Smoothened Receptors

LDE225 (NVP-LDE225) is a potent, selective and orally bioavailable Smoothened (SMO) antagonist that inhibits hedgehog (Hh) signaling pathway via antagonism of the Smoothened receptor (SMO).

LY2940680 has been shown to affect a cancer cell signaling pathway initiated by the Hedgehog (Hh) protein.

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.

SAG is a chlorobenzothiophene-containing compound which acts as a SMO agonist (EC50 = 3 nM) but inhibits hedgehog signaling at high concentrations (>1 uM).

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.

ALLO-2 is a potent drug-resistant Smoothened (Smo) mutant antagonist that inhibits Smo agonist Hh-Ag1.5-induced luciferase expression in TM3-Gli-Luc cells with IC50 of 6 nM.

J-2156 is a high potent, selective somatostatin receptor type 4 (SST4 receptor) agonist with IC50s of 0.05 nM and 0.07 nM for human and rat SST4 receptors, respectively. The ED50 of J-2156 in rats for the relief of mechanical allodynia and mechanical hyperalgesia in the ipsilateral hindpaws was 3.7 and 8.0 mg/kg, respectively.

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

MRT-83 is a potent antagonist of Smo, with an IC50 in the nanomolar range. MRT-83 also blocks Hedgehog (Hh) signaling.

SAG (hydrochloride) is a potent Smo receptor agonist, and activates the Hedgehog signaling pathway, with a Kd of 59 nM.

20(S)-hydroxyCholesterol (20α-Hydroxycholesterol) is an allosteric activator of the oncoprotein smoothened (Smo) that activates the hedgehog (Hh) signaling pathway with an EC50 of 3 μM in a gene transcription reporter assay using NIH3T3 cells.

GSA-10 is a potent agonist of the smooth (Smo) receptor, playing a crucial role in mediating Hedgehog (Hh) signaling pathways. This compound exhibits significant osteogenic activity and is valuable in regenerative medicine and research on cancer pathologies. Additionally, GSA-10 can be utilized in studies focused on adipogenesis and fat development, making it a versatile tool in biological research.

AZD8542 is a potent Smoothened (SMO) antagonist that effectively disrupts the Hedgehog (Hh) signaling pathway, which is crucial in tumor progression. This compound is particularly relevant in oncology research, focusing on the interactions within the tumor microenvironment and the stroma compartment. AZD8542's ability to inhibit Hh pathway activity makes it a valuable tool in the study of cancer therapies and tumor biology.

SAG dihydrochloride is a potent Smoothened (Smo) receptor agonist, with an EC50 of 3 nM and a Kd of 59 nM. This compound effectively activates the Hedgehog signaling pathway, providing a robust mechanism to counteract the inhibitory effects of Cyclopamine. SAG dihydrochloride is valuable for research in developmental biology, cancer biology, and therapeutic strategies targeting Hedgehog-related pathways.

KAAD-Cyclopamine is an antagonist of the Smoothened receptor, a critical component of the Hedgehog signaling pathway. This compound effectively inhibits hedgehog signaling, thereby influencing cell proliferation and differentiation processes. It is widely used in research related to developmental biology, cancer, and regenerative medicine, facilitating the study of signaling cascades and their implications in various diseases.

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.

BODIPY-Cyclopamine is a fluorescent ligand targeting the Smoothened (SMO) receptor, crucial for Hedgehog signaling pathway regulation. Dysregulation of this pathway is linked to tumorigenesis, making BODIPY-Cyclopamine valuable for research related to cancer biology. Utilizing the NanoBRET (Nanofluorescein bioluminescence resonance energy transfer) technique, this compound facilitates the sensitive detection of energy transfer between SMO and the fluorescent probe, enabling high-throughput screening and kinetic studies. Additionally, investigating the binding dynamics of BODIPY-Cyclopamine can assist in the development of SMO-targeted therapeutics.

MRT-81 is a potent antagonist of smoothened (Smo) receptors in both human and rodent models, exhibiting an IC50 value of 41 nM in Shh-light2 cells. This compound effectively inhibits hedgehog signaling pathways, making it a valuable tool in cancer research. Its ability to modulate Smo activity facilitates investigations into Hedgehog pathway-related tumors and their therapeutic interventions.

IHR-1 is a cell membrane impermeable antagonist of Smoothened (Smo), a key component of the Hedgehog signaling pathway. This compound effectively inhibits Smo activity, making it a valuable tool for studying Hedgehog-related biological processes and disease states, such as cancer and developmental disorders. IHR-1's specificity for Smo allows for targeted research into the mechanistic roles of this pathway in various cellular contexts.

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.

MRT-10 is a smoothened (Smo) antagonist that effectively inhibits Smo activity with an IC50 of 0.65 μM in various Hedgehog (Hh) signaling assays. By binding to the Bodipycyclopamine-binding site on the Smo receptor, MRT-10 serves as a valuable tool for investigating the roles of Hedgehog signaling in cancer biology. Its application may extend to studies focused on tumor growth and progression influenced by aberrant Hedgehog pathway activation.

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.

MRT-14 is a potent Smoothened (Smo) antagonist, specifically targeting the Hedgehog (Hh) signaling pathway. By inhibiting Smo, MRT-14 disrupts the signal transduction linked to Hh morphogens. This compound demonstrates potential for research applications in various cancers associated with dysregulated Hh signaling.

(Rac)-SAG is a potent agonist of the Smoothened (Smo) receptor, exhibiting an EC50 of 3 nM and a Kd of 59 nM. This compound activates the Hedgehog signaling pathway, making it an invaluable tool in studies focused on Smo-mediated processes. Additionally, (Rac)-SAG can counteract the inhibition of Smo by Cyclopamine, facilitating research into signaling and developmental biology.

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.

SMO-IN-4 is a potent oral antagonist of the Smoothened (SMO) protein, displaying an IC50 of 24 nM. This compound demonstrates significant antitumor activity and is utilized in research focused on hedgehog signaling pathways and cancer therapy. SMO-IN-4 serves as a valuable tool for investigating SMO-related mechanisms in various malignancies.

PF-5274857 hydrochloride is a potent, selective antagonist of Smoothened (Smo) with an IC50 of 5.8 nM and a Ki of 4.6 nM. Its oral bioavailability and ability to penetrate the blood-brain barrier enhance its utility in research on tumors, particularly brain tumors and brain metastases associated with an activated Hedgehog (Hh) signaling pathway. This compound is valuable for studies aimed at understanding Smo-mediated tumorigenesis and developing targeted therapeutics.

7-keto-25-Hydroxycholesterol is an oxysterol that acts as an activator of Smoothened (Smo). This compound interacts specifically with the extracellular cysteine-rich domain (CRD) of Smo, facilitating its activation. Research applications include studies on hedgehog signaling pathways and the exploration of Smo’s role in developmental biology and cancer.

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.