| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg | |||
| Other Sizes |
| Targets |
EZH2 0.55 μM (IC50) SIRT1
EZH2 (Histone Methyltransferase), Nrf2, and Sirtuin 1 (Sirt1). |
|---|---|
| ln Vitro |
Tanshindiol C (1–10 μM; for 24 hours) stimulates Prdx1 expression and mRNA levels in macrophages while activating Nrf2. Tanshindiol C inhibits the development of foam cells in macrophages caused by oxLDL by triggering the Prdx1/ABCA1 signaling pathway [1]. Tanshindiol C has a similar potency to that of EZH2 wild type (Ki value 176 nM) in inhibiting its activity [2]. With GI50 values of 1.5 μM and 9.5 μM, respectively, tanshindiol C suppresses the growth of Pfeiffer, U-2932 and Daudi (lymphoma), PC3 (prostate cancer), T98G and U87MG (glioma), and A549 (lung cancer) cell lines. 10.6, 4, 6, 5.7, 4.2, and 4 μM[2]. Pfeiffer cells accumulate in the sub-G1 phase when exposed to tanshindiol C (1–5 μM) for 72 hours, a sign that the cells had progressed to necrosis and apoptosis [2]. Important apoptosis-related protein indicators, such as cleaved caspase-3, caspase-7, and poly ADP-ribose polymerase (PRAP), have higher protein levels in cells when exposed to tanshindiol C (1-3 μM) over 72 hours. In cells, tanshindiol C dramatically lowers H3K27me3[2].
In macrophages, Tanshindiol C (1-10 microM) activates Nrf2 and upregulates Prdx1 expression. It protects macrophages from oxLDL-induced foam cell formation via Prdx1/ABCA1 signaling. It inhibits both wild-type and A667G mutant EZH2 activity with similar potencies (Ki value of 176 nM). It inhibits the growth of various cancer cell lines, including lymphoma (Pfeiffer, GI50=1.5 microM), prostate (PC3, GI50=6 microM), glioma (T986, GI50=5.7 microM), and lung cancer (A549, GI50=4.2 microM) cells. It induces accumulation of Pfeiffer cells in sub-G1 phase (1-5 microM; 72 hours), indicating late apoptosis and necrosis. It increases protein levels of cleaved caspase-3, caspase-7, and PARP. |
| ln Vivo |
Not available in the public domain. Its in vivo activity would typically be investigated in mouse models of cancer or atherosclerosis to evaluate its efficacy in inhibiting tumor growth or reducing atherosclerotic plaque formation.
|
| Enzyme Assay |
The inhibitory activity against EZH2 is measured using an in vitro methyltransferase assay. The enzyme is incubated with its substrate and S-adenosylmethionine in the presence of the compound, and the transfer of methyl groups is quantified. IC50 values are determined from dose-response curves.
|
| Cell Assay |
RT-PCR[1]
Cell Types: RAW264.7 cells Tested Concentrations: 1 μM, 3 μM, 10 μM Incubation Duration: 24 h Experimental Results: Upregulated the Nrf2 and Prdx1 mRNA levels. Western Blot Analysis[1] Cell Types: Mouse peritoneal macrophages Tested Concentrations: 1 μM, 3 μM, 10 μM Incubation Duration: 24 h Experimental Results: Activated Nrf2 and upregulated Prdx1 expression in macrophages. Cell Cycle Analysis[2] Cell Types: Pfeiffer cells Tested Concentrations: 1 μM, 2.5 μM and 5 μM Incubation Duration: 72 hrs (hours) Experimental Results: Induced accumulation of Pfeiffer cells in sub-G1 phase. Western Blot Analysis[2] Cell Types: Pfeiffer cells Tested Concentrations: 1 μM, 3 μM Incubation Duration: 72 hrs (hours) Experimental Results: The levels of H3K27me3 was Dramatically diminished in the cells. Cancer cell lines such as Pfeiffer, PC3, and A549 are treated with Tanshindiol C. Cell viability is assessed using assays like MTT or CellTiter-Glo to determine GI50 values. Apoptosis is evaluated by flow cytometry to measure sub-G1 phase accumulation and by Western blot for apoptosis markers like cleaved caspase-3. |
| ADME/Pharmacokinetics |
Physicochemical properties: Molecular Weight = 312.32, Molecular Formula = C18H16O5. Solubility: DMSO : 25 mg/mL (80.05 mM). Storage: 4degC, protect from light; in solvent -80degC for 6 months, -20degC for 1 month (protect from light).
|
| References |
|
| Additional Infomation |
Reports indicate that danshen and danshen contain tanshinone C, and relevant data is available for reference.
Tanshindiol C (CAS#: 97465-71-9) is a bioactive compound derived from the traditional Chinese medicine Danshen (Salvia miltiorrhiza). Its multiple targets and pathways make it a valuable tool for studying the molecular mechanisms of cancer and atherosclerosis. |
| Molecular Formula |
C18H16O5
|
|---|---|
| Molecular Weight |
312.32
|
| Exact Mass |
312.099
|
| CAS # |
97465-71-9
|
| PubChem CID |
126072
|
| Appearance |
Brown to red solid powder
|
| Density |
1.4±0.1 g/cm3
|
| Boiling Point |
561.5±50.0 °C at 760 mmHg
|
| Flash Point |
293.4±30.1 °C
|
| Vapour Pressure |
0.0±1.6 mmHg at 25°C
|
| Index of Refraction |
1.661
|
| LogP |
2.25
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
0
|
| Heavy Atom Count |
23
|
| Complexity |
546
|
| Defined Atom Stereocenter Count |
2
|
| SMILES |
CC1=COC2=C1C(=O)C(=O)C3=C2C=CC4=C3CC[C@H]([C@]4(C)O)O
|
| InChi Key |
RTKDBIDPGKCZJS-KZULUSFZSA-N
|
| InChi Code |
InChI=1S/C18H16O5/c1-8-7-23-17-10-3-5-11-9(4-6-12(19)18(11,2)22)14(10)16(21)15(20)13(8)17/h3,5,7,12,19,22H,4,6H2,1-2H3/t12-,18-/m1/s1
|
| Chemical Name |
(6R,7R)-6,7-dihydroxy-1,6-dimethyl-8,9-dihydro-7H-naphtho[1,2-g][1]benzofuran-10,11-dione
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| 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
|
|---|---|
| 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 | 3.2018 mL | 16.0092 mL | 32.0184 mL | |
| 5 mM | 0.6404 mL | 3.2018 mL | 6.4037 mL | |
| 10 mM | 0.3202 mL | 1.6009 mL | 3.2018 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.
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