeting the polyarginine pocket. Bioorg Chem. 2025;167:109212. [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

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. 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	3.5179 mL	17.5895 mL	35.1791 mL	87.9477 mL
	5 mM	0.7036 mL	3.5179 mL	7.0358 mL	17.5895 mL
	10 mM	0.3518 mL	1.7590 mL	3.5179 mL	8.7948 mL
	15 mM	0.2345 mL	1.1726 mL	2.3453 mL	5.8632 mL
	20 mM	0.1759 mL	0.8795 mL	1.7590 mL	4.3974 mL
	25 mM	0.1407 mL	0.7036 mL	1.4072 mL	3.5179 mL
	30 mM	0.1173 mL	0.5863 mL	1.1726 mL	2.9316 mL
	40 mM	0.0879 mL	0.4397 mL	0.8795 mL	2.1987 mL
	50 mM	0.0704 mL	0.3518 mL	0.7036 mL	1.7590 mL
	60 mM	0.0586 mL	0.2932 mL	0.5863 mL	1.4658 mL
	80 mM	0.0440 mL	0.2199 mL	0.4397 mL	1.0993 mL
	100 mM	0.0352 mL	0.1759 mL	0.3518 mL	0.8795 mL

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LIQ1

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

Metabolism/Protease Compound Library

Differentiation Inducing Compound Library

Glycolysis Compound Library

Pyroptosis Compound Library

Anti-Cancer Metabolism Compound Library

Angiogenesis-Related Compound Library

Glucose Metabolism Compound Library

Antidepressant Compound Library

Anti-Prostate Cancer Compound Library

Pain-Related Compound Library

Metabolic Enzyme Compound Library

Autoimmune Disease Compound Library

Cytokine Inhibitors Library

Multi-Target Compound Library

Radioprotector Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Lactic Acid Metabolic Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

Alle Interleukin Related Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

LIQ1

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

Metabolism/Protease Compound Library

Differentiation Inducing Compound Library

Glycolysis Compound Library

Pyroptosis Compound Library

Anti-Cancer Metabolism Compound Library

Angiogenesis-Related Compound Library

Glucose Metabolism Compound Library

Antidepressant Compound Library

Anti-Prostate Cancer Compound Library

Pain-Related Compound Library

Metabolic Enzyme Compound Library

Autoimmune Disease Compound Library

Cytokine Inhibitors Library

Multi-Target Compound Library

Radioprotector Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Lactic Acid Metabolic Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

Alle Interleukin Related Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

LIQ1 Related Classifications

HY-179371 Related Classifications