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-17024
    Cyclopamine
    		Antagonist 99.97%
    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
  • HY-10440
    Vismodegib
    		Inhibitor 99.97%
    Vismodegib (GDC-0449) is a BBB-permeable and 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
  • HY-17514
    Itraconazole
    		Antagonist 99.59%
    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
  • HY-100224
    SANT-1
    		Inhibitor 99.87%
    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.
    SANT-1
  • HY-122632
    Ciliobrevin D
    		Inhibitor 99.37%
    Ciliobrevin D is a cell-permeable, reversible and specific inhibitor of AAA+ ATPase motor cytoplasmic dynein. Ciliobrevin D inhibits Hedgehog (Hh) signaling and primary cilia formation. Ciliobrevin D inhibits dynein-dependent microtubule gliding and ATPase activity in vitro.
    Ciliobrevin D
  • HY-N9684
    Degalactotigonin
    		Inhibitor
    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.
    Degalactotigonin
  • HY-183335
    SMO-IN-6
    		Inhibitor
    Anticancer agent 321 is a Smoothened (SMO) inhibitor with a human IC50 of 0.12 μM, enhanced aqueous solubility, good plasma and metabolic stability, moderate therapeutic index, preliminary safety profile, and moderate oral bioavailability in rats.Anticancer agent 321 binds to SMO’s 7-transmembrane helical channel, forming hydrogen bonds with Asp384 and hydrophobic/π-π interactions with His470, Phe391, Tyr394, stabilizing SMO’s inactive conformation to inhibit Hedgehog/GLI signaling.Anticancer agent 321 inhibits proliferation, suppresses colony formation, induces apoptosis, and downregulates Hedgehog/GLI pathway target genes GLI1, GLI2, Ptch1, HHip in cancer cells.Anticancer agent 321 inhibits tumor growth, downregulates Ki67 and SOX2, and upregulates cleaved-caspase 3 in tumor tissues.Anticancer agent 321 can be used for the research of cutaneous squamous cell carcinoma.
    SMO-IN-6
  • HY-179535
    Axl-IN-21
    		Inhibitor
    Axl-IN-21 is an orally active and selective AXL inhibitor (Kd = 2.7 nM, IC50 = 4.0 nM). Axl-IN-21 displays kinase selectivity and retains strong activity against cancer-related mul-kinases (Mer with Kd = 1.4 nM, DDR1 with IC50 = 22.2 nM, HIPK4 with Kd = 11.0 nM and LOK with Kd =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] .
    Axl-IN-21
  • HY-113081
    1-Methyladenosine
    		Activator 99.92%
    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
  • HY-121802
    Dynarrestin
    		Inhibitor 98.18%
    Dynarrestin is a aminothiazole inhibitor of cytoplasmic dyneins 1 and 2. Dynarrestin rapidly and reversibly inhibits dynein 1-driven microtubule gliding in vitro plus a range of dynein 1- and 2-dependent processes in cells without affecting ATP hydrolysis and interfering with ciliogenesis. Dynarrestin suppresses hedgehog (Hh)-dependent proliferation of neuronal precursors and tumor cells.
    Dynarrestin
  • HY-100790
    Ciliobrevin A
    		Inhibitor 98.57%
    Ciliobrevin A (HPI-4) is a hedgehog (Hh) signaling pathway inhibitor with median inhibitory concentration (IC50) less than 10 μM.
    Ciliobrevin A
  • HY-N6954
    Garcinone C
    		Inhibitor 99.51%
    Garcinone C, a xanthone derivative, is a natural compound extracted from Garcinia oblongifolia that is used as an anti-inflammatory, astringency and granulation-promoting medicine, and has potential cytotoxic effects on certain cancers. Garcinone C stimulates the expression levels of ATR and 4E-BP1, arrests the cell cycle, inhibits cell viability of the human Nasopharyngeal carcinoma (NPC) cell lines CNE1, CNE2, HK1 and HONE1 in a time‑ and dose‑dependent manner through inhibition of Hedgehog signaling pathway. Garcinone C is orally active.
    Garcinone C
  • HY-B0508
    Ornidazole
    		Inhibitor 99.49%
    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
  • HY-18366A
    RU-SKI 43 hydrochloride
    		Inhibitor 98.81%
    RU-SKI 43 hydrochloride is a potent and selective Hedgehog acyltransferase (Hhat) inhibitor with an IC50 of 850 nM. RU-SKI 43 hydrochloride reduces Gli-1 activation through Smoothened-independent non-canonical signaling and decreases Akt and mTOR pathway activity. RU-SKI 43 hydrochloride has anti-cancer activity.
    RU-SKI 43 hydrochloride
  • HY-100515
    Robotnikinin
    		Inhibitor 98.98%
    Robotnikinin is a small molecule capable of binding to and inhibiting the activity of Sonic Hedgehog (Shh) signaling up stream of Smo.
    Robotnikinin
  • HY-124899
    Hh-Ag1.5
    		Agonist 99.90%
    Hh-Ag1.5 (SAg1.5) is a potent Hedgehog (Hh) agonist with an EC50 of 1 nM. Hh-Ag1.5 mediated reprogramming breaks the quiescence of noninjured liver stem cells for rescuing liver failure.
    Hh-Ag1.5
  • HY-12317
    GSA-10
    		Modulator ≥98.0%
    GSA-10 is a potent smooth (Smo) receptor agonist. GSA-10 is a potent osteogenic molecule. GSA-10 can mediate Hedgehog (Hh) signaling. GSA-10 can be used in regenerative medicine for cancer disease and in the study of fat development.
    GSA-10
  • HY-N0836
    Jervine
    		Inhibitor 99.28%
    Jervine (11-Ketocyclopamine) is a potent Hedgehog (Hh) inhibitor with an IC50 of 500-700 nM. Jervine is a natural teratogenic sterodial alkaloid from rhizomes of Veratrum nigrum. Jervine has anti-inflammatory and antioxidant properties.
    Jervine
  • HY-111040
    Hedgehog agonist 1
    		Agonist 98.78%
    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-13307
    JK184
    		Inhibitor 99.93%
    JK184 is a potent Hedgehog (Hh) pathway inhibitor with IC50 of 30 nM in mammalian cells.
    JK184
Cat. No. Product Name / Synonyms Application Reactivity