human smo

LEQ506 is a Smo inhibitor with IC50s of 2 nM and 4 nM for hSmo and mSmo, respectively.

Sonidegib (Erismodegib), a Smoothened (Smo) antagonist, inhibits Hedgehog (Hh) signaling with IC50 of 1.3 nM (mouse) and 2.5 nM (human), respectively.

Sonidegib diphosphate (LDE225 diphosphate) is a selective antagonist of Smo that inhibits murine Smo (IC50:1.3 nM) and human Smo (IC50:2.5 nM).

Cyclopamine-KAAD is a potent inhibitor of hedgehog signaling with an IC50 value of 20 nM in a Shh-LIGHT2 assay. It blocks binding of BODIPY-cyclopamine to cells expressing Smoothened (Smo) in a dose-dependent manner. Cyclopamine-KAAD is cell-permeable and binds to SmoA1 to promote its exit from the endoplasmic reticulum. It inhibits the invasion and migration (45.9 and 43.3% inhibition, respectively) of Bel-7402 hepatocarcinoma cells and decreases the expression of nuclear glioma-associated oncogene 1 (Gli1) and cytosolic MMP-9, pERK1, and pERK2 proteins in a dose-dependent manner. Cyclopamine-KAAD also increases TRAIL-mediated cell death in NCH82 and NCH89 human glioblastoma cultures and upregulates expression of the death receptors DR4 and DR5 in LN229 and U251 glioma cells.

Potent Smo antagonist (IC50 = 5 nM). Attenuates the leukemia-initiation potential of AML cells in a serial transplantation mouse model. Also eliminates self-propagation capacity of AML cells. Munchhof et al (2011) Discovery of PF-04449913, a potent and orally bioavailable inhibitor of smoothened. ACS Med.Chem.Lett. 3 106 PMID:24900436 |Fukushima et al (2016) Small-molecule Hedgehog inhibitor attenuates the leukemia-initiation potential of acute myeloid leukemia cells. Cancer Sci. 107 1422 PMID:27461445 |Giordani et al (2016) The human Smoothened inhibitor PF-04449913 induces exit from quiescence and loss of multipotent Drosophila hematopoietic progenitor cells. Oncotarget 7 55313 PMID:27486815

MRT-83 (hydrochloride) is a potent antagonist of the Smoothened (Smo) receptor, effectively inhibiting the Hedgehog (Hh) signaling pathway and BODIPY-cyclopamine binding to human Smo. With its potential applications in the study of cancer disease, MRT-83 (hydrochloride) demonstrates promising prospects for research purposes.

SMO-IN-3 is a potent inhibitor of smoothened (SMO) that acts on the hedgehog (Hh) signaling pathway (IC50: 34.09 nM). SMO-IN-3 inhibits the proliferation of Daoy, a human medulloblastoma cell line, and exhibits anticancer effects.

SMO-IN-2 is a potent smoothened (SMO) inhibitor of hedgehog (Hh) signaling.SMO-IN-2 shows antiproliferative activity and anticancer activity against human medulloblastoma cell lines.SMO-IN-2 can be used in the study of cancer.

MRT-81 is a potent antagonist of human and rodent smoothened receptors that inhibits hedgehog activity with an IC50 value of 41 nM in Shh-light2 cells.It is used in the study of cancer.