Home Angiogenesis VDA chemical - YAP inhibitor - Autophagy inhibitor - Apoptosis related activator - TEAD inhibitor Verteporfin For research use only.

Verteporfin

Synonyms: CL 318952

Verteporfin is a small molecule that inhibits TEAD–YAP association and YAP-induced liver overgrowth. It is also a potent second-generation photosensitizing agent derived from porphyrin. Verteporfin is an autophagy inhibitor. Verteporfin inhibits cell proliferation and induces apoptosis.

Verteporfin Chemical Structure

Verteporfin Chemical Structure

CAS: 129497-78-5

Selleck's Verteporfin has been cited by 132 publications

Purity & Quality Control

Batch: Purity: 99.31%
99.31

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Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HL-60 Function assay ~100 ng/mL DMSO increases DNA fragmentation levels 10607710
HL-60 cytotoxicity assay ~100 ng/mL DMSO inhibits cell viability 10607710
Jurkat Apoptosis assay ~280 nM DMSO induces a Bcl-2-dependent apoptosis 11245415
RIF-1 Function assay 1 μg/ml DMSO decreases oxygen consumption 12615718
RIF-1 cytotoxicity assay 1 μg/ml DMSO decrease to 20 ± 5% cell survival 12615718
SVEC4-10 Function assay 200 ng/ml DMSO induces microtubule depolymerization 16467106
SVEC4-10 Function assay 200 ng/ml DMSO induces stress actin fiber formation 16467106
ARPE-19 cytotoxicity assay ~0.1 μg/ml DMSO shows a dose-dependent toxicity 16987905
ARPE-19 Function assay 0.01 μg/ml DMSO increases VEGF and reduces PEDF expression 16987905
Y-79 Growth inhibitory assay ~1 μg/ml DMSO decreases retinoblastoma cell proliferation 18579764
WERI-Rb1 Growth inhibitory assay ~1 μg/ml DMSO decreases retinoblastoma cell proliferation 18579764
RB247C3 Growth inhibitory assay ~1 μg/ml DMSO decreases retinoblastoma cell proliferation 18579764
RB355 Growth inhibitory assay ~1 μg/ml DMSO decreases retinoblastoma cell proliferation 18579764
RB383 Growth inhibitory assay ~1 μg/ml DMSO decreases retinoblastoma cell proliferation 18579764
hFibro cytotoxicity assay 0.5 µg/ml DMSO decreases viability by 86,5% 23441114
pTMC cytotoxicity assay 0.5 µg/ml DMSO decreases viability by 92.9% 23441114
hTMC cytotoxicity assay 0.5 µg/ml DMSO decreases viability by 88.9% 23441114
ARPE-19 cytotoxicity assay 0.5 µg/ml DMSO decreases viability by 55.5% 23441114
Panc-1 Growth inhibitory assay 10 μM DMSO inhibits cell proliferation 24069069
MIA PaCa-2 Growth inhibitory assay 10 μM DMSO inhibits cell proliferation 24069069
BxPC-3 Growth inhibitory assay 10 μM DMSO inhibits cell proliferation completely 24069069
SU86.86 Growth inhibitory assay 10 μM DMSO inhibits cell proliferation completely 24069069
MCF-7 Autophagy assay 10 μM DMSO inhibits gemcitabine-induced autophagy 24069069
WERI Growth inhibitory assay ~10 μg/ml DMSO inhibits growth of retinoblastoma cells 24837142
WERI Function assay ~10 μg/ml DMSO blocks cell cycle progression 24837142
Y-79 Function assay ~10 μg/ml DMSO blocks cell cycle progression 24837142
Y-79 Function assay ~10 μg/ml DMSO affects YAP-TEAD proto-oncogene pathway 24837142
Y-79 Function assay ~10 μg/ml DMSO down-regulates pluripotency marker OCT-4 24837142
Phototoxicity assay B16F10 24 hrs IC50 = 1.07 μM 27136389
Phototoxicity assay B16F10 24 hrs IC50 = 1.2 μM 27136389
Phototoxicity assay A375 24 hrs IC50 = 2.06 μM 27136389
Dark toxicity assay B16F10 48 hrs IC50 = 24.92 μM 27136389
Dark toxicity assay B16F10 48 hrs IC50 = 25.03 μM 27136389
Dark toxicity assay A375 48 hrs IC50 = 36.33 μM 27136389
qHTS assay TC32 qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells 29435139
qHTS assay U-2 OS qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells 29435139
qHTS assay A673 qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
qHTS assay DAOY qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells 29435139
qHTS assay Saos-2 qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells 29435139
qHTS assay BT-37 qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells 29435139
qHTS assay RD qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells 29435139
qHTS assay SK-N-SH qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells 29435139
qHTS assay BT-12 qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells 29435139
qHTS assay MG 63 (6-TG R) qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells 29435139
qHTS assay OHS-50 qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells 29435139
qHTS assay Rh41 qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells 29435139
qHTS assay SJ-GBM2 qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells 29435139
qHTS assay SK-N-MC qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
qHTS assay LAN-5 qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells 29435139
Antitumor assay B16F10 2 mg/kg 2 hrs Antitumor activity against B16F10 cells implanted in C57BL/6 mouse assessed as tumor growth inhibition at 2 mg/kg, iv administered for 2 hrs followed by irradiation with laser at 150 J/cm'2 for 10 mins 27136389
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Biological Activity

Description Verteporfin is a small molecule that inhibits TEAD–YAP association and YAP-induced liver overgrowth. It is also a potent second-generation photosensitizing agent derived from porphyrin. Verteporfin is an autophagy inhibitor. Verteporfin inhibits cell proliferation and induces apoptosis.
Targets
VDA [1]
(Endothelial cells)		 YAP/TEAD interaction [3]
In vitro
In vitro

Verteporfin is about four times more efficient in absorbing light at wavelengths that penetrate tissues best (i.e., around 700 nm) and thus provides a much higher cytotoxic effect than hematoporphyrin (10 times more in human adherent cell lines). Verteporfin is lipophilic and is more readily taken up by malignant or activated cells, compared with normal or resting cells. Verteporfin binds with LDL to form a complex, which is then taken up into proliferating cells (e.g., neovascular endothelial cells) probably via LDL receptors and endocytosis. Verteporfin therapy achieves complete angiographic occlusion of the neovascular compartment by thrombosis of vascular channels, following selective endothelial damage. Verteporfin therapy selectively induces reproducible and isolated choriocapillary occlusion without alteration of overlying photoreceptors or ganglion cells, as shown by light and electron microscopy. [1]

Verteporfin conbined with light rapidly exhibits apoptotic changes reflected by caspase-3 and caspase-9 activation and PARP cleavage in HL-60 cells, changes that are blocked by the general caspase inhibitor ZVAD.fmk. [2]
Cell Research Cell lines Ki67+ and Sox10+ cells
Concentrations 2 uM
Incubation Time 72 h
Method

Cells were treated with verteporfin (2 µM) for 72 hr for Brdu staining.
Experimental Result Images Methods Biomarkers Images PMID
Western blot ECAD / Vimentin / Sox2 / CD44 / CD133 c-Myc / Bcl-2 p-S6(S240/244) / p-4EBP1(S65) beta-catenin 30467925
Growth inhibition assay Cell viability 28042502
Immunofluorescence p-YAP(Y357) Calreticulin YAP1 28404908
In Vivo
In vivo

Verteporfin can be used for angiographic visualization of choroidal vessels and CNV, which demonstrates that the photosensitizer accumulates rapidly in experimental CNV in monkeys. Verteporfin accumulates rapidly in the established vasculature of the choroid, RPE, and photoreceptors of rabbit eyes. Verteporfin reaches maximal tissue levels within 3 hours of intravenous injection, followed by a rapid decline within 24 hours in mice. Verteporfin is metabolized to a less active form in vivo and is cleared very rapidly, predominantly in the feces and a very small proportion excreted in urine. Verteporfin therapy effectively and selectively prevents fluorescein dye leakage from experimentally induced CNV in monkeys. [1]
Animal Research Animal Models Atoh1-Ptch mice
Dosages 100 mg/kg
Administration i.p.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04590664 Recruiting Glioblastoma|Recurrent Glioblastoma Emory University|National Cancer Institute (NCI) January 15 2021 Phase 1|Phase 2
NCT03797547 Unknown status Myopic Choroidal Neovascularisation Poitiers University Hospital June 22 2018 --
NCT01846273 Completed Age-related Macular Degeneration|Polypoidal Choroidal Vasculopathy Novartis Pharmaceuticals|Novartis August 7 2013 Phase 4
NCT00423189 Terminated Age-Related Macular Degeneration David M. Brown M.D.|Novartis Pharmaceuticals|Greater Houston Retina Research January 2007 Phase 4
NCT00403442 Terminated Macular Degeneration Vitreous -Retina- Macula Consultants of New York|QLT Inc. September 2006 Phase 1

Chemical lnformation & Solubility

Molecular Weight 718.79 Formula

C41H42N4O8
CAS No. 129497-78-5 SDF Download Verteporfin SDF
Smiles COC(=O)CCC1=C(C)C2=CC3=NC(=CC4=C(C)C(=C([NH]4)C=C5N=C(C=C1[NH]2)C(=C5C)CCC(O)=O)C=C)C6=CC=C(C(C(=O)OC)C36C)C(=O)OC
Storage (From the date of receipt) 3 years-20°C （in the dark）powder

In vitro
Batch:

DMSO : 100 mg/mL ( (139.12 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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