Cart summary

You have no items in your shopping cart.

Isosilybin

SKU: orb1303734

Description

Isosilybin and Silybin are potential PXR antagonists for research, aimed at mitigating CYP3A4-mediated drug-drug interactions. Studies in vitro and in vivo support their application in oncology research for improving therapeutic safety by modulating nuclear receptor pathways.

Research Area

Metabolism Research

Images & Validation

−
Isosilybin

Key Properties

−
CAS Number72581-71-6
MW482.44
Purity99.92%
FormulaC25H22O10
SMILESCOc1cc(ccc1O)C1Oc2ccc(cc2OC1CO)C1Oc2cc(O)cc(O)c2C(=O)[C@@H]1O
TargetCytochromes P450
SolubilityChloroform, Dichloromethane, Ethyl Acetate:Soluble;DMSO:88 mg/mL (182.41 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (6.84 mM)

Bioactivity

−
Target 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. 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. 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. 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.
Read more...
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.
Read more...

Storage & Handling

−
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

−
CYP3A4, Cytochrome P450, Isosilibinin, Isosilybin, Isosilybinin, Q100795, Q 100795

Similar Products

−
  • Isosilybin A

    Isosilybin A [orb1297319]

    99.88% (May vary between batches)

    142796-21-2

    482.44

    C25H22O10

    1 ml x 10 mM (in DMSO), 10 mg, 25 mg, 50 mg, 1 mg, 5 mg
  • Isosilybin B

    Isosilybin B [orb1684500]

    99.96%

    142796-22-3

    482.44

    C25H22O10

    5 mg, 1 mg, 10 mg, 25 mg, 50 mg, 1 ml x 10 mM (in DMSO)
  • Isosilybin (Standard)

    Isosilybin (Standard) [orb3140870]

    72581-71-6

    482.44

    C25H22O10

    10 mg
  • Isosilybin B (Standard)

    Isosilybin B (Standard) [orb3140871]

    142796-22-3

    482.44

    C25H22O10

    5 mg
  • Isosilybin A

    Isosilybin A [orb1218827]

    >98% (HPLC)

    142796-21-2

    482.4

    C25H22O10

    1 g, 500 mg, 200 mg, 100 mg, 10 mg, 5 mg
Quality Guarantee

Quality Guarantee

Explore bioreagents carefree to elevate your research. All our products are rigorously tested for performance. If a product does not perform as described on its datasheet, our scientific support team will provide expert troubleshooting, a prompt replacement, or a refund. For full details, please see our Terms & Conditions and Buying Guide. Contact us at [email protected].

Compound Identifiers

PubChem CID
45039613 ↗

Key Properties

−
No computed properties available.

Documents Download

Datasheet
Product Information
Download

Request a Document

Protocol Information

Find More Protocols

Isosilybin (orb1303734)

  • Star
  • Star
  • Star
  • Star
  • Star
  • 0.0
Based on 0 reviews

Participating in our Biorbyt product reviews program enables you to support fellow scientists by sharing your firsthand experience with our products.

Login to Submit a Review

No reviews yet

Login to review

Step 1: Enter information below

(Recommended: An additional animal making an allowance for loss during the experiment)

Step 2: Enter the in vivo formulation

(This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO +
%+
% Tween 80 +
%

Available Sizes

Select a size below

1 mg
¥ 910.00
5 mg
¥ 1,430.00
1 ml x 10 mM (in DMSO)
¥ 1,560.00
10 mg
¥ 1,950.00
25 mg
¥ 3,510.00
50 mg
¥ 6,110.00
100 mg
¥ 8,710.00
DispatchUsually dispatched within 3-5 working days
Bulk Enquiry
Need technical support? Find your Distributor Return and Tax Policy

Email

[email protected]

UK Office

+44 (0)1223 859353

US Office

+1 (415) 906-5211

CN Office

+86 (27)-87663101

Distributors

biorbyt.com/distributor