Smoothened Receptors

LDE225 is an orally bioavailable small-molecule Smoothened (Smo) antagonist with potential antineoplastic activity.

PF-5274857 is a novel Smo antagonist that specifically binds to Smo with a K(i) of 4.6 ?? 1.1 nmol/L and completely blocks the transcriptional activity of the downstream gene Gli1 with an IC(50) of 2.7 ?? 1.4 nmol/L in cells.

Saridegib is a potent and specific inhibitor of Smoothened (Smo), a key signaling transmembrane protein in the Hedgehog (Hh) pathway.

BMS-833923 (or XL-139) is an orally bioavailable small-molecule SMO (Smoothened) inhibitor with potential antineoplastic activity.

PF-04449913 is a potent and orally bioavailable inhibitor of smoothened.

Jervine is a naturally occuring steroidal alkaloid that causes cyclopia by blocking sonic hedgehog(Shh) signaling; Jervine is an inhibitor of Smo.

LEQ506 is a second-generation inhibitor of smoothened (Smo) with IC50s of 2 and 4 nM in human and mouse, respectively.

JNJ-1289 is a potent and selective inhibitor of human spermine oxidase (hSMOX), exhibiting a competitive and allosteric mechanism of action with an IC50 value of 50 nM. This compound is primarily utilized in research studies focused on polyamine catabolism, inflammation, and various cancer models, providing valuable insights into the role of hSMOX in these biological processes.

MRT-83 hydrochloride is a potent Smoothened (Smo) receptor antagonist. By inhibiting the Hedgehog (Hh) signaling pathway and BODIPY-cyclopamine binding to human Smo, MRT-83 hydrochloride demonstrates significant biological activity. This compound is particularly relevant for research applications focused on cancer and associated signaling pathways.

Glasdegib maleate is a potent smoothened inhibitor that selectively targets the human Smoothened (SMO) protein. With an IC50 value of 4 nM, this orally bioavailable compound effectively modulates the Hedgehog signaling pathway, making it valuable for research in cancer biology and developmental processes. Glasdegib maleate is primarily used in studies investigating tumor growth and metastasis driven by aberrant Hedgehog signaling.

Glasdegib hydrochloride is a potent smoothened (SMO) inhibitor, primarily targeting the Hedgehog signaling pathway. It exhibits high affinity for human SMO, with an IC50 of 4 nM, making it an effective tool for research in cancer biology and developmental processes. This compound is valuable for studies investigating the role of SMO in tumorigenesis and therapeutic resistance in various malignancies.

AZD7254 is an orally active Smoothened (SMO) inhibitor with a reported EC50 of 1.0 nM against Sonic Hedgehog (Shh) protein. This compound effectively modulates hedgehog signaling pathways, making it a valuable tool for investigating the role of SMO in various cancers and developmental disorders. Its potent inhibition of SMO activity supports research applications in targeted therapies and pathway analysis.

SMO-IN-1 is an orally active Smoothened (SMO) inhibitor that demonstrates an EC50 of 89 nM for sonic hedgehog (Shh) protein. This compound is effective in disrupting the hedgehog signaling pathway, making it a valuable tool in cancer research and developmental biology studies. It may be particularly relevant for investigating tumors associated with aberrant hedgehog signaling.

Saridegib hydrochloride is a selective inhibitor of Smoothened (Smo), a critical component of the Hedgehog (Hh) signaling pathway. By targeting Smo, this compound effectively disrupts Hh-mediated signaling, which is implicated in various developmental processes and diseases, including cancer. It is utilized in research to explore the role of the Hh pathway in tumorigenesis and as a potential therapeutic approach in Smo-dependent malignancies.