Art. -Nr.: HY-120215

KT203

Name: KT203
Brand: MedChemExpress
SKU: HY-120215
Price: 100.00 USD
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KT203 is a selective ABHD6 inhibitor. KT203 is peripherally restricted and cannot cross the blood-brain barrier, producing near-complete inhibition of hepatic ABHD6 while brain ABHD6 remains essentially unaffected. KT203 reduces cellular MAG hydrolase activity and blocks the hydrolysis of the endocannabinoid arachidonoylglycerol. KT203 inhibits pro-inflammatory cytokine expression, induces anti-inflammatory interleukin signaling and lipid metabolism gene expression, increases 2-MAG and DHA (HY-B2167)-containing lipid mediators, and reduces circulating TNF-α in LPS-exposed mice. KT203 inhibits PRRSV replication. KT203 can be used for research on NSCLC, obesity-related chronic inflammation, endotoxemia, and porcine reproductive and respiratory syndrome.

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Reinheit : 99.64%
CAS. Nr.: 1402612-64-9
Formel: C₂₈H₂₆N₄O₃
Molecular Weight:466.53

Speicherung:

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

KT203 Chemical Structure

CAS. Nr.: 1402612-64-9

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

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

Biologische Aktivität

Beschreibung

IC₅₀ & Target

IC50: 0.31 nM (ABHD6 in Neuro2A cells)^[1].

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Cellular Effect

Cell Line	Type	Value	Description	References
N2a	IC50	0.31 nM	In situ inhibition of ABHD6 in Neuro2A cells assessed by gel-based competitive ABPP after 4 hrs exposure with KT203. In situ inhibition of ABHD6 in Neuro2A cells assessed by gel-based competitive ABPP after 4 hrs exposure with KT203.	24152295
PAM	CC₅₀	14.06 μM	Cytotoxicity against porcine alveolar macrophages (PAMs) assessed as viability reduction incubated 24 hrs by CCK-8 assay. Cytotoxicity against porcine alveolar macrophages (PAMs) assessed as viability reduction incubated 24 hrs by CCK-8 assay.	40619342

In Vitro

Anti-cancerGlutamate Release or ReceptorsMitochondrial FunctionInnate ImmunityCarbohydrate MetabolismCytokines & ChemokinesLipid MetabolismLipid Inflammatory MediatorsViral InfectionOthers

Anti-cancer

KT203 (10 nM; 8 h) reduces the migration and invasion capacity of NSCLC cell lines without consistent antiproliferative effects^[1].

Glutamate Release or Receptors

Mitochondrial Function

KT203 does not attenuate NMDA-induced mitochondrial calcium overload in primary rat cortical neurons^[6].

Innate Immunity

Carbohydrate Metabolism

KT203 (10 µM) does not alter lactate release from MMe-polarized RAW264.7 macrophages^[4].

Innate Immunity

Cytokines & Chemokines

KT203 (10 µM) reduces the release of TNFα and MCP1 from MMe-polarized RAW264.7 macrophages^[4].

Innate Immunity

Cytokines & Chemokines

Lipid Metabolism

KT203 (10 µM) upregulates Plin2, Fabp4, Cd36, and Cpt1a and downregulates Tnfa and Mcp1 in MMe-polarized RAW264.7 macrophages, without significantly altering Cd11c^[4].
KT203 (10 µM) increases the expression of PLIN2, PPARA, and PPARG and decreases TNFA in MMe-polarized THP1 macrophages^[4].

Innate Immunity

Lipid Metabolism

KT203 (10 µM) increases the levels of 2-MAG species C16:0, C18:0, and C18:1 as well as total MAG C16:0 in MMe-polarized RAW264.7 macrophages^[4].
KT203 (10 μM; 24 h) reduces glycerol release in RAW 264.7 macrophages and moderately reduces glycerol release in THP-1 macrophages^[7].

Lipid Inflammatory Mediators

KT203 is a potent in vitro ABHD6 inhibitor in mouse brain and Neuro2A membrane proteomes (IC₅₀ 0.82 nM)^[5].
KT203 (3 nM; 4 h) blocks >90% of ABHD6 activity in Neuro2A cells and shows no significant cross-reactivity with approximately 50 other serine hydrolases^[5].

Lipid Metabolism

KT203 (10 nM) strongly inhibits MAG hydrolase activity in SPC-A-1 and A549 NSCLC cell extracts, reducing C16:0 MAG hydrolysis by 96.1% and 94.3%, and C18:1 MAG hydrolysis by 77.4% and 81.0%, respectively^[1].

Viral Infection

KT203 (24 h post-infection) dose-dependently reduces PRRSV N protein in CH-1a-infected Marc145 cells^[8].

Others

KT203 (30 min) inactivates ABHD6 in the proteome of primary rat cortical neurons^[6].
KT203 (0-200 µM; 24 h) has a CC₅₀ of 103.1 µM in Marc145 cells^[8].
KT203 (0-100 µM; 24 h) has a CC₅₀ of 14.06 µM in PAM^[8].
KT203 inhibits ABHD6 in cells with an IC₅₀ of 0.8 nM^[9].

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

Cell Cytotoxicity Assay^[8]

Cell Line:

Marc145 cells
Concentration:

0 to 200 µM
Incubation Time:

24 h
Result:

CC₅₀ was 103.1 µM in Marc145 cells.

Western Blot Analysis^[8]

Cell Line:

Marc145 cells
Concentration:

Various concentrations
Incubation Time:

24 h after infection
Result:

Significantly reduced PRRSV N protein expression compared with DMSO at all tested concentrations.

In Vivo

Innate ImmunityAdaptive ImmunityCytokines & ChemokinesImmune Tolerance & ImmunosuppressionOthers

Innate Immunity

Adaptive Immunity

Cytokines & Chemokines

Immune Tolerance & Immunosuppression

KT203 (2 mg/kg; i.p.; once daily; from the day after MOG injection through 30 days post-immunization) does not improve neurological disability or inflammation in EAE mice despite peripheral and chronic CNS ABHD6 inhibition^[6].

Innate Immunity

Cytokines & Chemokines

KT203 (1 mg/kg; i.p.; single dose 1 h after LPS; 24 h follow-up) reduces circulating TNF-α in LPS-challenged WT mice, indicating in vivo anti-inflammatory efficacy^[7].

Others

KT203 (0.1-1 mg/kg; i.p.; single dose; 4 hr) is a potent peripherally restricted ABHD6 inhibitor in vivo, producing near-complete liver ABHD6 inhibition at 1 mg/kg i.p. while showing negligible brain ABHD6 inhibition^[5].
KT203 (single injection) does not engage brain ABHD6 in healthy mice^[6].

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

Animal Model:

C57BL/6^[5]
Dosage:

0.1-1 mg/kg
Administration:

i.p.; single dose; 4 hr
Result:

In liver, near-complete ABHD6 blockade was produced at 1 mg/kg and approximately 80% ABHD6 inhibition was maintained at lower doses.
In brain, negligible ABHD6 inhibition occurred at all doses tested.
Good selectivity was shown in brain and liver, with no observed CES1 inhibition.

Animal Model:

C57BL/6 (female, 10 weeks old)^[6]
Dosage:

2 mg/kg
Administration:

i.p.; once daily; from the day after MOG injection through 30 days post-immunization
Result:

Did not modulate the course of EAE disease progression.
At 30 days post-immunization, neurological disability was comparable to vehicle.
Did not attenuate the corticospinal tract conduction latency deficit.
Did not reduce spinal cord lesion number or CD11b+ microglia/macrophage density, and inflammatory marker mRNA levels (Iba1, COX-2, TNFα, IL1β) in spinal cord, striatum, and hippocampus were similar to vehicle.
After chronic EAE, completely inactivated brain ABHD6 at 30 days post-immunization, although activity was restricted to the periphery during immunization and the early acute phase.
Did not reduce cannabinoid agonist-stimulated [35S]GTPγS binding in striatum or cerebellum.
No significant CB1 receptor downregulation was observed.

Animal Model:

C57BL/6N (male, 12-16 weeks)^[7]
Dosage:

1 mg/kg
Administration:

i.p.; single dose; one hour after LPS; 24 h follow-up
Result:

Circulating TNF-α was lowered in LPS-challenged WT mice compared with vehicle-treated controls.
Plasma TNF-α reduction was observed within one hour of administration.

Related Protocols :

Chemical Information

CAS. Nr. 1402612-64-9
Appearance Solid
Molecular Weight 466.53
Formel C₂₈H₂₆N₄O₃
Color White to yellow
SMILES

O=C(N1C(CCCC1)CC2=CC=CC=C2)N3N=NC(C4=CC=C(C=C4)C5=CC=CC(C(O)=O)=C5)=C3
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 : 100 mg/mL (214.35 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

2.1435 mL

10.7174 mL

21.4348 mL

5 mM

0.4287 mL

2.1435 mL

4.2870 mL

10 mM

0.2143 mL

1.0717 mL

2.1435 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 (5.36 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% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.36 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 (286 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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]. Tang Z, et al. Enhanced monoacylglycerol lipolysis by ABHD6 promotes NSCLC pathogenesis. EBioMedicine. 2020 Mar;53:102696. [Content Brief]

[2]. Orabi D, et al. The lipid hydrolase ABHD6 is a therapeutic target in metabolic dysfunction-associated steatotic liver disease (MASLD)-related hepatocellular carcinoma. bioRxiv. 2025 Aug 2:2025-07.

[3]. Healey RD, et al. Discovery and mechanism of action of small molecule inhibitors of ceramidases. Angewandte Chemie International Edition. 2022 Jan 10;61(2):e202109967. [Content Brief]

[4]. Poursharifi P, et al. ABHD6 suppression promotes anti-inflammatory polarization of adipose tissue macrophages via 2-monoacylglycerol/PPAR signaling in obese mice. Molecular metabolism. 2023 Dec;78:101822.

[5]. Hsu KL, et al. Discovery and optimization of piperidyl-1,2,3-triazole ureas as potent, selective, and in vivo-active inhibitors of α/β-hydrolase domain containing 6 (ABHD6). Journal of medicinal chemistry. 2013 Nov 14;56(21):8270-9. [Content Brief]

[6]. Manterola A, et al. Re-examining the potential of targeting ABHD6 in multiple sclerosis: Efficacy of systemic and peripherally restricted inhibitors in experimental autoimmune encephalomyelitis. Neuropharmacology. 2018 Oct 1;141:181-91. [Content Brief]

[7]. Poursharifi P, et al. ABHD6 suppression attenuates pro-inflammatory responses in mice and promotes anti-inflammatory polarization of macrophages during endotoxin stress. Biochimica et Biophysica Acta (BBA)-Molecular and Cell Biology of Lipids. 2025 Oct 6:159694.

[8]. He Z, et al. Identification of compounds targeting porcine reproductive and respiratory syndrome virus nsp3 and evaluation of their antiviral efficacy. Virulence. 2025 Dec 31;16(1):2530176. [Content Brief]

[9]. Maramai S, et al. Targeting Endocannabinoid Metabolism: an Arrow with Multiple Tips Against Multiple Sclerosis. ChemMedChem. 2020 Nov 04;15(21):1985-2003.

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	2.1435 mL	10.7174 mL	21.4348 mL	53.5871 mL
	5 mM	0.4287 mL	2.1435 mL	4.2870 mL	10.7174 mL
	10 mM	0.2143 mL	1.0717 mL	2.1435 mL	5.3587 mL
	15 mM	0.1429 mL	0.7145 mL	1.4290 mL	3.5725 mL
	20 mM	0.1072 mL	0.5359 mL	1.0717 mL	2.6794 mL
	25 mM	0.0857 mL	0.4287 mL	0.8574 mL	2.1435 mL
	30 mM	0.0714 mL	0.3572 mL	0.7145 mL	1.7862 mL
	40 mM	0.0536 mL	0.2679 mL	0.5359 mL	1.3397 mL
	50 mM	0.0429 mL	0.2143 mL	0.4287 mL	1.0717 mL
	60 mM	0.0357 mL	0.1786 mL	0.3572 mL	0.8931 mL
	80 mM	0.0268 mL	0.1340 mL	0.2679 mL	0.6698 mL
	100 mM	0.0214 mL	0.1072 mL	0.2143 mL	0.5359 mL

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KT203

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