Smo Antagonist

Sonidegib (Erismodegib) is a potent and selective Smo antagonist with IC₅₀ of 1.3 nM and 2.5 nM for mouse and human Smo in binding assay, respectively.

SANT-1, a potent Smo antagonist, inhibits Hedgehog signaling. SANT-1 shows IC₅₀s of 20 nM and 30 nM in Shh-LIGHT2 and SmoA1-LIGHT2 assay, respectively.

KAAD-Cyclopamine, a hedgehog signaling inhibitor, is a smoothened antagonist.

Sonidegib diphosphate (Erismodegib diphosphate) is a potent and selective Smo antagonist with IC₅₀ of 1.3 nM and 2.5 nM for mouse and human Smo in binding assay, respectively.

PF-5274857 is a potent, selective, orally active and brain-penetrant antagonist of Smo, with an IC₅₀ of 5.8 nM and K_i of 4.6 nM. PF-5274857 has potential for research of tumor types including brain tumors and brain metastasis driven by an activated Hh pathway.

S1PL-IN-31 (compound ) is an oral active sphingosine-1-phosphate (S1P) lyase inhibitor with the IC₅₀ of 210 nM. S1PL-IN-31 is Smoothened receptor antagonist with the IC₅₀ of 440 nM. S1PL-IN-31 can be used for study of experimental autoimmune encephalomyelitis.

MK-4101 is a Smoothened (SMO) antagonist (IC₅₀ of 1.1 µM for 293 cells ) and also a potent inhibitor of the hedgehog pathway (IC₅₀ of 1.5 µM for mouse cells; IC₅₀ of 1 µM for KYSE180 oesophageal cancer cells). MK-4101 has robust antitumor activity that inhibits tumor cell proliferation and induces extensive apoptosis.

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.

MRT-81 is a potent antagonist of human and rodent smoothened (Smo) receptors, with an IC₅₀ value of 41 nM in the Shh-light2 cells. MRT-81 has potent hedgehog inhibiting activity. MRT-81 can be used for the research of cancer.

SANT-1 (GMP) is SANT-1 (HY-100224) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. SANT-1, a potent Smo antagonist, inhibits Hedgehog signaling.

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

IHR-1 is a cell membrane impermeable Smo antagonist.

MRT-83 (hydrochloride) is the potent antagonist of Smoothened (Smo) receptor. MRT-83 (hydrochloride) inhibits the Hedgehog (Hh) signaling pathway and BODIPY-cyclopamine binding to human Smo. MRT-83 (hydrochloride) has the potential for researching cancer disease.

AZD8542 is an antagonist of Smoothened (SMO), playing an important role in oncology. AZD8542 is an Hedgehog (Hh) pathway antagonist on tumor progression with an emphasis on the role of the stroma compartment.

MRT-10 is a seven-transmembrane receptor smoothened (Smo) antagonist with an IC₅₀ of 0.65 μM in the micromolar range in various Hedgehog (Hh) assays. MRT-10 binds to the Smo receptor at the level of the Bodipycyclopamine binding site. MRT-10 can be used for the research of cancer.

Smo antagonist M25 is a smoothened antagonist for inhibition of the hedgehog pathway.

LAB687 is a microsomal triglyceride transfer protein (MTP) inhibitor with an IC₅₀ of 0.9 nM for apolipoprotein B (apoB) secretion in HepG2 cells. LAB687 also acts as a Smoothened (Smo) antagonist, with IC₅₀ values of 2.48 μM and 3.42 μM against mouse and human Smo receptors, respectively. LAB687 reduces triglyceride and low-density lipoprotein cholesterol (LDL-C) levels, and inhibits the Hedgehog signaling pathway. LAB687 can be used in studies related to Hedgehog-dependent cancers.

MRT-14 is a potent antagonist of Smo. Smo is the major component involved in signal transduction of the Hedgehog (Hh) morphogens. MRT-14 has the potential for the research of several types of cancers linked to abnormal Hh signaling.

IHR-Cy3 is a potent fluorescent Smo antagonist with an IC₅₀ of 100 nM.

SMO-IN-4 (Compound 24) is a potent and orally active smoothened antagonist (IC₅₀: 24 nM). SMO-IN-4 has antitumor activity.