- Cat. No.
- A10258
Vismodegib (GDC-0449)
Synonyms: GDC-0449
GDC-0449 (Vismodegib) is a more potent novel and specific synthetic oral hedgehog pathway inhibitor with an IC50 of 3 nM.
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Hedgehog pathway inhibitors and activators act on a signaling route that patterns embryos and tissues. The hedgehog gene emerged from a 1980 Drosophila screen for mutations that alter segment number and polarity. In mammals, Sonic, Indian and Desert hedgehog ligands bind the receptor Patched 1 (PTCH1), which then releases its block on Smoothened. Pathway activity converts glioma-associated oncogene (GLI) proteins into transcriptional activators. Inherited PTCH1 mutations were linked in 1996 to nevoid basal cell carcinoma syndrome. Vismodegib acts at Smoothened, whereas GANT61 blocks GLI-mediated transcription further downstream. Purmorphamine activates the pathway, and JK 184 is listed as a Hedgehog inhibitor. Compounds aimed at the transcription factors are also grouped in the neighboring Gli category.
Synonyms: GDC-0449
GDC-0449 (Vismodegib) is a more potent novel and specific synthetic oral hedgehog pathway inhibitor with an IC50 of 3 nM.
Synonyms: NSC136476
GANT61 is an inhibitor for GLI1 as well as GLI2-induced transcription, inhibits hedgehog with IC50 of 5 μM, displays selectivity over other pathways, such as TNF and glucocorticoid receptor gene transactivation.
Purmorphamine is a 2,6,9-trisubstituted purine that promotes the differentiation of both human and mouse mesenchymal progenitor cells into osteoblasts.
Synonyms: 11-deoxojervine
Cyclopamine is a Smo or hedgehog signaling pathway inhibitor.
Synonyms: LY-2940680
LY2940680 has been shown to affect a cancer cell signaling pathway initiated by the Hedgehog (Hh) protein.
TAK-441 is a pyrrolo[3,2-c]pyridine derivative, as a highly potent and orally active hedgehog signaling inhibitor.
GANT 58 is a potent Gli antagonist that inhibits GLI1-induced transcription with IC50 of 5 μM.
HhAntag is a small molecule inhibitor of GLI1-mediated transcription, an essential down-stream element of the Hedgehog (Hh) pathway.
Hh-Ag1.5 is one of the most potent and selective small-molecule agonists of the Hedgehog pathway, targeting Smoothened (Smo) with an EC50 ~1 nM.
JK184 is potent downstream hedgehog (Hh) signaling inhibitor that prevents Gli-dependent transcriptional activity (IC50 = 30 nM).
SANT-1 is a potent, cell-permeable inhibitor of Sonic hedgehog (Shh) signaling; high affinity antagonist of smoothened activity (KD = 1.2 nM). Inhibits smoothened agonist effects with an IC50 of 20 nM (in Shh-LIGHT2 cells).
MK-4101 is a potent and selective inhibitor of the Hedgehog Pathway.
Synonyms: Hhat Inhibitor
RU-SKI 43 is a small molecule inhibitor of Hhat(Hedgehog acyltransferase), the enzyme responsible for the attachment of palmitate onto Shh.
Synonyms: Ciliobrevin A
HPI-4 is a hedgehog (Hh) signaling pathway inhibitor with median inhibitory concentration (IC50) less than 10 μM.
Mebendazole is a highly effective, broad-spectrum antihelmintic indicated for the treatment of nematode infestations; has been found as a hedgehog inhibitor.
Dynarrestin is a aminothiazole inhibitor of cytoplasmic dyneins 1 and 2.
U18666A, a cell permeable drug, is a cholesterol synthesis and transport inhibitor.
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.
Neurodazine is a neurogenesis inducer that promotes the differentiation of pluripotent cells into neuronal lineages. This compound activates the Wnt and Shh signaling pathways, facilitating neural development and potentially improving neuroregeneration applications. Neurodazine is suitable for research in developmental biology, neuroscience, and regenerative medicine.
CUR61414 is a potent inhibitor of the Hedgehog signaling pathway, specifically targeting the Smoothened (Smo) protein with a Ki value of 44 nM. This small-molecule aminoproline derivative demonstrates selective activity, inducing apoptosis in cancer cells while sparing adjacent non-tumor cells. CUR61414 is valuable for research applications focused on cancer biology and therapeutic strategies aimed at manipulating Hedgehog pathway activity.
TPB15 is a potent inhibitor of Hedgehog (Hh) signaling, specifically targeting Smoothened (Smo). This compound effectively induces cell cycle arrest and apoptosis in MDA-MB-468 breast cancer cells by blocking Smo translocation into cilia and reducing the expression of Smo protein and mRNA. Additionally, TPB15 downregulates glioma-associated oncogene 1 (Gli1), a key downstream regulator. TPB15 demonstrates significant anti-tumor activity with a favorable toxicity profile, making it a valuable tool for cancer research focused on Hedgehog pathway modulation.
Hedgehog IN-9 is a potent Hedgehog inhibitor that primarily targets the inhibition of GLI1 expression. It has been shown to enhance BRD2 protein levels in cells and effectively inhibit the growth of medulloblastoma spheroid cells. Additionally, Hedgehog IN-9 can be utilized for the synthesis of photoaffinity labeling probes, making it a valuable tool in cancer research and related biochemical applications.
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Robotnikinin is a small molecule inhibitor targeting the Sonic Hedgehog (Shh) signaling pathway by binding to and inhibiting its upstream activator, Smoothened (Smo). This compound demonstrates significant biological activity in modulating Shh-related cellular processes, making it a valuable tool for studying developmental biology and cancer research. Its application may also extend to exploring therapeutic strategies in diseases associated with aberrant Shh signaling.
Hedgehog agonist 1 is a potent Hedgehog (Hh) pathway activator with an EC50 of 0.3 nM. This compound facilitates the modulation of Hh signaling, making it useful for investigating its role in stroke and various neurological disorders. Its ability to activate Hh signaling pathways may provide valuable insights into therapeutic strategies for neurodegenerative conditions.
Hh Pathway-IN-1 is a potent inhibitor of the Hedgehog (Hh) signaling pathway, acting primarily as a Gli antagonist. With an IC50 value of 1.1 µM in C3H10T1/2 cells, it demonstrates significant inhibition of Hh pathway functionality while sparing Wnt signaling. Hh Pathway-IN-1 exhibits anti-proliferative effects and reduces GLI1 mRNA expression, contributing to its efficacy in inhibiting colony formation in a dose-dependent manner. This compound is valuable for research in developmental biology and cancer therapeutics targeting the Hedgehog pathway.