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Demethylzeylasteral

Catalog No.GC38160 Copy One-Click Copy Product Info

Demethylzeylasteral is a triterpenoid compound derived from the traditional Chinese medicine Tripterygium wilfordii.

Products are for research use only. Not for human use. We do not sell to patients.

Demethylzeylasteral Chemical Structure

Cas No.: 107316-88-1

Size Price Stock Qty
10mM (in 1mL DMSO)
$37.00
In stock
1mg
$17.00
In stock
5mg
$35.00
In stock
10mg
$56.00
In stock
25mg
$112.00
In stock
50mg
$146.00
In stock
100mg
$191.00
In stock

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Sample solution is provided at 25 µL, 10mM.



Description of Demethylzeylasteral

Demethylzeylasteral is a triterpenoid compound derived from the traditional Chinese medicine Tripterygium wilfordii [1]. Demethylzeylasteral can inhibit T cell activation, inflammatory factor release, NF-κB and JAK/STAT signaling pathways, and induce tumor cell apoptosis and cell cycle arrest [2-3]. Demethylzeylasteral has significant immunosuppressive, anti-inflammatory and anti-tumor biological activities [4].

In MV3 and A375 cells, Demethylzeylasteral (1μM, 5μM, 10μM, 20μM; 48h) inhibits cell proliferation in melanoma cells [5]. In SW480 cells, Demethylzeylasteral (1μM, 5μM, 10μM, 20μM; 24h, 48h, 72h, 96h) inhibited the colorectal cell malignancy [6]. In MKN-45 cells, Demethylzeylasteral (50nM, 100nM, 500nM, 1µM, 5µM, 10µM, 30µM, 50µM, 100µM; 24h) has cytotoxic effects on human gastric cancer cells [7].

In DSS-induced colitis model, Demethylzeylasteral (5mg/kg, 10mg/kg, 20mg/kg; ip; 9d) exhibited a robust anti-inflammatory activity in vitro [8]. In MRL/lpr mice, treated with Demethylzeylasteral (0.6mg/10g, 1.2mg/10g; ig; 9d) showed a significant improvement in 24h proteinuria and the levels of anti-dsDNA antibody in serum [9]. In the rat kidney transplant model, treated with Demethylzeylasteral (10mg/kg, 20mg/kg; ip; 14d)significantly prolonged the survival of kidney-transplanted rats [10].

References:
[1]. Sun X, Shen B, Yu H, et al. Therapeutic potential of demethylzeylasteral, a triterpenoid of the genus Tripterygium wilfordii. Fitoterapia. 2022 Nov 1; 163: 105333.
[2]. Lv L, Zhou F, Quan Y, et al. Demethylzeylasteral exerts potent efficacy against non-small-cell lung cancer via the P53 signaling pathway. Translational Oncology. 2024 Aug 1; 46: 101989.
[3]. Pan L, Feng F, Wu J, et al. Demethylzeylasteral targets lactate by inhibiting histone lactylation to suppress the tumorigenicity of liver cancer stem cells. Pharmacological research. 2022 Jul 1; 181: 106270.
[4]. Li W, Han F, Tang K, et al. Inhibiting NF-κB-S100A11 signaling and targeting S100A11 for anticancer effects of demethylzeylasteral in human colon cancer. Biomedicine & Pharmacotherapy. 2023 Dec 1; 168: 115725.
[5]. Zhao Y, He J, Li J, et al. Demethylzeylasteral inhibits cell proliferation and induces apoptosis through suppressing MCL1 in melanoma cells. Cell death & disease. 2017 Oct; 8(10): e3133.
[6]. Yang Y, Han J, Ma Y, et al. Demethylzeylasteral inhibits cell proliferation and enhances cell chemosensitivity to 5-fluorouracil in Colorectal Cancer cells. Journal of Cancer. 2020 Aug 19; 11(20): 6059.
[7]. Yang Y, Zhao M, Hu T, et al. Identification of an antitumor effect of demethylzeylasteral on human gastric cancer cells. Oncology Letters. 2021 Jan; 21(1): 49.
[8]. Wen T, Liu T, Chen H, et al. Demethylzeylasteral alleviates inflammation and colitis via dual suppression of NF-κB and STAT3/5 by targeting IKKα/β and JAK2. International Immunopharmacology. 2024 Dec 5; 142: 113260.
[9]. Hu Q, Yang C, Wang Q, et al. Demethylzeylasteral (T-96) treatment ameliorates mice lupus nephritis accompanied by inhibiting activation of NF-κB pathway. PloS one. 2015 Jul 24; 10(7): e0133724.
[10]. Xu W, Lin Z, Yang C, et al. Immunosuppressive effects of demethylzeylasteral in a rat kidney transplantation model. International immunopharmacology. 2009 Jul 1; 9(7-8): 996-1001.

Protocol of Demethylzeylasteral

Cell experiment [1]:

Cell lines

MV3 and A375 cells

Preparation Method

Demethylzeylasteral was dissolved in DMSO as 40mM stock solution. Demethylzeylasteral was then used to treat melanoma cell lines, MV3 and A375 with different concentration (1μM, 5μM, 10μM, 20μM), DMSO was used as control.

Reaction Conditions

1μM, 5μM, 10μM, 20μM; 48h

Applications

Demethylzeylasteral inhibits cell proliferation in melanoma cells.
Animal experiment [2]:

Animal models

DSS-induced colitis model

Preparation Method

Based on body weight, mice were randomly divided into six groups, including control group, DSS group, DSS + SASP (Sulfasalazine, 50mg/kg, positive control) group, DSS + Demethylzeylasteral (5mg/kg, low dose) group, DSS + Demethylzeylasteral (10mg/kg, middle dose) group, DSS + Demethylzeylasteral (20mg/kg, high dose) group. Mice were injected intraperitoneally with Demethylzeylasteral, SASP, or vehicle (5% DMSO, 30% PEG400, and 65% normal saline) for 9 days. Then, mice were orally administered with 4% DSS solution to induce colitis at the 2th to 9th day of drug administration. During the experiment, loose and bloody stools as well as body weight of mice were daily recorded.

Dosage form

5mg/kg, 10mg/kg, 20mg/kg; ip; 9d

Applications

Demethylzeylasteral exhibited a robust anti-inflammatory activity in vitro.

References:
[1]. Zhao Y, He J, Li J, et al. Demethylzeylasteral inhibits cell proliferation and induces apoptosis through suppressing MCL1 in melanoma cells. Cell death & disease. 2017 Oct; 8(10): e3133.
[2]. Wen T, Liu T, Chen H, et al. Demethylzeylasteral alleviates inflammation and colitis via dual suppression of NF-κB and STAT3/5 by targeting IKKα/β and JAK2. International Immunopharmacology. 2024 Dec 5; 142: 113260.

Chemical Properties of Demethylzeylasteral

Cas No. 107316-88-1 SDF
Canonical SMILES C[C@](C1=CC2=O)(CC[C@]3(C)[C@@]4([H])C[C@@](C(O)=O)(C)CC3)[C@]4(CC[C@]1(C5=C2C(C=O)=C(O)C(O)=C5)C)C
Formula C29H36O6 M.Wt 480.59
Solubility DMSO: 250 mg/mL (520.19 mM) Storage Store at 2-8°C,protect from light
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of Demethylzeylasteral

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 2.0808 mL 10.4039 mL 20.8078 mL
5 mM 416.2 μL 2.0808 mL 4.1616 mL
10 mM 208.1 μL 1.0404 mL 2.0808 mL
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In vivo Formulation Calculator (Clear solution) of Demethylzeylasteral

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

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Average Rating: 5 ★★★★★ (Based on Reviews and 3 reference(s) in Google Scholar.)

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