Verteporfin (Visudyne) --- YAP Inhibitor

Verteporfin (Visudyne) is a potent and selective YAP inhibitor, disrupts YAP-TEAD interactions and enhances trypsin cleavage of YAP with EC50 ~100 nM. It inhibits growth and proliferation of retinoblastoma cells. It also significantly blocks cancer stem cell (CSC) properties in cells with high YAP1 and a high proportion of ALDH1(+). In vivo it can suppress YAP-induced liver overgrowth in mice.

Product information

CAS Number: 129497-78-5

Molecular Weight: 718.79

Formula: C41H42N4O8

Chemical Name:  3-[(23S,24R)-14-Ethenyl-5-(3-methoxy-3-oxopropyl)-22,23-bis(methoxycarbonyl)-4,10,15,24-tetramethyl-25,26,27,28-tetraazahexacyclo[16.6.1.13,6.18,11.113,16.019,24]octacosa-1,3,5,7,9,11(27),12,14,16,18(25),19,21-dodecaen-9-yl]propanoic acid

Smiles: COC(=O)CCC1C2=CC3=NC(=CC4NC(C=C5N=C(C=C(N2)C=1C)[C@]1(C)[C@@H](C(=CC=C15)C(=O)OC)C(=O)OC)=C(C)C=4C=C)C(C)=C3CCC(O)=O

InChiKey: YTZALCGQUPRCGW-MXVXOLGGSA-N

InChi: InChI=1S/C41H42N4O8/c1-9-23-20(2)29-17-34-27-13-10-26(39(49)52-7)38(40(50)53-8)41(27,5)35(45-34)19-30-22(4)25(12-15-37(48)51-6)33(44-30)18-32-24(11-14-36(46)47)21(3)28(43-32)16-31(23)42-29/h9-10,13,16-19,38,42,44H,1,11-12,14-15H2,2-8H3,(H,46,47)/b28-16-,29-17-,30-19-,31-16-,32-18-,33-18-,34-17-,35-19-/t38-,41+/m0/s1

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO up to 50 mM

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

Verteporfin was used at 10 µM final concentration in various in vitro assays.

In Vivo:

Verteporfin was administered by intraperitoneal injection at 100 mg/Kg once every other day in liver overgrowth model.

References:

1. Liu-Chittenden Y, et al. Genetic and pharmacological disruption of the TEAD-YAP complex suppresses the oncogenic activity of YAP. (2012) Genes Dev. 26(12):1300-5.
2. Brodowska K, et al. The clinically used photosensitizer Verteporfin (VP) inhibits YAP-TEAD and human retinoblastoma cell growth in vitro without light activation. (2014) Exp Eye Res. 124:67-73.
3. Song S, et al. Hippo coactivator YAP1 upregulates SOX9 and endows esophageal cancer cells with stem-like properties. (2014) Cancer Res. 74(15):4170-82.

Products are for research use only. Not for human use.

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