Demethylzeylasteral (T-96)

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

Demethylzeylasteral (T-96) Chemical Structure

Demethylzeylasteral (T-96) Chemical Structure

CAS No. 107316-88-1

Purity & Quality Control

Demethylzeylasteral (T-96) Related Products

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
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].
Cell Research 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.

In Vivo
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].
Animal Research Animal Models C57BL/6 mice
Dosages 1.2 and 0.6 mg/10g
Administration by gavage

Chemical Information & Solubility

Molecular Weight 480.59 Formula

C29H36O6

CAS No. 107316-88-1 SDF Download Demethylzeylasteral (T-96) SDF
Smiles CC12CCC(CC1C3(CCC4(C5=CC(=C(C(=C5C(=O)C=C4C3(CC2)C)C=O)O)O)C)C)(C)C(=O)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 96 mg/mL ( (199.75 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 33 mg/mL

Water : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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