| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg | |||
| Other Sizes |
| Targets |
Multiple targets including NF-kappaB, MAPK, p300 Histone Acetyltransferase (HAT), Protein Kinase C (PKC), and Keap1-Nrf2 pathway. Curcumin D6 acts as an inhibitor of NF-kappaB activation and MAPK signaling, reducing pro-inflammatory cytokine production. It is also an inhibitor of p300 HAT, suppressing histone acetylation and gene transcription. Curcumin activates the Keap1-Nrf2 pathway, enhancing antioxidant response element (ARE)-mediated gene expression, and induces apoptosis in cancer cells by activating caspases.
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| ln Vitro |
Curcumin induces apoptosis in a variety of cancer cell lines in vitro, including breast, colon, pancreatic, and prostate cancer cells, with IC50 values typically ranging from 10-50 uM after 24-72 hours of treatment. It inhibits phorbol ester-induced protein kinase C (PKC) activity and reduces the production of pro-inflammatory cytokines (TNFalpha, IL-1beta, IL-6) in peripheral blood mononuclear cells (PBMCs) and alveolar macrophages. Curcumin also exhibits antioxidant properties by scavenging free radicals and upregulating Nrf2 target genes (e.g., HO-1, NQO1, GCLC).
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| ln Vivo |
In animal models, curcumin demonstrates anti-inflammatory and anti-tumor activity. In a mouse model of colitis (DSS-induced), oral curcumin (50-200 mg/kg) reduces disease activity index, colonic myeloperoxidase activity, and inflammatory cytokine levels (TNFalpha, IL-6). In xenograft models of human cancer (e.g., MDA-MB-231 breast cancer), intraperitoneal curcumin (50 mg/kg, 3-5 times weekly) inhibits tumor growth by 40-60%. Curcumin also reduces phorbol ester-induced skin tumor promotion in mice in a dose-dependent manner.
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| Enzyme Assay |
NF-kappaB activity can be assessed by EMSA or luciferase reporter assays: HEK-293T cells are transfected with an NF-kappaB luciferase reporter plasmid (3×kappaB-luc) plus Renilla. Cells are treated with curcumin D6 (1-50 uM) for 1 hour before stimulation with TNFalpha (10 ng/mL, 6 hours). Luciferase activity is measured using dual-luciferase assay. p300 HAT inhibition is measured using a fluorescent HAT activity assay: purified recombinant p300 (0.5-2 ug) is incubated with varying curcumin concentrations, 10 uM acetyl-CoA, and a biotinylated histone H3 peptide substrate (20 uM) for 60 minutes at 37degC. HAT activity is quantified by time-resolved fluorescence (excitation 320 nm, emission 405 nm). IC50 values are calculated.
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| Cell Assay |
RAW 264.7 macrophages or THP-1 monocytes are seeded in 96-well plates (2 × 10⁵ cells/well) in RPMI-1640 with 10% FBS. Cells are treated with curcumin D6 (0.1-50 uM) for 1-2 hours, then stimulated with LPS (1 ug/mL) for 6-24 hours. Supernatants are collected for cytokine quantification by ELISA (TNFalpha, IL-6, IL-1beta). Cell lysates are prepared for Western blotting to detect phosphorylated and total IkappaBalpha, p65, p38, JNK, and ERK1/2 (for MAPK analysis). For apoptosis assays, MCF-7 or MDA-MB-231 breast cancer cells are treated with curcumin D6 (10-100 uM) for 24-72 hours, and apoptosis is quantified by Annexin V-FITC/PI flow cytometry and caspase-3/9 activity assays.
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| Animal Protocol |
Female BALB/c nude mice (6-8 weeks old) bearing subcutaneous MDA-MB-231 or HCT-116 xenografts (tumor volume ~100 mm3) are randomized (n=8-10/group). Curcumin D6 is formulated in 5% DMSO + 40% PEG300 + 5% Tween 80 + 50% saline or in corn oil. Mice receive curcumin (50-200 mg/kg) or vehicle intraperitoneally or orally once daily for 14-28 days. Tumor volumes are measured by calipers twice weekly. At termination, tumors are excised, weighed, and processed for histology (H&E, Ki67 immunohistochemistry), Western blot (NF-kappaB, MAPK, cleaved caspase-3), and qPCR (inflammatory cytokines, Nrf2 target genes). Plasma is collected for curcumin quantification by LC-MS/MS.
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| ADME/Pharmacokinetics |
Curcumin D6 serves as an internal standard for bioanalytical LC-MS/MS quantification. Curcumin is poorly water-soluble (<1 ug/mL) and has very low oral bioavailability (<1% in humans) due to extensive first-pass glucuronidation and sulfation in the gut and liver. It is rapidly metabolized by UDP-glucuronosyltransferases (UGTs) and sulfotransferases (SULTs) to curcumin glucuronide and curcumin sulfate. The elimination half-life is short (1-2 hours in rodents). High doses (≥ 2 g/kg) are required to achieve therapeutic plasma concentrations in animals.
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| Toxicity/Toxicokinetics |
Curcumin is generally recognized as safe (GRAS) by the FDA. In clinical trials, oral curcumin (up to 12 g/day) is well tolerated, with minor gastrointestinal side effects (nausea, diarrhea, dyspepsia). High doses can cause yellow discoloration of stool. No organ toxicity or dose-limiting toxicity has been observed in Phase I clinical trials. In rodent studies, oral LD50 is > 5000 mg/kg. Intraperitoneal administration (200 mg/kg/day) for 14 days causes no significant mortality or body weight loss.
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| References |
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| Additional Infomation |
Curcumin has been used in traditional medicine for centuries and remains a popular dietary supplement for its anti-inflammatory and antioxidant properties. Despite its excellent safety profile, the clinical utility of curcumin is limited by its extremely poor bioavailability. Various formulation strategies (nanoparticles, liposomes, phytosomes, adjuvants like piperine) have been developed to improve oral absorption. The D6-labeled version is a research internal standard used for accurate quantification in biological samples. Curcumin has been investigated in hundreds of clinical trials for conditions including arthritis, metabolic syndrome, inflammatory bowel disease, and cancer prevention, but robust clinical efficacy remains to be established.
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| Molecular Formula |
C21H20O6
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| Molecular Weight |
368.3799
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| Exact Mass |
374.164
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| CAS # |
1246833-26-0
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| Related CAS # |
Curcumin;458-37-7
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| PubChem CID |
53464495
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
3.369
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
27
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| Complexity |
507
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(/C=C/C1C=CC(O)=C(OC([2H])([2H])[2H])C=1)CC(/C=C/C1C=CC(O)=C(OC([2H])([2H])[2H])C=1)=O
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| InChi Key |
VFLDPWHFBUODDF-BQWNYRPNSA-N
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| InChi Code |
InChI=1S/C21H20O6/c1-26-20-11-14(5-9-18(20)24)3-7-16(22)13-17(23)8-4-15-6-10-19(25)21(12-15)27-2/h3-12,24-25H,13H2,1-2H3/b7-3+,8-4+/i1D3,2D3
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| Chemical Name |
(1E,6E)-1,7-bis[4-hydroxy-3-(trideuteriomethoxy)phenyl]hepta-1,6-diene-3,5-dione
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7146 mL | 13.5729 mL | 27.1459 mL | |
| 5 mM | 0.5429 mL | 2.7146 mL | 5.4292 mL | |
| 10 mM | 0.2715 mL | 1.3573 mL | 2.7146 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.