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
    		99.62%
    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-113081AS
    1-Methyladenosine-d3 hydrochloride
    		Activator
    1-Methyladenosine-d3 hydrochloride is the hydrochloride salt form of deuterium labeled 1-Methyladenosine (HY-113081). 1-Methyladenosine is an RNA modification that can serve as a tumor marker, with elevated levels in the body associated with cancer development. Following 1-methyladenosine methylation, upregulation of PPARδ expression regulates cholesterol metabolism and activates Hedgehog signaling pathway, driving liver tumorigenesis.
    1-Methyladenosine-d<sub>3</sub> hydrochloride
  • HY-100036
    MK-4101
    		Inhibitor 98.31%
    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.
    MK-4101
  • HY-18366
    RU-SKI 43
    		Inhibitor
    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.
    RU-SKI 43
  • HY-113965
    CUR61414
    		Inhibitor 99.04%
    CUR61414 is a novel, potent and cell permeable Hedgehog signaling pathway inhibitor (IC50 =100-200 nM). CUR61414 is a small-molecule aminoproline class compound and selectively binds to smoothened (Smo) with a Ki  value of 44 nM. CUR-61414 can induce apoptosis in cancer cells without affecting neighboring non-tumor cells.
    CUR61414
  • HY-17514S
    Itraconazole-d5
    		Antagonist 99.55%
    Itraconazole-d5 is the deuterium labeled Itraconazole. 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[1][2][3].
    Itraconazole-d<sub>5</sub>
  • 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-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-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-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-161459
    GLI1-IN-1
    		Inhibitor
    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.
    GLI1-IN-1
  • HY-122814
    Hedgehog IN-1
    		Inhibitor
    Hedgehog IN-1 (Compound 7d) is an inhibitor for Hedgehog protein with IC50 of 70 nM.
    Hedgehog IN-1
  • HY-17024R
    Cyclopamine (Standard)
    		Antagonist
    Cyclopamine (Standard) is the analytical standard of Cyclopamine. This product is intended for research and analytical applications. Cyclopamine is a Hedgehog (Hh) pathway antagonist with an IC50 of 46 nM in the Hh cell assay. Cyclopamine is also a selective Smo inhibitor.
    Cyclopamine (Standard)
  • HY-161175
    IMP-1575
    		Inhibitor
    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.
    IMP-1575
  • 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-113081R
    1-Methyladenosine (Standard)
    		Activator
    1-Methyladenosine (Standard) is the analytical standard of 1-Methyladenosine. This product is intended for research and analytical applications. 1-Methyladenosine is an RNA modification that can serve as a tumor marker, with elevated levels in the body associated with cancer development. Following 1-methyladenosine methylation, upregulation of PPARδ expression regulates cholesterol metabolism and activates Hedgehog signaling pathway, driving liver tumorigenesis. In Vitro:Compared to surrounding tumor tissues, 1-methyladenosine methylation in RNA is aberrantly elevated in hepatocellular carcinoma (HCC) cell lines and liver cancer stem cells (CSCs). Methylated 1-methyladenosine can promote cholesterol synthesis and activate the Hedgehog signaling pathway by enhancing the translation of PPARδ in liver CSCs, ultimately driving the self-renewal and tumorigenesis of liver cancer stem cells.
    1-Methyladenosine (Standard)
  • 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
Cat. No. Product Name / Synonyms Application Reactivity