GNE-7883 free base · Synonyms: GNE 7883 · GNE7883

GNE-7883 is a potent, reversible, allosteric inhibitor of the YAP1-TEAD interaction.

For research use only. Not for human or veterinary use.

Target YAP

Research area Cancer

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Data Sheet SDS COA

GNE-7883 structure

CAS No.: 2648450-42-2

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
100 mg	USD 498.00	BP-02039-100mg	In stock	Get quote
250 mg	USD 798.00	BP-02039-250mg	In stock	Get quote
500 mg	USD 1,298.00	BP-02039-500mg	In stock	Get quote
1 g	USD 2,098.00	BP-02039-1g	In stock	Get quote
2 g	USD 3,598.00	BP-02039-2g	In stock	Get quote

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Description

GNE-7883 (GNE7883) is a potent, reversible, allosteric inhibitor of the YAP1-TEAD interaction.

Biological activity

GNE-7883 (GNE7883) is a potent, reversible, allosteric inhibitor of the YAP1-TEAD interaction. The potent inhibition of pan-TEAD lipidation with GNE-7883 translated well to the disruption of YAP1 binding to each of the four TEAD isoforms by the YAP1 HTRF assay. GNE-7883 potently inhibited proliferation of the OVCAR-8 and NCI-H226 cells, with EC50 values of 115 nM and 333 nM, respectively. GNE-7883 (250 mg/kg, subcutaneous dosing) showed strong in vivo tumor growth inhibition (TGI) of 102% in the mesothelioma NCIH226 xenograft mouse model.

Identifiers

SMILES: O=C1C=C(C2=CC=C(C3CCCCC3)C=C2)NC4=C(C(N5CC(CF)C5)=O)C(C6=NC=CN=C6C)=NN14
InChIKey: UNRTVIQQMJRQLZ-UHFFFAOYSA-N

Specifications

MW (average): 500.5673
Formula: C₂₈H₂₉FN₆O₂
CAS No.: 2648450-42-2
Physical state: Solid
Color: White to light yellow
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20°C, 3 years , 4°C, 2 years ; In solvent -20°C, 1 year

Solubility

Soluble in DMSO

In vitro: DMSO : 50 mg/mL

Documents

References

[1]. Holden, Jeffrey K et al. “Small Molecule Dysregulation of TEAD Lipidation Induces a Dominant-Negative Inhibition of Hippo Pathway Signaling.” Cell reports vol. 31,12 (2020): 107809.

[2]. Barry ER, Simov V, Valtingojer I, Venier O. Recent Therapeutic Approaches to Modulate the Hippo Pathway in Oncology and Regenerative Medicine. Cells. 2021 Oct 11;10(10):2715. PMID: 34685695; PMCID: PMC8534579.

Same target

Search YAP

Same research area

Search Cancer