Hedgehog Inhibitor

Hedgehog IN-8 effectively inhibits hedgehog signaling and phosphodiesterase activity.

MK-4101 (Standard) is the analytical standard of MK-4101 (HY-100036). This product is intended for research and analytical applications. MK-4101 is a Smoothened (SMO) antagonist (IC50 of 1.1 μM for 293 cells ) and also a potent inhibitor of the hedgehog pathway (IC50 of 1.5 μM for mouse cells; IC50 of 1 μM for KYSE180 oesophageal cancer cells). MK-4101 has robust antitumor activity that inhibits tumor cell proliferation and induces extensive apoptosis.

MRT-92 is a Smoothened (Smo) antagonist (K_i=0.7 nM) with anticancer activity. MRT-92 inhibits Hedgehog signaling pathway and rodent cerebellar granule cell proliferation by blocking overlapping binding sites in the transmembrane domain of the Smoothened receptor (IC₅₀=0.4 nM). MRT-92 can be used in the study of cerebellar glioma.

GLI1-IN-3 (Compound 11a), a triterpenoid analogue, can inhibit Hedgehog signaling in GLI1 overexpression cancer cells. GLI1-IN-3 inhibits the proliferation in NSCLC and prostate cancer cell lines exhibiting hyper-activated Hh signaling. GLI1-IN-3 can also decrease the expression of endogenous GLI1 protein and its target genes associated with tumor progression and proliferation in A549 and DU-145 cancer cells.

MDB5 is a Hedgehog pathway and Smoothened inhibitor that binds to the 7-TM domain of Smo. MDB5 reduces hepatic stellate cell activation, extracellular matrix-related gene expression, collagen deposition, hydroxyproline content and epithelial-mesenchymal transition, and prevents sinusoidal endothelial cell capillarization. MDB5 induces G1 and S phase cell cycle arrest, triggers apoptosis by upregulating Bax and downregulating Bcl-2, and also decreases oxygen consumption rate, glucose uptake, transglutaminase activity and fibronectin matrix assembly. MDB5 reduces the levels of liver injury markers, hepatic triglyceride deposition and hepatic steatosis, restores the tissue structure of the kidney and spleen, and inhibits pancreatic tumor growth without causing body weight loss. MDB5 can be loaded into PEG-PCC-g-DC micelles, achieving high drug loading, sustained release, improved water solubility, enhanced cellular uptake and optimized hepatic distribution, with good tolerance in mice. MDB5 is applicable to research related to alcohol-associated liver disease, liver fibrosis and pancreatic cancer.

SMO-IN-2 is a potent smoothened (SMO) inhibitor with an IC₅₀ value of 123.4 nM for hedgehog (Hh) signaling pathway. SMO-IN-2 has antiproliferative activity against human medulloblastoma cell line Daoy. Anticancer activity.

Vismodegib-d₄ is deuterium labeled Vismodegib. Vismodegib (GDC-0449) is an orally active hedgehog pathway inhibitor with an IC₅₀ of 3 nM. Vismodegib also inhibits P-gp, ABCG2 with IC₅₀ values of 3.0 μM and 1.4 μM, respectively.

SANT-1 (Standard) is the analytical standard of SANT-1 (HY-100224). This product is intended for research and analytical applications. SANT-1, a potent Smo antagonist, inhibits Hedgehog signaling. SANT-1 shows IC50s of 20 nM and 30 nM in Shh-LIGHT2 and SmoA1-LIGHT2 assay, respectively.

RUSKI-201 is a potent and specific Hedgehog acyltransferase (Hhat) inhibitor, with an IC₅₀ of 0.20 μM. RUSKI-201 is able to block Hh signaling from Shh overexpressing cells and inhibits Hh palmitoylation. RUSKI-201 is potential Hhat chemical probe in cells and can used in studies of Hhat catalytic function.

BRD50837 is a potent inhibitor of Sonic Hedgehog (Shh), with the EC₅₀ of 0.09 μM. BRD50837 plays an important role in cancer research.

SMANT hydrochloride (Standard) is the analytical standard of SMANT (hydrochloride) (HY-108508). This product is intended for research and analytical applications. SMANT hydrochloride is a Smoothened (Smo) signaling inhibitor. SMANT hydrochloride is antagonist of Smo accumulation within the primary cilium (PC). SMANT hydrochloride has an equivalent activity in inhibiting SmoM2 (oncogenic form of Smo) and wild-type Smo.