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EBCL-0048

Hippo signaling pathway ligands

The Hippo signaling pathway is a highly conserved regulatory network, crucial for controlling organ size, tissue regeneration, and cellular proliferation. It functions by integrating extracellular and intracellular signals to modulate gene expression, primarily through the regulation of the YAP/TAZ transcriptional co-activators. The pathway is present in nearly all multicellular organisms, underscoring its essential role in maintaining tissue homeostasis and preventing tumorigenesis. Dysregulation of the Hippo pathway is associated with various cancers, fibrosis, and other pathological conditions, making it a promising therapeutic target in oncology and regenerative medicine.

Library of Hippo signaling pathway ligands comprises 365 small molecules designed to target key components of the pathway. This library includes inhibitors and activators suitable for exploring therapeutic applications in cancer treatment, tissue repair, immune modulation, and metabolic disorders.


Related terms: Hippo, STK3, STK4, LATS2 , LATS1, TEF1, TEF3, TEF4

Library image

The Hippo tumor-suppressor pathway (Created by BioRender.com)

Preplated options

Dry powder/solution (DMSO)Dry powder
Number of compounds365
Comment
Dry powder/solution (DMSO)DMSO
Number of compounds270
Comment

Highlights

Molecule highlight
EBC-12065CAS: 557795-19-4

Sunitinib is a multi-targeted receptor tyrosine kinase inhibitor.

Molecule highlight
EBC-220032CAS: 755038-02-9

BI-2536 is an inhibitor of BRD4, it also has selectivity for Plk1 over Plk2 and Plk3.

Molecule highlight
EBC-145263CAS: 1181488-31-2

The compound shows inhibitory activity against various protein kinases.

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Disclaimer

All our products are for research purpose only. Any personal or non-scientific use is strictly prohibited.

Note

All the compounds with solubility below 10 mM are shipped as 2 mM solutions.

Product Features

Product Features:

  • A set of 365 Hippo-active molecules with sub-10 micromolar activity coefficient values for HTS/HCS programs.
  • The library is composed of ligands that target all major pharmaceutically relevant hippo pathway targets.
  • Library of Hippo signaling pathway ligands covers novel promising preclinical lead compounds, clinical candidates and approved drugs.
  • Calculated structural diversity of the collection: 0.86.
  • Comprehensive documentation with structures, trivial names, activity coefficient values, types of action on target and references to original literature.
  • NMR and LCMS validated purity.
  • All the compounds are available in stock for hit follow-up.
  • The library is continuously updated.

Product Details

  • Format: 10 - 100 µL of 10 mM DMSO stock solutions; dry powders (1 mg);
  • Container: 384-well microplates;
  • Storage: - 18 °C;
  • Shipping: Dry ice.

Utility

  • High throughput screening (HTS);
  • High content screening (HCS);
  • Cherry picking.

Library Composition

Name
Occurrence in the library, times

Serine/threonine-protein kinase 3

43

43

Number of compounds

43

Serine/threonine-protein kinase 4

10

10

Number of compounds

10

Transcriptional enhancer factor TEF-3

4

4

Number of compounds

4

Serine/threonine-protein kinase LATS2

1

1

Number of compounds

1

WW domain-containing transcription regulator protein 1

1

1

Number of compounds

1

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