Demethylzeylasteral (T-96)

Catalog No.S3608

Demethylzeylasteral (T-96) Chemical Structure

Molecular Weight(MW): 480.59

Demethylzeylasteral (T-96), the active component isolated from Tripterygium wilfordii Hook F., inhibits UDP-glucuronosyltransferase (UGT) isoforms UGT1A6 and UGT2B7 with immunosuppressive effects.

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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]
()
UGT2B7 [1]
()
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

Cell Research:

[2]

+ Expand
  • 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.


    (Only for Reference)
Animal Research:

[3]

+ Expand
  • Animal Models: C57BL/6 mice
  • Formulation: anhydrous ethanol, q.s. with water
  • Dosages: 1.2 and 0.6 mg/10g
  • Administration: by gavage
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 96 mg/mL (199.75 mM)
Ethanol 33 mg/mL (68.66 mM)
Water 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.

Chemical Information

Molecular Weight 480.59
Formula

C29H36O6

CAS No. 107316-88-1
Storage powder
in solvent
Synonyms N/A

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID