2. Signaling Pathways
  3. Stem Cell/Wnt
  4. Hedgehog

Hedgehog

Hedgehog

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Hedgehog (Hh) is composed of N-terminal and C-terminal domains that dissociate in a self-catalyzed proteolytic cleavage reaction. The N-terminal product HhNp, modified by cholesterol during self-cleavage, harbors all known Hh signaling activities. When synthesized in the absence of the C-terminal domain (and hence lacking cholesterol modification), the N-terminal domain is aberrantly targeted and released selectively into the retina.

Hedgehog signaling pathway is linked to tumorigenesis and is aberrantly activated in a variety of cancers. Hh ligands bind to and suppress the transmembrane receptor Patched (PTCH), which suppresses Smoothened (SMO), a seven-transmembrane-helix protein that positively regulates the Hh pathway.

Sonic hedgehog (Shh) is a morphogen essential to the developing nervous system that continues to play an important role in adult life by contributing to cell proliferation and differentiation, maintaining blood-brain barrier integrity, and being cytoprotective against oxidative and excitotoxic stress, all features of importance in amyotrophic lateral sclerosis (ALS).

Indian hedgehog (Ihh), a signaling molecule that plays a pivotal role in the regulation of chondrocyte proliferation, maturation, and ossification both in long-bone development and digit joint formation, has also been found to be essential for temporomandibular joint (TMJ) development.

Desert hedgehog (Dhh), one of the Hedgehog family members, is expressed by Schwann cells of peripheral nerves.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-153730
    Hedgehog IN-5
    		Inhibitor
    Hedgehog IN-5 is an orally active small molecule inhibitor of the hedgehog pathway. Hedgehog IN-5 can be used for the research of fibrotic disease.
    Hedgehog IN-5
  • HY-148440
    RL-0070933
    		Modulator
    RL-0070933 is a potent smo cilial modulator with an EC50 value of 0.02 µM. RL-0070933 modulates the translocation and/or accumulation of smoothened to the primary cilia by hedgehog signaling pathway.
    RL-0070933
  • HY-122017
    Methoxy-SANT-2
    		Antagonist
    Methoxy-SANT-2 (TC-132) is a potent hedgehog antagonist with an IC50 value of 79.8 nM. Methoxy-SANT-2 inhibits the Gli1 reporter gene expression. Methoxy-SANT-2 has the potential for the research of cancer.
    Methoxy-SANT-2
  • HY-100224G
    SANT-1 (GMP)
    		Inhibitor
    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.
    SANT-1 (GMP)
  • HY-10440R
    Vismodegib (Standard)
    		Inhibitor
    Vismodegib (Standard) is the analytical standard of Vismodegib. This product is intended for research and analytical applications. 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.
    Vismodegib (Standard)
  • HY-B0508R
    Ornidazole (Standard)
    		Inhibitor
    Ornidazole (Standard) is the analytical standard of Ornidazole. This product is intended for research and analytical applications. 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.
    Ornidazole (Standard)
  • HY-W838042
    Hedgehog IN-8
    		Inhibitor
    Hedgehog IN-8 effectively inhibits hedgehog signaling and phosphodiesterase activity.
    Hedgehog IN-8
  • HY-123752
    MS-0022
    		Antagonist
    MS-0022 is a Smoothened (SMO) antagonist. MS-0022 can inhibit the Hedgehog (Hh) signaling pathway. MS-0022 can be used in anti-tumor research.
    MS-0022
  • HY-117903A
    MRT-92
    		Inhibitor
    MRT-92 is a Smoothened (Smo) antagonist (Ki=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.
    MRT-92
  • HY-172449
    GLI1-IN-3
    		Inhibitor
    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.
    GLI1-IN-3
  • HY-156814
    HPP-9
    		Inhibitor
    HPP-9 is a Proteolysis-Targeting Chimeras （PROTACs） based on Hedgehog Pathway Inhibitor-1 (HPI-1), with the pIC50 of 6.71, that can degrade BET bromodomains. HPP-9 has antitumor activity[1[.
    HPP-9
  • HY-150564
    SMO-IN-2
    		Inhibitor 98.12%
    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.
    SMO-IN-2
  • HY-17514R
    Itraconazole (Standard)
    		Antagonist
    Itraconazole (Standard) is the analytical standard of Itraconazole. This product is intended for research and analytical applications. Itraconazole (R51211) is a triazole antifungal agent and a potent and orally active Hedgehog (Hh) signaling pathway antagonist with an IC50 of ~800 nM. Itraconazole potently inhibits lanosterol 14α-demethylase (cytochrome P450 enzyme), thereby inhibits the oxidative conversion of lanosterol to ergosterol. Itraconazole has anticancer and antiangiogenic effects. Itraconazole is a oxysterol-binding protein (OSBP) inhibitor.
    Itraconazole (Standard)
  • HY-W705354
    Vismodegib-d4
    		Inhibitor
    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.
    Vismodegib-d<sub>4</sub>
  • HY-123781
    RUSKI-201
    		Inhibitor
    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.
    RUSKI-201
  • HY-120664
    BRD50837
    		Inhibitor
    BRD50837 is a potent inhibitor of Sonic Hedgehog (Shh), with the EC50 of 0.09 μM. BRD50837 plays an important role in cancer research.
    BRD50837
Cat. No. Product Name / Synonyms Application Reactivity