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Art. -Nr.: HY-160461

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LTK-14A

LTK-14A, a derivative of Garcinol (HY-107569), is an orally effective selective inhibitor of histone butyrylation. LTK-14A selectively inhibits butyrylation without affecting acetylation by interacting with the C1438 residue in the catalytic domain of p300. LTK-14A significantly inhibits H4K5 butyrylation in vitro and downregulates the expression of adipogenic genes, thereby blocking adipogenesis. LTK-14A inhibits body weight gain and reduces body weight in obese mice. LTK-14A can be used in obesity-related research.

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CAS. Nr.: 71118-00-8
Formel: C₄₀H₅₄O₆
Molecular Weight:630.85

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (299 KB)

LTK-14A Chemical Structure

CAS. Nr.: 71118-00-8

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Use of MCE Products

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

Biologische Aktivität
- Beschreibung
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Alle HDAC Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	>20 μM Compound: 6b	Antiproliferative activity against human A549 cells after 72 hrs by MTT assay Antiproliferative activity against human A549 cells after 72 hrs by MTT assay	[PMID: 30500683]
HEL	IC₅₀	>20 μM Compound: 6b	Antiproliferative activity against HEL cells after 72 hrs by MTT assay Antiproliferative activity against HEL cells after 72 hrs by MTT assay	[PMID: 30500683]
HeLa	IC₅₀	19.68 μM Compound: 6b	Antiproliferative activity against human HeLa cells after 72 hrs by MTT assay Antiproliferative activity against human HeLa cells after 72 hrs by MTT assay	[PMID: 30500683]
K562	IC₅₀	>20 μM Compound: 6b	Antiproliferative activity against human K562 cells after 72 hrs by MTT assay Antiproliferative activity against human K562 cells after 72 hrs by MTT assay	[PMID: 30500683]
MCF7	IC₅₀	>20 μM Compound: 6b	Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay	[PMID: 30500683]

In Vitro

LTK-14A (10-25 μM) selectively inhibits p300-catalyzed histone butyrylation without affecting acetyltransferase activity in in vitro reconstitution assays, and this selective inhibitory effect depends on the Cys1438 residue^[1].
LTK-14A (25 μM; 6 days) is cell-permeable and exhibits metabolic stability in 3T3L1 preadipocytes^[1].
LTK-14A (25 μM; 2-6 days) shows no toxicity to 3T3L1 preadipocytes^[1].
LTK-14A (25 μM; 8 days) potently inhibits adipogenesis in 3T3L1 preadipocytes by suppressing the expression of pro-adipogenic genes and disrupting lipid metabolic pathways^[1].
LTK-14A (25 μM) specifically inhibits histone butyrylation in 3T3L1 preadipocytes (with particularly prominent effects on H3K23 and H4K5), without altering histone acetylation or other tested post-translational modifications^[1].
LTK-14A (10-1000 μg/plate) shows no mutagenicity towards Salmonella typhimurium strains TA97a, TA98, TA100 and TA102 at high concentrations, regardless of the presence of metabolic activation^[1].

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

Cell Viability Assay^[1]

Cell Line:

3T3L1 pre-adipocytes
Concentration:

25 μM
Incubation Time:

2, 4 and 6 days
Result:

Does not reduce cellular oxidoreductase activity (a marker of metabolic output and viability) at any tested time point compared to control cells.

Cell Differentiation Assay^[1]

Cell Line:

3T3L1 pre-adipocytes
Concentration:

25 μM
Incubation Time:

8 days total: 2 days in differentiation medium, then 6 days in maintenance medium with alternate-day treatment
Result:

Causes a significant reduction in Oil Red-O staining, indicating strong inhibition of adipocyte differentiation.
Downregulates 2200 genes and upregulates 1309 genes compared to controls, with a predominant effect on lipid metabolism pathways.
Confirms downregulation of pro-adipogenic genes including Pparg, Lep, Slc2a4, and Adipoq via Real Time qPCR.

In Vivo

LTK-14A (50 mg/kg; mixed with high-fat diet; ad libitum continuous intake; 16 weeks) alleviates high-fat diet-induced body weight gain, adipocyte hypertrophy and hepatic steatosis in male C57BL/6J mice by inhibiting H4K5 butyrylation without altering histone acetylation^[1].
LTK-14A (50 mg/kg; p.o.; daily; for 30 consecutive days) reduces body weight, fat content, and the expression of adipogenesis-promoting genes in genetically obese db/db mice by inhibiting H₄K5 butyrylation without altering histone acetylation levels^[1].

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

Animal Model:

C57BL/6J (male, 8 weeks old, high-fat diet-induced obesity model)^[1]
Dosage:

50 mg/kg
Administration:

mixed with high-fat diet; 16 weeks
Result:

Produced weight gain intermediate between normal chow and untreated high-fat diet-fed mice.
Reduced epididymal fat pad weight compared to untreated high-fat diet-fed mice.
Eliminated adipocyte hypertrophy and hepatic steatosis observed in untreated high-fat diet-fed mice.
Reduced H4K5 butyrylation in liver and epididymal fat pads compared to untreated high-fat diet-fed mice.
Left histone acetylation levels (H3K14, H3K18, H4K12) unchanged across groups.
Maintained food intake similar to untreated high-fat diet-fed mice.

Animal Model:

db/db (male, 8-10 weeks old, genetic obesity model); db+/- (male, 8-10 weeks old)^[1]
Dosage:

50 mg/kg
Administration:

i.g.; daily; 30 days
Result:

Arrested weight gain and reduced body weight in db/db mice by the end of the 30-day period.
Reduced liver and epididymal fat pad weights compared to vehicle-treated db/db mice.
Eliminated adipocyte hypertrophy and hepatocyte ballooning observed in vehicle-treated db/db mice.
Reduced H4K5 butyrylation in liver and epididymal fat pads compared to vehicle-treated db/db mice.
Left histone acetylation levels (H3K14, H3K18, H4K12) largely unchanged across groups.
Robustly inhibited expression of pro-adipogenic genes (Pparg, Lep, Slc2a4, Adipoq) in epididymal fat pads.

Chemical Information

CAS. Nr. 71118-00-8
Molecular Weight 630.85
Formel C₄₀H₅₄O₆
SMILES

O=C([C@]1(C(C)2C)C/C=C(C)\C)[C@@](C[C@H]2C/C=C(C)/C)(C[C@@H]3C/C=C(C)\C)C(OC(C)3C)=C(C1=O)C(C(C=C4)=CC(OC)=C4OC)=O
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (299 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]. Bhattacharya A, et al. Butyrylation Meets Adipogenesis-Probed by a p300-Catalyzed Acylation-Specific Small Molecule Inhibitor: Implication in Anti-obesity Therapy. Journal of medicinal chemistry. 2022 Sep 22;65(18):12273-12291. [Content Brief]

Calculators

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)}

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.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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