Hedgehog Inhibitor

T-1330 (Compound 45) is a Hh pathway inhibitor and reduces Gli1 expression.

HL2-m5 is the inhibitor for the interaction between sonic hedgehog/patched (Shh/PTCH1) with K_d of 170 nM for Shh. HL2-m5 inhibits activation of Hedgehog signaling pathway and transcription of Gli-controlled gene with an IC₅₀ of 230 nM.

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.

RU-SKI 43 is a potent and selective Hedgehog acyltransferase (Hhat) inhibitor with an IC₅₀ of 850 nM. RU-SKI 43 reduces Gli-1 activation through Smoothened-independent non-canonical signaling and decreases Akt and mTOR pathway activity. RU-SKI 43 has anti-cancer activity.

SANT-1 (GMP) is SANT-1 (HY-100224) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. SANT-1, a potent Smo antagonist, inhibits Hedgehog signaling.

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

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.

SMO-IN-3 (compound 12a) is a potent smoothened (SMO) inhibitor with an IC₅₀ value of 34.09 nM for hedgehog (Hh) signaling pathway. SMO-IN-3 has antiproliferative activity against human medulloblastoma cell line Daoy. Anticancer activity.

Ornidazole-d₅ is deuterium labeled Ornidazole. Ornidazole (Ro 7-0207) is a nitroimidazole derivative with anti-trichomonad activity and in vitro activity against a variety of anaerobic bacteria. Ornidazole inhibits Sonic hedgehog (Shh) signaling pathway, exhibits antitumor activity. Ornidazole can be used in research of Crohn’s disease.

Degalactotigonin is a saponin-selective inhibitor targeting the EGFR, GSK3β and Hedgehog/Gli1 pathways and can be isolated from Solanum nigrum (Solanum nigrum). Degalactotigonin inhibits EGFR phosphorylation and the downstream Akt/ERK signaling pathway, and at the same time inhibits the Hedgehog/Gli1 pathway through GSK3β inactivation, thereby inducing cancer cell apoptosis, arresting the cell cycle, and inhibiting migration and invasion. Degalactotigonin can be used in targeted research on malignant tumors such as pancreatic cancer and osteosarcoma.

Smo antagonist M25 is a smoothened antagonist for inhibition of the hedgehog pathway.

Hedgehog IN-2 (Compound 20) is an inhibitor of Hedgehog pathway with an IC₅₀ value less than 0.003 μM in C3H10T1/2 cells.

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.

Sutherlandioside D is a natural product present in the aerial parts of Sutherlandia frutescens. Sutherlandioside D acts as an inhibitor of the Gli/hedgehog signaling pathway and exhibits reactive oxygen species (ROS) regulatory activity. Sutherlandioside D inhibits Gli reporter gene activity and reduces ROS production. Sutherlandioside D can be used in prostate cancer-related research.

Jervine (Standard) (11-Ketocyclopamine (Standard)) is the analytical standard of Jervine (HY-N0836). This product is intended for research and analytical applications. Jervine (11-Ketocyclopamine) is an orally active steroidal alkaloid and Hedgehog signaling pathway inhibitor. Jervine can be isolated from Veratrum californicum. Jervine regulates Wnt, inhibits the AKT/mTOR signaling pathway, and activates the AMPK signaling pathway. Jervine induces DNA damage, Apoptosis, Autophagy, ROS production and Mitochondrial damage. Jervine exhibits anti-cancer and anti-inflammatory activities. Jervine reduces tumor growth rate and weight in xenograft models. Jervine can be used in studies related to triple-negative breast cancer, nasopharyngeal carcinoma and non-small cell lung cancer.

LAB687 is a microsomal triglyceride transfer protein (MTP) inhibitor with an IC₅₀ of 0.9 nM for apolipoprotein B (apoB) secretion in HepG2 cells. LAB687 also acts as a Smoothened (Smo) antagonist, with IC₅₀ values of 2.48 μM and 3.42 μM against mouse and human Smo receptors, respectively. LAB687 reduces triglyceride and low-density lipoprotein cholesterol (LDL-C) levels, and inhibits the Hedgehog signaling pathway. LAB687 can be used in studies related to Hedgehog-dependent cancers.

SMO-IN-5 ((Compound 25(B31)) is a potent and competitive inhibitor of smoothened (SMO) that can inhibit Hedgehog (Hh) signaling. SMO-IN-5 interacts with Smo through hydrogen bonds, hydrophobic interactions, and electrostatic forces. SMO-IN-5 inhibits PC cell proliferation, migration, and induces apoptosis by suppressing Gli1 expression. SMO-IN-5 exhibits antitumor activity in pancreatic cancer..

IMP-1575 is the most potent Hedgehog acyltransferase (HHAT) inhibitor, with an IC₅₀ of 0.75 μM for inhibition of purified HHAT. IMP-1575 can be used for the research of cancer.

Axl-IN-21 is an orally active and selective AXL inhibitor (K_d = 2.7 nM, IC₅₀ = 4.0 nM). Axl-IN-21 displays kinase selectivity and retains strong activity against cancer-related mul-kinases (Mer with K_d = 1.4 nM, DDR1 with IC₅₀ = 22.2 nM, HIPK4 with K_d = 11.0 nM and LOK with K_d =10 nM). Axl-IN-21 overcomes tumor microenvironment-driven resistance by blocking CAF-derived GAS6-induced AXL/STAT3/ABCG1 signaling, restoring chemosensitivity and inhibiting drug efflux in gastric cancer (GC). Axl-IN-21 suppresses TGF-β1-induced epithelial-mesenchymal transition (EMT), migration, and invasion in MDA-MB-231 cells. Axl-IN-21 exhibits no significant cytotoxicity in non-cancerous cells. Axl-IN-21 can be research for triple negative breast cancer and gastric cancer^{[1] [2]} .

IPI-269609 is an orally effective Smoothed (SMO) inhibitor that targets the Hedgehog (Hh) signaling pathway. IPI-269609 specifically reduces the ALDH-bright (high aldehyde dehydrogenase activity) cell subset, which is considered the "cancer stem cells" in pancreatic cancer. IPI-269609 significantly inhibits the migration and colony formation of pancreatic cancer cells. IPI-269609 effectively inhibits pancreatic cancer metastasis in a mouse model. IPI-269609 can be used for pancreatic cancer research.