2. Acetylshikonin

Acetylshikonin is an oral active anti-cancer, anti-inflammatory, antioxidant, anti-fertility, antibacterial, and neuroprotective agent. Acetylshikonin is a inhibitor of acetylcholinase (AChE) (IC50=34.6 μM) and nonselective cytochrome P450. Acetylshikonin can induce Apoptosis and Autophagy in cancer cells. Acetylshikonin regulates blood glucose, liver fat metabolism, and renal fibrosis, and is used in the study of diabetes, diabetic nephropathy (DN), obesity, and nonalcoholic fatty liver disease (NAFLD).

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Acetylshikonin Chemical Structure

Acetylshikonin Chemical Structure

CAS No. : 24502-78-1

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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 108 In-stock
Solution
10 mM * 1 mL in DMSO USD 108 In-stock
Solid
5 mg USD 99 In-stock
10 mg USD 168 In-stock
25 mg USD 335 In-stock
50 mg USD 530 In-stock
100 mg USD 840 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Acetylshikonin:

Acetylshikonin Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Acetylshikonin

  • Biological Activity

  • Purity & Documentation

  • Customer Review

Description

Acetylshikonin is an oral active anti-cancer, anti-inflammatory, antioxidant, anti-fertility, antibacterial, and neuroprotective agent. Acetylshikonin is a inhibitor of acetylcholinase (AChE) (IC50=34.6 μM) and nonselective cytochrome P450. Acetylshikonin can induce Apoptosis and Autophagy in cancer cells. Acetylshikonin regulates blood glucose, liver fat metabolism, and renal fibrosis, and is used in the study of diabetes, diabetic nephropathy (DN), obesity, and nonalcoholic fatty liver disease (NAFLD)[1][2][3][4][5][6][7][8][9].

IC50 & Target

IC50: 1.4-4.0 μM (all P450s)[2]
IC50: 34.6 μM (AChE)[8].
In Vitro

Acetylshikonin(1.6-100 μM) inhibits the proliferation of oral cancer cells KB-R5 with IC50 40 μM[6].
Acetylshikonin (20-80 μM; 24 h) can induce Apoptosis and (20-80 μM) Autophagy of KB-R5 cells, and block mTOR/PI3K/AKT signaling pathway in KB-R5 cells[6].
Acetylshikonin (1-10 μM; 12 h) inhibits H2O2 (500 μM; 4 h) H2O2- (500 μM; 4 h ) induced Apoptosis of neuroblastoma SH-SY5Y and pc12 cells[8].
Acetylshikonin (0.01-5 μM/L; 2 h) has anti-CoxSackievirus A16 (CVA16) activity in the adsorption/invasion stage with EC50 was 0.04 μmol/L. However, has no effective in the pre-infection, replication and release stages[2].
Acetylshikonin (0.01-1 μM; 30 min) promotes glucose uptake by skeletal muscle cells L6 through PLC-β3/PKCδ mediation, thereby reducing blood glucose level[3].
Acetylshikonin (1-5 μg/mL; 48 h) inhibits TGF-β1 (5 ng/mL) induced renal fibrosis in HK2 cells[5].

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

Acetylshikonin Related Antibodies

Apoptosis Analysis[6]

Cell Line: KB-R5 (oral cancer cell line)
Concentration: 20 μM, 40 μM, 80 μM
Incubation Time: 24 h
Result: Changed the morphology of the nucleus.
Increased apoptosis ratio.

Western Blot Analysis[6]

Cell Line: KB-R5 (oral cancer cell line)
Concentration: 20 μM, 40 μM, 80 μM
Incubation Time:
Result: Increased the expression of Beclin-1 and LC3-II and inhibited the expression of p62. However, had no effect on the expression of LC3-I and Vps34.
Decreased the expression of p-mTOR, p-PI3K and p-AKT in a concentration-dependent manner.

Cell Viability Assay[2]

Cell Line: CVA16-induced human rhabdomyosarcoma (RD) cells
Concentration: 0.01-5 μM/L (1:1 mix with CVA16 strain TA271)
Incubation Time: 2 h
Result: Reduced CVA16-induced cytopathic effect with inhibition rates of 80% at the concentration of 0.08 μmol/L.

Western Blot Analysis[3]

Cell Line: L6 (rat skeletal muscle cells)
Concentration: 0.01 μM, 0.1 μM, 1 μM
Incubation Time: 2 h
Result: Significantly up-regulated phosphorylation of PKCδ.
Up-regulates the expression of glucose transporter 4 (GLUT4).and PLC-β3.
In Vivo

Acetylshikonin (50 mg/kg; Intraperitoneal injection; Three times per week for 6 weeks) significantly inhibited tumor growth in BALB/c nude mice in a concentration-dependent manner[6].
Acetylshikonin (270-1080 mg/kg; Intragastric administration; Once a day for 30 days) reduces D-galactose-induced (150 mg/kg) cognitive impairment and hippohippoal aging by reducing oxidative stress and neuroinflammation and inhibiting the activation of the p53/p21 signaling pathway in mice[1].
Acetylshikonin (2 mg/kg; Intramuscular injection; Single dose) inhibits Coxsackievirus A16 (CVA16) replication in mice[2].
Acetylshikonin (100 mg/kg; Intragastric administration; Once a day for eight weeks) inhibits renal fibrosis by inhibiting TGF-β1/Smad pathway without affecting blood glucose, thus reducing the damage of renal function in streptozotocin (STZ) -induced diabetic C57BL/6 mice[5].
Acetylshikonin (10 mk/kg; Intraperitoneal injection; Once a day for three days) reduces alloxouracil- (180 mg/kg; Intraperitoneal injection; Single dose) induced blood glucose level in diabetic mice[3].
Acetylshikonin (540 mg/kg; Oral administration; Once a day for eight weeks) reduces liver fat accumulation by regulating fat metabolism and liver inflammation in obese C57BL/6J mice, thereby improving obesity and nonalcoholic fatty liver disease (NAFLD)[4].
Acetylshikonin (120-1080 mg/kg; Intragastric administration;) doesn’t affect the ability of pregnancy in Sprague-Dawley rats at low doses (120 mg/kg and 360 mg/kg), but inhibits the ability of pregnancy in Sprague-Dawley rats at high doses (1080 mg/kg) by affecting the secretion of gonadotropin (GTH) and reducing the levels of serum follicle-stimulating hormone (FSH) and luteinizing hormone (LH)[7].

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

Animal Model: D-galactose (D-gal)-induced sub-acuteaging mouse model of Alzheimer’s disease (AD)[1]
Dosage: 270 mg/kg, 540 mg/kg, 1080 mg/kg
Administration: Intragastrical administration (i.g.); Once daily for 30 days. After D-gal treatment (150 mg/kg; Subcutaneous injection (s.c.); Once daily for 30 days)
Result: Decreased levels of the pro-inflammatory cytokines IL-1β and TNF-α.
Decreased the content of MDA and increased the activity of SOD.
Significantly mitigated D-Gal-induced downregulation of SIRT1 in hippocampal neurons.
Significantly inhibited the expression of p53, acetyl-p53, and p21 in mice (all proteins associated with hippocampal aging).
Animal Model: CAV16-indeced ICR suckling mice model[2]
Dosage: 2 mg/kg
Administration: Intramuscular injection (i.m.); Single dose. After CVA16 treatment (10[5.5] TCID50/g; Intramuscular injection (i.m.); Single dose )
Result: Delayed death of the mice (6 days post-infection and 7 dpi), and eventually resulted in a survival rate of 50% and 70% for the mice in the treatment and prevention groups, respectively (the death of the control mice began at 4 days after infection and all died at 6 days after infection).
Animal Model: Obese male C57BL/6J Mice model[4]
Dosage: 540 mg/kg
Administration: Oral gavage (P.O.); Once daily for 8 weeks
Result: Reduced body mass index (BMI) and food efficiency in obese mice by 17.1% and 48.2%, respectively.
Decreased plasma glucose, CHE, AST and ALT levels by 34.1%, 45.5% and 27.2%, respectively.
Significantly inhibited the levels of serum proinflammatory cytokines TNF-α, IL-6 and IL-1β by 49.1%, 41.1% and 45.6%, respectively.
Molecular Weight

330.33

Formula

C18H18O6
CAS No.
Appearance

Solid

Color

Brown to khaki

SMILES

O=C1C([C@H](OC(C)=O)C/C=C(C)\C)=CC(C2=C1C(O)=CC=C2O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (151.36 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 3.0273 mL 15.1364 mL 30.2728 mL
5 mM 0.6055 mL 3.0273 mL 6.0546 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 (protect from 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)

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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 (7.57 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    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:

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(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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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 (protect from 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: 99.39%

COA (259 KB) HNMR (231 KB) LCMS (87 KB)

Handling Instructions (2659 KB)

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 (protect from 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 3.0273 mL 15.1364 mL 30.2728 mL 75.6819 mL
5 mM 0.6055 mL 3.0273 mL 6.0546 mL 15.1364 mL
10 mM 0.3027 mL 1.5136 mL 3.0273 mL 7.5682 mL
15 mM 0.2018 mL 1.0091 mL 2.0182 mL 5.0455 mL
20 mM 0.1514 mL 0.7568 mL 1.5136 mL 3.7841 mL
25 mM 0.1211 mL 0.6055 mL 1.2109 mL 3.0273 mL
30 mM 0.1009 mL 0.5045 mL 1.0091 mL 2.5227 mL
40 mM 0.0757 mL 0.3784 mL 0.7568 mL 1.8920 mL
50 mM 0.0605 mL 0.3027 mL 0.6055 mL 1.5136 mL
60 mM 0.0505 mL 0.2523 mL 0.5045 mL 1.2614 mL
80 mM 0.0378 mL 0.1892 mL 0.3784 mL 0.9460 mL
100 mM 0.0303 mL 0.1514 mL 0.3027 mL 0.7568 mL
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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:

Acetylshikonin24502-78-1Inhibitorinhibitorinhibit

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