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.
For research use only. We do not sell to patients.
- CAS No.: 71118-00-8
- Formula: C40H54O6
- Molecular Weight:630.85
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
>20 μM
Compound: 6b
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Antiproliferative activity against human A549 cells after 72 hrs by MTT assay
Antiproliferative activity against human A549 cells after 72 hrs by MTT assay
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[PMID: 30500683] |
| HEL | IC50 |
>20 μM
Compound: 6b
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Antiproliferative activity against HEL cells after 72 hrs by MTT assay
Antiproliferative activity against HEL cells after 72 hrs by MTT assay
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[PMID: 30500683] |
| HeLa | IC50 |
19.68 μM
Compound: 6b
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Antiproliferative activity against human HeLa cells after 72 hrs by MTT assay
Antiproliferative activity against human HeLa cells after 72 hrs by MTT assay
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[PMID: 30500683] |
| K562 | IC50 |
>20 μM
Compound: 6b
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Antiproliferative activity against human K562 cells after 72 hrs by MTT assay
Antiproliferative activity against human K562 cells after 72 hrs by MTT assay
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[PMID: 30500683] |
| MCF7 | IC50 |
>20 μM
Compound: 6b
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Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay
Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay
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[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.
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Cell Line:3T3L1 pre-adipocytes
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Concentration:25 μM
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Incubation Time:2, 4 and 6 days
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Result:Does not reduce cellular oxidoreductase activity (a marker of metabolic output and viability) at any tested time point compared to control cells.
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Cell Line:3T3L1 pre-adipocytes
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Concentration:25 μM
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Incubation Time:8 days total: 2 days in differentiation medium, then 6 days in maintenance medium with alternate-day treatment
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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; 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.
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Animal Model:C57BL/6J (male, 8 weeks old, high-fat diet-induced obesity model)[1]
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Dosage:50 mg/kg
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Administration:mixed with high-fat diet; 16 weeks
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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.
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Animal Model:db/db (male, 8-10 weeks old, genetic obesity model); db+/- (male, 8-10 weeks old)[1]
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Dosage:50 mg/kg
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Administration:i.g.; daily; 30 days
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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
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CAS No. 71118-00-8
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Molecular Weight 630.85
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Formula C40H54O6
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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
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
LTK-14A Related Classifications
HY-160461 Related Classifications
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