| Size | Price | |
|---|---|---|
| 100mg | ||
| 250mg | ||
| 500mg | ||
| Other Sizes |
| Targets |
Apoptosis, Autophagy[2]
|
|---|---|
| ln Vitro |
Isoangustone A (10 and 20 μM; 48 and 72 h) promotes cell cycle arrest in the G1 phase and decreases the proliferation of SK-MEL-28 cells [1]. Via the Akt/GSK3β and MKK4/MKK7/JNKs signaling pathways, isoangustone A (10 and 20 μM; 48 h) promotes the reduction in the amount of G1 phase-related proteins [1]. Through ATP competition, isoangustone A directly binds to and inhibits the kinase activities of PI3-K, MKK4, and MKK7 [1]. By triggering AMPK signaling, isoangustone A (20 μM; 0.5–4 h) stimulates autophagy in colorectal cancer cells [2]. [2] Isoangustone A (1–20 μM; 0-100 min) decreases the respiration of mitochondria. In SW480 cells, isoangustone A (15 μM; 6 h) causes apoptosis [2]. In human renal mesangial cells, isoangustone A (1–20 μM; 3 days) reduces fibrosis and inflammation [3].
|
| ln Vivo |
The tumor development, volume, and weight of mice SK-MEL-28 xenografts are greatly reduced by isoangustone A (2 or 10 mg/kg; ip; daily for 35 days) [1].
|
| Cell Assay |
Cell Proliferation Assay[1]
Cell Types: SK-MEL-28 Tested Concentrations: 10 and 20 μM Incubation Duration: 48 and 72 h Experimental Results: Inhibited proliferation in a dose- and time-dependent manner. Cell Cycle Analysis[1] Cell Types: SK-MEL-28 Tested Concentrations: 10 and 20 μM Incubation Duration: 48 h Experimental Results: Caused cell cycle arrest at G1 phase. Western Blot Analysis[1] Cell Types: SK-MEL-28 Tested Concentrations: 10 and 20 μM Incubation Duration: 48 h Experimental Results: Inhibited the expression of cyclin D1 and cyclin E. Suppressed phosphorylation of Rb in a dose-dependent manner. Inhibited the phosphorylation of Akt (Ser473, Thr308) and GSK3β (Ser9). Suppressed the phosphorylation of JNK1/2, but had no effect on ERK1/2 or p38. Cell Autophagy Assay[2] Cell Types: SW480 cells Tested Concentrations: 20 μM Incubation Duration: 0.5, 2 and 4 h Experimental Results: Deformed mitochondria, nondegradable cellular debris were all observable together with autophagic vacuoles in cells after 4 h. Apoptosis Analysis[2] Cell Types: SW480 cells Tested Concentrations: 15 μM Incubation Duration: |
| Animal Protocol |
Animal/Disease Models: Male Balb/c nu/nu (nude) mice, SK-MEL-28 xenograft model[1]
Doses: 2 or 10 mg/kg Route of Administration: intraperitoneal (ip)injection, daily for 35 days Experimental Results: Dramatically suppressed tumor weight compared to the control group. Markedly inhibited the expression of proliferating cell nuclear antigen (PCNA). diminished phosphorylation levels of Akt. |
| References |
[1]. Song NR, et al. Isoangustone A, a novel licorice compound, inhibits cell proliferation by targeting PI3K, MKK4, and MKK7 in human melanoma. Cancer Prev Res (Phila). 2013 Dec;6(12):1293-303.
[2]. Tang S, et al. Isoangustone A induces autophagic cell death in colorectal cancer cells by activating AMPK signaling. Fitoterapia. 2021 Jul;152:104935. [3]. Li J, et al. Isoangustone A suppresses mesangial fibrosis and inflammation in human renal mesangial cells. Exp Biol Med (Maywood). 2011 Apr 1;236(4):435-44. |
| Molecular Formula |
C25H26O6
|
|---|---|
| Molecular Weight |
422.47
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| CAS # |
129280-34-8
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| Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
|
| SMILES |
C/C(=C/CC1=C(O)C=C(O)C=C1C1=CC(=O)C2=C(C=C(C(C/C=C(\C)/C)=C2O1)O)O)/C
|
| 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)
|
| 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 | 2.3670 mL | 11.8352 mL | 23.6703 mL | |
| 5 mM | 0.4734 mL | 2.3670 mL | 4.7341 mL | |
| 10 mM | 0.2367 mL | 1.1835 mL | 2.3670 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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