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-17514S1
    Itraconazole-d3
    		≥99.0%
    Itraconazole-d3 is the deuterium labeled Itraconazole (HY-17514)[1].
    Itraconazole-d<sub>3</sub>
  • HY-107408
    SANT 2
    		Antagonist 99.41%
    SANT 2 is a potent antagonist of Hh-signaling pathway. Hedgehog (Hh) signaling plays an important role in cell signaling of embryonic development and adult tissue homeostasis. SANT 2 has the potential for the research of several malignancies including Gorlin syndrome (a disorder predisposing to basal cell carcinoma, medulloblastoma and rhabdomyosarcoma), prostate, pancreatic and breast cancers.
    SANT 2
  • HY-150567
    SMO-IN-3
    		Inhibitor
    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.
    SMO-IN-3
  • HY-153456
    Hedgehog IN-2
    		Inhibitor
    Hedgehog IN-2 (Compound 20) is an inhibitor of Hedgehog pathway with an IC50 value less than 0.003 μM in C3H10T1/2 cells.
    Hedgehog IN-2
  • HY-16475
    TAK-441
    		Inhibitor 98.47%
    TAK-441 is a highly potent and orally active hedgehog (Hh) signaling inhibitor with an IC50value of 4.4 nM. TAK-441 has strong antitumor activity in solid tumors.
    TAK-441
  • HY-162274
    Oxazepine
    Oxazepine (compound 4a) has antimicrobial viability via binding OMPA/ exo-1,3-beta-glucanase proteins. Oxazepine is a hedgehog signaling inhibitor with antitumor viability.
    Oxazepine
  • HY-111040
    Hedgehog agonist 1
    		Agonist 99.83%
    Hh agonist 1 (compound 21k) is a potent Hedgehog (Hh) agonist, with an EC50 0.3 nM. Hh agonist 1 can be used for the research of stroke and other neurological disorders.
    Hedgehog agonist 1
  • HY-162372
    Hedgehog IN-6
    		Inhibitor
    Hedgehog IN-6 (Compound Q29) is a Hedgehog (Hh) inhibitor that can be used in cancer research. Hedgehog IN-6 inhibits the hedgehog (Hh) pathway by binding to the cysteine-rich domain (CRD) of Smoothened (Smo) and blocking its cholesterization.
    Hedgehog IN-6
  • HY-123781A
    RUSKI-201 dihydrochloride
    		Inhibitor
    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.
    RUSKI-201 dihydrochloride
  • HY-150564
    SMO-IN-2
    		Inhibitor
    SMO-IN-2 (compound 1) 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-153457
    Hedgehog IN-3
    		Inhibitor
    Hedgehog IN-3 (compound 3) is a hedgehog pathway inhibitor (IC50 = 0.01 µM). Hedgehog IN-3 can be used in cancer research.
    Hedgehog IN-3
  • HY-N8270
    Physalin H
    		Inhibitor
    Physalin H is a natural product that can be isolated from Solanum nigrum. Physalin H is an inhibitor of Hedgehog (Hh) signaling and it disrupts GLI1-DNA-complex formation. Physalin H inhibits GLI1 transcription with an IC50 value of 0.7 μM. Physalin H shows cytotoxicity to PANC1 and DU145 cells with IC50 values of 5.7 and 6.8 μM, respectively.
    Physalin H
  • HY-108508
    SMANT hydrochloride
    		Inhibitor 99.90%
    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.
    SMANT hydrochloride
  • HY-143400
    HSP70-IN-3
    		Inhibitor
    HSP70-IN-3 is a potent HSP70 inhibitor (IC50s of 1.1 and 1.9 μM in ASZ001 and C3H10T1/2, respectively). HSP70-IN-3 has anti-Hh (Hedgehog signaling) activity and anti-proliferative activity and reduces expression of the oncogenic transcription factor GLI1.
    HSP70-IN-3
  • HY-147670
    TPB15
    		Inhibitor
    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.
    TPB15
  • HY-17514S2
    Itraconazole-d9
    Itraconazole-d9 is the deuterium labeled Itraconazole[1]. 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[2][3][4][5].
    Itraconazole-d<sub>9</sub>
  • 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-120499
    AZD8542
    		Antagonist
    AZD8542 is an antagonist of Smoothened (SMO), playing an important role in oncology. AZD8542 is a? Hedgehog (Hh) pathway antagonist on tumor progression with an emphasis on the role of the stroma compartment.
    AZD8542
  • 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
Cat. No. Product Name / Synonyms Application Reactivity