Gli

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.

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.

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.

Glaucocalyxin A is an ent-kauranoid diterpene derived from Rabdosia japonica var. This compound acts as an apoptosis inducer by inhibiting the nuclear translocation of Five-zinc finger Glis 1 (GLI1), effectively modulating the PI3K/Akt signaling pathway. Its notable antitumor properties make Glaucocalyxin A a valuable reagent for research in cancer biology, particularly in studies focused on osteosarcoma.

Degalactotigonin is a saponin-selective inhibitor that targets key pathways, including EGFR, GSK3β, and Hedgehog/Gli1. It effectively inhibits EGFR phosphorylation and the downstream Akt/ERK signaling pathway, while also disrupting the Hedgehog/Gli1 pathway through the inactivation of GSK3β. These actions result in the induction of apoptosis in cancer cells, cell cycle arrest, and inhibition of cell migration and invasion. Degalactotigonin is suitable for research focused on malignant tumors, particularly pancreatic cancer and osteosarcoma.

Adropin (34-76) is a secretory fragment of the Adropin protein known for its role as a hypoglycemic agent. This compound effectively reduces cAMP levels and inhibits glucose production in hepatocytes, contributing to its hypoglycemic effect. Additionally, Adropin (34-76) demonstrates antifibrotic properties through the inhibition of the GLI1 signaling pathway, making it valuable for research in metabolic regulation and fibrosis-related studies.

NL-103 is a potent histone deacetylase (HDAC) inhibitor, exhibiting IC50 values of 21.3 nM, 57 nM, 74 nM, and 680 nM for HDAC1, HDAC2, HDAC3, and HDAC6, respectively. This compound also targets the Hedgehog signaling pathway, leading to the downregulation of Gli2 expression. NL-103 is primarily utilized in cancer research, providing valuable insights into HDAC regulation and its role in tumor biology.

GLI1-IN-1 is a potent inhibitor of GLI-1, effectively targeting the Hedgehog (HH) signaling pathway with an IC50 of 1.3 μM. This compound demonstrates significant anticancer activity, inducing apoptosis and inhibiting growth in colorectal cancer cells. GLI1-IN-1’s excellent water solubility enhances its applicability for various research studies focused on cancer biology and therapeutic interventions.

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.

SANT 2 is a potent antagonist of the Hedgehog (Hh) signaling pathway, specifically inhibiting the expression of Gli1. This compound has been shown to induce developmental delays in medaka embryos, making it a valuable tool for studying embryonic development. SANT 2 has significant research applications in various malignancies, including Gorlin syndrome, as well as prostate, pancreatic, and breast cancers, thereby aiding in the exploration of targeted therapies for these conditions.

T-1330 is an inhibitor of the Hedgehog (Hh) signaling pathway, specifically targeting the downstream effector Gli1. By effectively reducing Gli1 expression, T-1330 plays a crucial role in modulating Hh pathway activity. This compound is useful in research applications related to developmental biology and cancer therapy, particularly in studies investigating aberrant Hh signaling in various malignancies.

Physalin H is a bioactive compound extracted from Solanum nigrum, functioning as a Hedgehog (Hh) signaling inhibitor. It effectively disrupts GLI1-DNA complex formation and inhibits GLI1 transcription with an IC50 of 0.7 μM. Additionally, Physalin H exhibits cytotoxic effects on PANC1 and DU145 cancer cell lines, demonstrating IC50 values of 5.7 μM and 6.8 μM, respectively. This compound is valuable for research into Hh pathway modulation and cancer therapeutics.

Methoxy-SANT-2 is a potent Hedgehog pathway antagonist, demonstrating an IC50 value of 79.8 nM. It effectively inhibits Gli1 reporter gene expression, making it a valuable tool in investigating Hedgehog signaling. This compound is suitable for research applications focused on cancer biology and therapeutic strategies targeting the Hedgehog pathway.

Prostaglandin E1 ethanolamide is a prostaglandin analog that primarily targets the GLI2 signaling pathway. This compound has been shown to inhibit GLI2-induced expression of downstream genes such as Gli1 and Ptch1, demonstrating its potential in regulating tumor growth. As a valuable tool for cancer research, Prostaglandin E1 ethanolamide may facilitate investigations into therapeutic strategies that disrupt GLI2-mediated oncogenic processes.

Glabrescione B is a Gli1-DNA interaction inhibitor that targets the Hedgehog (Hh) signaling pathway. This compound disrupts the activity of Gli1 by preventing its binding to DNA, thereby inhibiting the growth of Hedgehog-dependent tumor cells. Additionally, Glabrescione B impairs the self-renewal capacity and clonogenic potential of tumor-derived stem cells, making it a valuable tool for studying Hh-related cancers and stem cell biology.