Cat. No.: HY-W082785A

L6H21

1 Cited Publications

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Based on 1 publication(s) in Google Scholar

L6H21, a Chalcone (HY-121054) derivative, is an orally active, potent and specific myeloid differentiation 2 (MD-2) inhibitor. L6H21 directly binds to MD-2 protein with a high affinity and low K_D value of 33.3 μM, blocking the formation of the LPS-TLR4/MD-2 complex. L6H21 inhibits LPS-induced expression of TNF-α and IL-6 in RAW264.7 macrophages, with IC₅₀ values of 6.58 and 8.59 μM, respectively. L6H21 can be used for alcoholic liver disease, metabolic disturbance and neuroinflammation research.

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

Purity: 99.19%
CAS No.: 24533-47-9
Formula: C₁₈H₁₈O₄
Molecular Weight:298.34

Storage:

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

L6H21 Chemical Structure

CAS No.: 24533-47-9

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Fluorescent Dye

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

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

Description

IC₅₀ & Target

IL-6

8.59 μM (IC₅₀)

TLR4

NF-κB

NLRP3 inflammasome

IL-1β

Caspase 3

Bcl-2

Bax

All TNF Receptor Isoforms :

All Interleukin Related Isoforms :

All Toll-like Receptor (TLR) Isoforms :

All NF-κB Isoforms :

All NOD-like Receptor (NLR) Isoforms :

All Caspase Isoforms :

All Bcl-2 Family Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
HT-29	IC₅₀	41.74 μM Compound: 27	Cytotoxicity against Homo sapiens (human) HT-29 cells after 72 hr by MTT assay Cytotoxicity against Homo sapiens (human) HT-29 cells after 72 hr by MTT assay	10.1007/s00044-011-9549-9
Peritoneal macrophage	IC₅₀	10 μM Compound: L6H21	Inhibition of LPS-induced IL-6 secretion in mouse primary peritoneal macrophages by ELISA Inhibition of LPS-induced IL-6 secretion in mouse primary peritoneal macrophages by ELISA	[PMID: 36399795]
Peritoneal macrophage	IC₅₀	10 μM Compound: L6H21	Inhibition of LPS-induced TNF-alpha secretion in mouse primary peritoneal macrophages by ELISA Inhibition of LPS-induced TNF-alpha secretion in mouse primary peritoneal macrophages by ELISA	[PMID: 36399795]
SGC-7901	IC₅₀	13.08 μM Compound: 27	Cytotoxicity against Homo sapiens (human) SGC7901 cells after 72 hr by MTT assay Cytotoxicity against Homo sapiens (human) SGC7901 cells after 72 hr by MTT assay	10.1007/s00044-011-9549-9

In Vitro

L6H21 (10 μM, 2 h) inhibits EtOH + LPS-induced apoptosis and mitochondrial damage in RAW264.7 cells^[1].
L6H21 (10 μM, 2 h) attenuates EtOH + LPS-induced ROS formation and TLR4-NF-κB activation, and decreases NLRP3 inflammasome activation^[1].

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

Apoptosis Analysis^[1]

Cell Line:

RAW264.7 cells (mouse macrophage cell line)
Concentration:

10 μM
Incubation Time:

2 hours
Result:

Markedly decreased apoptotic cell numbers; completely inhibited EtOH + LPS-induced increase in Bax/Bcl-2; markedly decreased EtOH + LPS-induced elevation in cleaved caspase-3 protein.

Western Blot Analysis^[1]

Cell Line:

RAW264.7 cells (mouse macrophage cell line)
Concentration:

10 μM
Incubation Time:

2 hours
Result:

Reduced EtOH + LPS-induced TLR4–NF-κB signaling; completely inhibited the increase in TLR4 and NF-κB p65 nuclear level induced by EtOH and LPS. Attenuated EtOH + LPS-induced expression of NLRP3 inflammasome; inhibited the elevated NLRP3 and IL-1β protein expression; decreased the expression of p20, an active form of caspase-1.

Cell Viability Assay^[1]

Cell Line:

RAW264.7 cells (mouse macrophage cell line)
Concentration:

10 and 20 μM
Incubation Time:

2 hours
Result:

The loss of cell viability by EtOH + LPS was prevented by L6H21 pretreatment. Slightly decreased cell viability a higher dose of 20 μM.

In Vivo

L6H21 (10 mg/kg, Oral gavage, daily) effectively inhibits EtOH + LPS-induced hepatic fat accumulation, hepatic steatosis and liver injury^[1].
L6H21 (0-40 mg/kg, Orally, daily for 4 weeks) attenuates metabolic disturbance, restores cognition and attenuates brain pathologies dose and time-dependently in HFD-fed rats, and shows neuroprotective effect in a model of prediabetes^[2].

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

Animal Model:

Male C57BL6 mice (8-10 weeks old, n = 36, 8 mice in each group, 25-30 g, with EtOH and LPS)^[1]
Dosage:

10 mg/kg
Administration:

Oral gavage, daily, before EtOH feeding
Result:

Decreased hepatic triglyceride (TG) concentration, markedly decreased serum alanine transaminase (ALT) and aspartate transaminase (AST) levels; Significantly decreased inflammation in liver tissue induced by EtOH + LPS.

Animal Model:

Male Wistar rats (6-7 weeks old, 250 g, a normal diet (ND) (n=8) or a high-fat diet (HFD) (n=104) for 16 weeks)^[2]
Dosage:

0, 10, 20, and 40 mg/kg
Administration:

Orally, daily for 1, 2 or 4 weeks
Result:

Ameliorated brain mitochondrial dysfunction in HFD-fed rats at 2-week administration time point; improved brain mitochondrial function in a dose-dependent manner for 4 weeks. Reduced hippocampal apoptosis in prediabetes for 4 weeks. Attenuated the reduction of dendritic spine volume and density for 4 weeks. Preserved microglial morphology in a dose-dependent manner.

Chemical Information

CAS No. 24533-47-9
Appearance Solid
Molecular Weight 298.34
Formula C₁₈H₁₈O₄
Color White to off-white
SMILES

O=C(C1=CC=C(OC)C=C1)/C=C/C2=CC=CC(OC)=C2OC
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

Publications (1)

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Journal Impact Factor

Int J Mol Sci

A Novel Hybrid Peptide VLP-Aβ Efficiently Regulates Immunity by Stimulating Myeloid Differentiation Protein and Activating the NF-κB Pathway. [Abstract]

2025 Jun 18;26(12):5834. PMID: 40565297

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (335.19 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

3.3519 mL

16.7594 mL

33.5188 mL

5 mM

0.6704 mL

3.3519 mL

6.7038 mL

10 mM

0.3352 mL

1.6759 mL

3.3519 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.

Molarity Calculator

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

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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 (8.38 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 2.5 mg/mL.

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% Corn Oil

Solubility: 2.5 mg/mL (8.38 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 2.5 mg/mL. 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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (281 KB)
SDS (458 KB)
- English - EN (458 KB)
- Français - FR (458 KB)
- Deutsch - DE (458 KB)
- Norwegian - NO (458 KB)
- Español - ES (458 KB)
- Swedish - SV (458 KB)
- Italian - IT (458 KB)
- Korean - KR (458 KB)
- Portuguese - PT (458 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)

References

[1]. Kong X, et al. Chalcone Derivative L6H21 Reduces EtOH + LPS-Induced Liver Injury Through Inhibition of NLRP3 Inflammasome Activation. Alcohol Clin Exp Res. 2019 Aug;43(8):1662-1671. [Content Brief]

[2]. Oo TT, et al. L6H21 protects against cognitive impairment and brain pathologies via toll-like receptor 4-myeloid differentiation factor 2 signalling in prediabetic rats. Br J Pharmacol. 2022 Mar;179(6):1220-1236. [Content Brief]

[3]. Yi Wang, et al. MD-2 as the target of a novel small molecule, L6H21, in the attenuation of LPS-induced inflammatory response and sepsis. Br J Pharmacol. 2015 Sep;172(17):4391-405. [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	3.3519 mL	16.7594 mL	33.5188 mL	83.7970 mL
	5 mM	0.6704 mL	3.3519 mL	6.7038 mL	16.7594 mL
	10 mM	0.3352 mL	1.6759 mL	3.3519 mL	8.3797 mL
	15 mM	0.2235 mL	1.1173 mL	2.2346 mL	5.5865 mL
	20 mM	0.1676 mL	0.8380 mL	1.6759 mL	4.1899 mL
	25 mM	0.1341 mL	0.6704 mL	1.3408 mL	3.3519 mL
	30 mM	0.1117 mL	0.5586 mL	1.1173 mL	2.7932 mL
	40 mM	0.0838 mL	0.4190 mL	0.8380 mL	2.0949 mL
	50 mM	0.0670 mL	0.3352 mL	0.6704 mL	1.6759 mL
	60 mM	0.0559 mL	0.2793 mL	0.5586 mL	1.3966 mL
	80 mM	0.0419 mL	0.2095 mL	0.4190 mL	1.0475 mL
	100 mM	0.0335 mL	0.1676 mL	0.3352 mL	0.8380 mL

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L6H21

Apoptosis Compound Library

Immunology/Inflammation Compound Library

Metabolism/Protease Compound Library

NF-κB Signaling Compound Library

Stem Cell Signaling Compound Library

Small Molecule Immuno-Oncology Compound Library

Anti-Aging Compound Library

Antioxidant Compound Library

Differentiation Inducing Compound Library

Anti-diabetic Compound Library

Oxygen Sensing Compound Library

Pyroptosis Compound Library

Orally Active Compound Library

Neuroprotective Compound Library

Anti-Breast Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Neurodegenerative Disease-related Compound Library

Anti-Obesity Compound Library

Angiogenesis-Related Compound Library

Mitochondria-Targeted Compound Library

Transcription Factor-Targeted Library

Anti-Liver Cancer Compound Library

Antidepressant Compound Library

Anti-Prostate Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Cancer Stem Cells Compound Library

Pain-Related Compound Library

Mitochondrial Protection Compound Library

Protease Inhibitor Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Autoimmune Disease Compound Library

Highly Selective Inhibitors Library

Cytokine Inhibitors Library

Cell Death Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Macrophage Related Compound Library

Multi-Target Compound Library

Radioprotector Library

Mitophagy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Fibrosis Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Pattern Recognition Receptors Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) L6H21

All TNF Receptor Isoforms

All Interleukin Related Isoforms

All Toll-like Receptor (TLR) Isoforms

All NF-κB Isoforms

All NOD-like Receptor (NLR) Isoforms

All Caspase Isoforms

All Bcl-2 Family Isoforms

Biological Activity

Chemical Information

Publications (1)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

L6H21 Related Classifications

Cat. No.: HY-W082785A