Hedgehog

Cyclopamine is a Smo or hedgehog signaling pathway inhibitor.

TAK-441 is a pyrrolo[3,2-c]pyridine derivative, as a highly potent and orally active hedgehog signaling inhibitor.

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.

RU-SKI 43 is a small molecule inhibitor of Hhat(Hedgehog acyltransferase), the enzyme responsible for the attachment of palmitate onto Shh.

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.

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.

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.

3-epi-Vitamin D3, also known as Epicholecalciferol, functions as a Hedgehog pathway inhibitor, exhibiting an IC50 value of 39.2 μM in U87MG cell lines. This Vitamin D3 analogue is useful in studies investigating the modulation of the Hedgehog signaling pathway, which plays a critical role in cellular growth and differentiation. 3-epi-Vitamin D3 may have potential applications in cancer research, particularly in contexts where Hedgehog dysregulation is implicated.

Hedgehog IN-1 is a potent inhibitor of the Hedgehog signaling pathway, demonstrating an IC50 of 70 nM. This compound effectively blocks Hedgehog protein activity, making it valuable for research into developmental biology and cancer therapeutics. Hedgehog IN-1 is instrumental in studies aimed at understanding the role of the Hedgehog pathway in tumorigenesis and potential therapeutic applications in related disorders.

Hedgehog IN-2 is a potent inhibitor of the Hedgehog signaling pathway, exhibiting an IC50 value of less than 0.003 μM in C3H10T1/2 cells. This compound effectively disrupts Hedgehog-mediated cellular signaling, making it a valuable tool for studying embryonic development, cancer biology, and regenerative medicine. Its high potency and specificity enable researchers to investigate the role of the Hedgehog pathway in various biological processes and disease states.

Hedgehog IN-6 is a potent Hedgehog (Hh) inhibitor that targets the Hh signaling pathway by binding to the cysteine-rich domain (CRD) of Smoothened (Smo). By obstructing the cholesterization of Smo, Hedgehog IN-6 effectively inhibits Hh pathway activation, which is crucial in various cancer types. This compound is valuable for research applications aimed at understanding and manipulating Hh signaling in oncogenesis and developmental biology.

HPP-9 is a Hedgehog Pathway inhibitor designed as a Proteolysis-Targeting Chimera (PROTAC) that effectively degrades BET bromodomains. With a pIC50 of 6.71, HPP-9 exhibits significant antitumor activity. This compound is valuable for research applications focused on cancer biology and the modulation of the Hedgehog signaling pathway.

Hedgehog IN-3 is a potent inhibitor of the Hedgehog signaling pathway, exhibiting an IC50 of 0.01 µM. This compound is primarily utilized in cancer research to investigate the role of Hedgehog-mediated signaling in tumorigenesis and cellular proliferation. Its effectiveness in modulating this pathway makes it a valuable tool for studying various malignancies and developing targeted therapeutic strategies.

Hedgehog IN-10 is a potent inhibitor of the Hedgehog signaling pathway, targeting essential components in cellular signaling. This compound demonstrates significant antitumor activity, making it a valuable tool for cancer research. Its ability to modulate Hedgehog signaling contributes to investigations into therapeutic strategies for tumors associated with dysregulated Hedgehog pathway activity.

Hedgehog IN-5 is a small molecule inhibitor that targets the Hedgehog signaling pathway. This orally active compound is primarily employed in research pertaining to fibrotic diseases, providing valuable insights into the mechanisms underlying this condition. Its ability to modulate Hedgehog pathway activity makes it a significant tool for exploring therapeutic strategies in related biological contexts.

Hedgehog IN-4 is a potent inhibitor of the Hedgehog signaling pathway, acting as a benzamide derivative with an IC50 of 0.050 nM. It effectively disrupts Hedgehog-mediated cellular processes, making it valuable for research on developmental biology, cancer, and regenerative medicine. Its ability to modulate this critical pathway allows for exploration into the mechanisms of diseases associated with Hedgehog signaling dysregulation.