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

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Based on 1 publication(s) in Google Scholar

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.
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

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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LIQ1 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
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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