2. Metabolic Enzyme/Protease Immunology/Inflammation
  3. Pyruvate Kinase Interleukin Related
  4. LIQ1

LIQ1, a flavonoid derivative, is a potent Pyruvate kinase M2 (PKM2) allosteric inhibitor (IC50 = 0.39 μM; Kd = 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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LIQ1

LIQ1 Chemical Structure

CAS No. : 2606032-80-6

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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10 mM * 1 mL in DMSO In-stock
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LIQ1 Related Antibodies

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Description

LIQ1, a flavonoid derivative, is a potent Pyruvate kinase M2 (PKM2) allosteric inhibitor (IC50 = 0.39 μM; Kd = 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].

IC50 & Target[1]

PKM2

0.39 μM (IC50)

PKM2

4.5 μM (Kd)

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 (Tm) by 3.4 °C[1].
LIQ1 significantly reduces the inhibitory effect on PKM2 R43A (IC50 = 4.10 μM; Kd = 11.1 μM) compared to wild-type PKM2 (IC50 = 0.98 μM; Kd = 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.

LIQ1 Related Antibodies
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).
Molecular Weight

284.26

Formula

C16H12O5
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.5179 mL 17.5895 mL 35.1791 mL
5 mM 0.7036 mL 3.5179 mL 7.0358 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • 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

×
Volume (start)

V1

=
Concentration (final)

C2

×
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 (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.

    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% (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.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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).
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. 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 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:

LIQ12606032-80-6LIQ 1LIQ-1Pyruvate KinaseInterleukin RelatedILAllosteric inhibitorPyruvate kinase M2Polyarginine pocketInhibitorinhibitorinhibit

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