Gli Inhibitor

GANT 61 is an inhibitor of Gli1 and Gli2 targeting the Hedgehog/GLI pathway.

Adropin (34-76) is a secretory domain of Adropin. Adropin (34-76) can inhibit cAMP level and glucose production in hepatocytes, and has a hypoglycemic effect. Adropin (34-76) plays an antifibrotic role by inhibiting the GLI1 signaling pathway.

Taladegib is a Smoothened (SMO) antagonist. Taladegib hydrochloride inhibits the Hedgehog signaling pathway, with an IC₅₀ of 5.5 nM for suppressing GLI1 mRNA expression in DAOY cells and an IC₅₀ of 7.6 nM in CGNP cell proliferation assays. Taladegib binds to the extracellular loop region (site 1) of the transmembrane domain of the SMO receptor, competes with cyclopamine for SMO binding, and thereby inhibits Gli-dependent transcription. Taladegib can be used in studies of Hedgehog pathway-related cancers.

Glabrescione B is the first compound that binds the Hedgehog (Hh) modulator Gli1. Glabrescione B impairs its activity by interfering with Gli1-DNA interaction. Glabrescione B inhibits the growth of Hedgehog-dependent tumor cells, the self-renewal ability, and clonogenicity of tumor-derived stem cells.

Anticancer agent 321 is a Smoothened (SMO) inhibitor with a human IC₅₀ of 0.12 μM, enhanced aqueous solubility, good plasma and metabolic stability, moderate therapeutic index, preliminary safety profile, and moderate oral bioavailability in rats.Anticancer agent 321 binds to SMO’s 7-transmembrane helical channel, forming hydrogen bonds with Asp384 and hydrophobic/π-π interactions with His470, Phe391, Tyr394, stabilizing SMO’s inactive conformation to inhibit Hedgehog/GLI signaling.Anticancer agent 321 inhibits proliferation, suppresses colony formation, induces apoptosis, and downregulates Hedgehog/GLI pathway target genes GLI1, GLI2, Ptch1, HHip in cancer cells.Anticancer agent 321 inhibits tumor growth, downregulates Ki67 and SOX2, and upregulates cleaved-caspase 3 in tumor tissues.Anticancer agent 321 can be used for the research of cutaneous squamous cell carcinoma.

GLI-IN-1 is a potent, PKC-dependent Gli inhibitor. GLI-IN-1 binds to the C1 domain of PKC, forms hydrogen-bonding interactions with the M239 residue, and mediates the inhibition of downstream Gli via a PKC-mediated, Smoothened-independent mechanism. GLI-IN-1 can be used in studies of Gli-driven cancers and osteogenic differentiation.

GLI1-IN-1 (CBC-1) is a GLI-1 inhibitor with excellent water solubility and anticancer activity. GLI1-IN-1 can induce apoptosis and suppress the growth of colorectal cancer by inhibiting the Hedgehog(HH) (IC₅₀=1.3 μM) pathway.

NL-103 is an inhibitor of histone deacetylases (HDACs) and Hedgehog, with the IC₅₀ values ​​of 21.3 nM, 57 nM, 74 nM, and 680 nM for HDAC1, HDAC2, HDAC3, and HDAC6, respectively. NL-103 can downregulate the expression of Gli2. NL-103 can be used in anti-cancer research.

Hedgehog IN-9 (Compound 1) is a Hedgehog inhibitor. Hedgehog IN-9 prevents GLI1 expression and enhances cellular BRD2 protein levels. Hedgehog IN-9 inhibits growth of medulloblastoma spheroid cells and can be used for synthesis of photoaffinity labeling probe.

TPB15 is an orally active and potent Hh (Hedgehog) signaling inhibitor. TPB15 markedly induces cell cycle arrest and apoptosis in MDA-MB-468 cells. TPB15 blocks Smo (Smoothened) translocation into the cilia and reduced Smo protein and mRNA expression. TPB15 inhibits the expression of the downstream regulatory factor glioma-associated oncogene 1 (Gli1). TPB15 shows good anti-tumor activity with low toxicity.

Taladegib (LY2940680) hydrochloride is a Smoothened (SMO) antagonist. Taladegib hydrochloride inhibits the Hedgehog signaling pathway, with an IC₅₀ of 5.5 nM for suppressing GLI1 mRNA expression in DAOY cells and an IC₅₀ of 7.6 nM in CGNP cell proliferation assays. Taladegib hydrochloride binds to the extracellular loop region (site 1) of the transmembrane domain of the SMO receptor, competes with cyclopamine for SMO binding, and thereby inhibits Gli-dependent transcription. Taladegib hydrochloride can be used in studies of Hedgehog pathway-related cancers.

GANT 61 (Standard) is the analytical standard of GANT 61. This product is intended for research and analytical applications. GANT 61 is an inhibitor of Gli1 and Gli2 targeting the Hedgehog/GLI pathway.