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Isosilybin

🥰Excellent
Catalog No. T3797Cas No. 72581-71-6
Alias Isosilybinin, Isosilibinin

Isosilybin (Isosilibinin) and Silybin might be suitable candidates to design potent PXR antagonists to prevent drug-drug interactions via CYP3A4 in cancer patients.

Isosilybin

Isosilybin

🥰Excellent
Purity: 100%
Catalog No. T3797Alias Isosilybinin, IsosilibininCas No. 72581-71-6
Isosilybin (Isosilibinin) and Silybin might be suitable candidates to design potent PXR antagonists to prevent drug-drug interactions via CYP3A4 in cancer patients.
Pack SizePriceAvailabilityQuantity
1 mg$30In Stock
5 mg$68In Stock
10 mg$105In Stock
25 mg$228In Stock
50 mg$425In Stock
100 mg$628In Stock
1 mL x 10 mM (in DMSO)$72In Stock
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Purity:100%
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Product Introduction

Bioactivity
Description
Isosilybin (Isosilibinin) and Silybin might be suitable candidates to design potent PXR antagonists to prevent drug-drug interactions via CYP3A4 in cancer patients.
Targets&IC50
CYP3A4:74 μM.
In vitro
The reporter gene assay demonstrates that the milk thistle constituents silybin and isosilybin inhibit the PXR-mediated induction of CYP3A4, with isosilybin being a more potent inhibitor. Concentrations of 89, 133, and 200 μM of isosilybin decrease CYP3A4 induction by 64, 82, and 88%, respectively, and achieve an IC50 of 74 μM[1]. Additionally, the diastereoisomers isosilybin B and isosilybin A, derived from silymarin, exhibit anti-prostate cancer (PCA) activity through cell cycle arrest and apoptosis induction in human prostate cancer cells LNCaP and 22Rv1[2]. Isosilybin B enhances phosphorylation of Akt and Mdm2, leading to androgen receptor degradation, which is reversed by PI3K inhibitor pretreatment. This process facilitates the formation of a complex that promotes phosphorylation-dependent ubiquitination and subsequent degradation of the androgen receptor[3]. Isosilybin A significantly activates PPARγ at a 30 μM concentration, leading to a concentration-dependent transactivation of a PPARγ-dependent luciferase reporter. In silico docking studies indicate isosilybin A interacts with the receptor's ligand-binding domain through an additional hydrogen bond not found with inactive silymarin constituents[4].
Cell Research
LNCaP cells and 22Rv1 cells are plated and treated at 40–50% confluency with different doses of isosilybin B and isosilybin A (10–90 μM in medium) dissolved originally in Dimethyl sulfoxide (DMSO) for the desired time periods (24–48 h) in serum condition. An equal amount of DMSO (vehicle) is present in each treatment, including control; DMSO concentration did not exceed 0.1% (v/v) in any treatment. At the end of desired treatments, total cell number is determined by counting each sample in duplicate using a hemocytometer under an inverted microscope. Cell viability is determined using trypan blue exclusion method[2].
AliasIsosilybinin, Isosilibinin
Chemical Properties
Molecular Weight482.44
FormulaC25H22O10
Cas No.72581-71-6
SmilesCOc1cc(ccc1O)C1Oc2ccc(cc2OC1CO)C1Oc2cc(O)cc(O)c2C(=O)[C@@H]1O
Relative Density.1.527 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 88 mg/mL (182.4 mM)
Chloroform, Dichloromethane, Ethyl Acetate: Soluble
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.0728 mL10.3640 mL20.7280 mL103.6398 mL
5 mM0.4146 mL2.0728 mL4.1456 mL20.7280 mL
10 mM0.2073 mL1.0364 mL2.0728 mL10.3640 mL
20 mM0.1036 mL0.5182 mL1.0364 mL5.1820 mL
50 mM0.0415 mL0.2073 mL0.4146 mL2.0728 mL
100 mM0.0207 mL0.1036 mL0.2073 mL1.0364 mL

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