2. PI3K/Akt/mTOR MAPK/ERK Pathway NF-κB
  3. PI3K Akt mTOR p38 MAPK NF-κB
  4. Calebin A

Calebin A is a PI3K/Akt/mTOR, MAPK, and NF-κB inhibitor with oral effectiveness. Calebin A can block the autophagy-repressive, inhibiting apoptosis. Calebin A has anti-tumor activity by epigenetic regulation. Calebin A suppresses adipogenesis, modulates thermogenesis, and enriches gut probiotics. Calebin A can be used in research on osteoarthritis, Alzheimer's disease, type 2 diabetes, malignant peripheral nerve sheath tumors, and colorectal cancer.

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

Calebin A

Calebin A Chemical Structure

CAS No. : 336784-82-8

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Calebin A Related Antibodies

Top Publications Citing Use of Products

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PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

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Akt Akt1 Akt2 Akt3

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mTOR mTORC1 mTORC2

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p38 MAPK Akt1 p38α p38β MAPK13 p38δ p38γ

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NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

  • Biological Activity

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Description

Calebin A is a PI3K/Akt/mTOR, MAPK, and NF-κB inhibitor with oral effectiveness. Calebin A can block the autophagy-repressive, inhibiting apoptosis. Calebin A has anti-tumor activity by epigenetic regulation. Calebin A suppresses adipogenesis, modulates thermogenesis, and enriches gut probiotics. Calebin A can be used in research on osteoarthritis, Alzheimer's disease, type 2 diabetes, malignant peripheral nerve sheath tumors, and colorectal cancer[1][2][3][4][5].

Cellular Effect
Cell Line Type Value Description References
IMR-32 ED50
1.4 μg/mL
Compound: 1
Evaluated for neuronal cell protectivity against beta-amyloid (25,35) insult towards IMR-32 human neuroblastoma cell
Evaluated for neuronal cell protectivity against beta-amyloid (25,35) insult towards IMR-32 human neuroblastoma cell
[PMID: 11549465]
PC-12 ED50
1 μg/mL
Compound: 1
Evaluated for neuronal cell protectivity against beta-amyloid (25,35) insult towards PC12 rat pheochromocytoma cell
Evaluated for neuronal cell protectivity against beta-amyloid (25,35) insult towards PC12 rat pheochromocytoma cell
[PMID: 11549465]
PC-12 ED50
1 μg/mL
Compound: 1, calebin-A
Protection against beta-amyloid (25 to 35) insult in rat PC12 cells assessed as viable cells after 24 hrs by MTT assay
Protection against beta-amyloid (25 to 35) insult in rat PC12 cells assessed as viable cells after 24 hrs by MTT assay
[PMID: 12350137]
PC-12 ED50
2 μg/mL
Compound: 1, calebin-A
Protection against beta-amyloid (1 to 42) insult in rat PC12 cells assessed as viable cells after 24 hrs by MTT assay
Protection against beta-amyloid (1 to 42) insult in rat PC12 cells assessed as viable cells after 24 hrs by MTT assay
[PMID: 12350137]
In Vitro

Calebin A (5 μM) suppresses apoptosis and promotes autophagic Beclin-1 expression in primary canine chondrocytes cultured in an osteoarthritis environment[1].
Calebin A (5 μM) upregulates ECM and autophagy markers, downregulates inflammation, degradation, apoptosis, and mTOR/PI3K/Akt signaling in primary canine chondrocytes cultured in an osteoarthritis environment, with effects dependent on intact autophagy[1].
Calebin A inhibits colonosphere formation, proliferation, invasion/migration, and enhances apoptosis in HCT116, RKO, and SW480 colorectal cancer cells via modulation of TNF-β/NF-κB signaling and associated biomarkers[2].
Calebin A overcomes vincristine resistance, induces G2/M-phase arrest and apoptosis in SGC7901 gastric cancer cells via modulation of MAPK signaling and P-glycoprotein[2].
Calebin A reduces growth and viability of Sup-T1 lymphoma cells and modulates epigenetic enzymes (HAT, HDAC, PCAF)[2].
Calebin A down-regulates inflammation in canine tenocytes via NF-κB/Scleraxis signaling[2].
Calebin A (20 μM) suppresses adipogenesis and induces lipolysis in adipocytes, with lipolysis induced at 20 μM[2].
Calebin A (25 μM; 24 h) induces G2/M phase decrease and G1 phase increase in STS26T, S462-TY, ST8814, and T265 MPNST cells, arresting cell cycle progression[3].
Calebin A (12.5-25 μM) downregulates phosphorylated AKT, phosphorylated ERK1/2, survivin, hTERT, and acetylated histone H3 in MPNST cells[3].

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

Calebin A Related Antibodies

Cell Proliferation Assay[3]

Cell Line: S462-TY, ST8814, T265, STS26T MPNST cell lines; LinNF primary neurofibroma cells
Concentration: 6.25, 12.5, 25, 50, 100 μM
Incubation Time: 24 h
Result: Decreased viability of MPNST cell lines at 12.5-25 μM; reduced survival by less than 50% in all MPNST cell lines with 25 μM treatment; inhibited growth of primary neurofibroma cells.

Cell Cycle Analysis[3]

Cell Line: STS26T, S462-TY, ST8814, T265 MPNST cell lines
Concentration: 25 μM
Incubation Time: 24 h
Result: Decreased STS26T cells in G2/M phase from 12.6% to 11.4% and increased G1 phase from 73.6% to 74.6%; reduced S462-TY G2/M phase from 19.7% to 8.8%, ST8814 G2/M phase from 6.4% to 6.0%, and T265 G2/M phase from 23.1% to 18.3%.

Cell Proliferation Assay[5]

Cell Line: HCT116 colorectal cancer cells (co-cultured with MRC-5 fibroblasts and Jurkat T-lymphocytes in multicellular proinflammatory TME; or co-cultured with MRC-5 fibroblasts and 10 ng/ml TNF-β in TNF-β-TME)
Concentration: 1-5 μM (10 days treatments); 5 μM (4 h immunofluorescence assay)
Incubation Time: 10 days (MTT, colonosphere, invasion, Western blotting); 4 h (immunofluorescence)
Result: Dose-dependently inhibited HCT116 cell proliferation, with maximum inhibition at 5 μM. Reduced colonosphere formation and invasion dose-dependently. Decreased nuclear p65-NF-κB labeling to 21% in multicellular TME and 22% in TNF-β-TME at 5 μM after 4 h treatment. Increased apoptosis to 59% in multicellular TME and 48% in TNF-β-TME at 5 μM after 4 h treatment. Suppressed p65-NF-κB phosphorylation, NF-κB-regulated gene products (MMP-9, CXCR4, Ki-67, β1-integrin), and cancer stem cell markers (CD133, CD44, ALDH1) dose-dependently. Increased cleaved caspase-3 dose-dependently.
Parmacokinetics
Species Dose Route T1/2 CLtotal CLrenal CLhepatic
Rat[6] 20 mg/kg i.v. 3.43 μg/mL 61 L/h/kg 0.11 L/h/kg 60.9 L/h/kg
Rat[6] 100 mg/kg p.o. 1.18 μg/mL 11244.3 L/h/kg 0.274 L/h/kg 11244.0 L/h/kg
In Vivo

Calebin A (100 mg/kg/d; p.o.; daily; 90 days) is safe when administered orally to female and male Wistar rats for 90 days, with no observed toxicity[2].
Calebin A (500 mg/kg; oral; single dose ) exhibits pharmacokinetic properties including ~0.5% bioavailability, 1-3 hour serum half-life, and primarily non-renal excretion in male Sprague-Dawley rats[2].
Calebin A (100 mg/kg; i.p.; three times a week; 15 days) significantly reduces xenograft tumor size in a mouse MPNST model[3].
Calebin A (0.1-0.5%; dietary supplementation; daily; 12 weeks) exhibits dose-dependent anti-obesity effects in high-fat diet-induced obese mice by reducing body weight and blood glucose, restoring liver weight, enhancing adaptive thermogenesis, and modulating gut microbiota composition[4].

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

Animal Model: Balb/c nude (male, 4 weeks old, MPNST xenograft model with S462-TY cells)[3]
Dosage: 100 mg/kg
Administration: i.p.; three times a week; 15 days
Result: Significantly decreased xenograft tumor size two weeks post-treatment.
Animal Model: C57BL/6 (male, 4 weeks old, high-fat diet-induced obesity)[4]
Dosage: 0.1%; 0.5%
Administration: high-fat diet (HFD) supplementation; daily; 12 weeks
Result: Reduced body weight in a dose-dependent manner; lowered fasting blood glucose and liver weight to normal diet levels (0.5% dose); decreased weights of white, beige, and brown adipose tissues (0.5% dose); improved liver color by reducing lipid accumulation (0.5% dose); better maintained rectal temperature with a higher area under the curve for temperature change than the high-fat diet group during 4°C cold exposure (0.5% dose); reduced Firmicutes-to-Bacteroidetes ratio from 1.24 ± 0.29 to 1.03 ± 0.42 (0.5% dose); increased Verrucomicrobia phylum abundance from 0.002 ± 0.001 to 0.022 ± 0.02 (0.5% dose); enriched genera including Akkermansia, Butyricicoccus, Ruminiclostridium_9, and unidentified_Ruminococcaceae (0.5% dose).
Molecular Weight

384.38

Formula

C21H20O7
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

COC(C=C1/C=C/C(OCC(/C=C/C2=CC(OC)=C(C=C2)O)=O)=O)=C(C=C1)O
Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (260.16 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6016 mL 13.0080 mL 26.0159 mL
5 mM 0.5203 mL 2.6016 mL 5.2032 mL
View the Complete Stock Solution Preparation Table

* 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 (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

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    90% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (6.50 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 98.00%

SDS (252 KB)

COA (244 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* 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 (sealed storage, away from moisture and light). 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 2.6016 mL 13.0080 mL 26.0159 mL 65.0398 mL
5 mM 0.5203 mL 2.6016 mL 5.2032 mL 13.0080 mL
10 mM 0.2602 mL 1.3008 mL 2.6016 mL 6.5040 mL
15 mM 0.1734 mL 0.8672 mL 1.7344 mL 4.3360 mL
20 mM 0.1301 mL 0.6504 mL 1.3008 mL 3.2520 mL
25 mM 0.1041 mL 0.5203 mL 1.0406 mL 2.6016 mL
30 mM 0.0867 mL 0.4336 mL 0.8672 mL 2.1680 mL
40 mM 0.0650 mL 0.3252 mL 0.6504 mL 1.6260 mL
50 mM 0.0520 mL 0.2602 mL 0.5203 mL 1.3008 mL
60 mM 0.0434 mL 0.2168 mL 0.4336 mL 1.0840 mL
80 mM 0.0325 mL 0.1626 mL 0.3252 mL 0.8130 mL
100 mM 0.0260 mL 0.1301 mL 0.2602 mL 0.6504 mL
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Calebin A Related Classifications

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:

Calebin A336784-82-8PI3KAktmTORp38 MAPKNF-κBPhosphoinositide 3-kinasePKBProtein kinase BMammalian target of RapamycinNuclear factor-κBNuclear factor-kappaBextracellular signal-regulated kinase (ERK)histone acetyltransferase (HAT)c-Jun N-terminal kinase (JNK)cyclooxygenase-2 (COX-2)MMP9Wistar ratsInhibitorinhibitorinhibit

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