Demethylzeylasteral (T-96)

Catalog No.S3608 Batch:S360802

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Technical Data

Formula

C29H36O6
Molecular Weight 480.59 CAS No. 107316-88-1
Solubility (25°C)* In vitro DMSO 96 mg/mL (199.75 mM)
Ethanol 16 mg/mL (33.29 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description Demethylzeylasteral (T-96), the active component isolated from Tripterygium wilfordii Hook F., inhibits UDP-glucuronosyltransferase (UGT) isoforms UGT1A6 and UGT2B7 with immunosuppressive effects.
Targets
UGT1A6 [1]
(Cell-free assay)		 UGT2B7 [1]
(Cell-free assay)
0.6 μM(Ki) 17.3 μM(Ki)
In vitro Demethylzeylasteral shows strong inhibition towards UGT1A6 and UGT2B7, with negligible influence towards UGT1A9[1]. Demethylzeylasteral has an anti-tumor property in melanoma cells. Demethylzeylasteral not only inhibits cell proliferation through cell cycle arrest at S phase, but also induces cell apoptosis in melanoma cells. CDK2 and Cycin E1 decrease in a dose-dependent manner after Demethylzeylasteral treatment. Demethylzeylasteral inhibits MCL1, whose overexpression recovers the proliferation ability inhibited by demethylzeylasteral. Demethylzeylasteral inhibits clonogenicity and tumorigenesis in melanoma cells through downregulating the expression of MCL1. Demethylzeylasteral is found to inhibit Ca2+ currents in mouse spermatogonia and has an antifertility ability[2].
In vivo T-96 demonstrates a significant proteinuria reduction both in a time and concentration-dependent manner. T-96 significantly inhibits the activation of NF-kB in the kidneys of MRL/lpr mice. In addition, T-96 reduces the secretion of pro-inflammatory mediators such as TNF-α, COX-2 and ICAM-1[3].

Protocol (from reference)

Cell Assay:

[2]
  • Cell lines

    melanoma cell lines, MV3 and A375

  • Concentrations

    1, 5, 10 and 20 μM

  • Incubation Time

    48 h

  • Method

    Melanoma cell lines, MV3 and A375, are treated with different concentrations of demethylzeylasteral (1, 5, 10 and 20 μM, dimethyl sulfoxide (DMSO) is used as control) for 48 h.
Animal Study:

[3]
  • Animal Models

    C57BL/6 mice

  • Dosages

    1.2 and 0.6 mg/10g

  • Administration

    by gavage

Selleck's Demethylzeylasteral (T-96) has been cited by 2 publications

Demethylzelasteral inhibits proliferation and EMT via repressing Wnt/β-catenin signaling in esophageal squamous cell carcinoma [ J Cancer, 2021, 12(13):3967-3975] PubMed: 34093803
T-96 attenuates inflammation by inhibiting NF-κB in adjuvant-induced arthritis. [ Front Biosci (Landmark Ed), 2020, 25:498-512] PubMed: 31585899

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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