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-N6954R
    Garcinone C (Standard)
    		Inhibitor
    Garcinone C (Standard) is the analytical standard of Garcinone C. This product is intended for research and analytical applications. 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 (Standard)
  • 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-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-14115
    Hedgehog IN-10
    		Inhibitor
    Hedgehog IN-10 (compound 24) is a potent Hedgehog inhibitor. Hedgehog IN-10 exhibits significant antitumor effect.
    Hedgehog IN-10
  • HY-175299
    Hedgehog IN-11
    		Inhibitor
    Hedgehog IN-11 is an orally active Hedgehog inhibitor. Hedgehog IN-11 downregulates the expression of O6-methylguanine-DNA methyltransferase (MGMT) to impair the Temozolomide (TMZ) (HY-17364) resistance by inhibiting the Hedgehog pathway. Hedgehog IN-11 shows improved inhibition of cell migration and invasion, and induced cell apoptosis in TMZ-resistant GBM cell lines. Hedgehog IN-11 is predicted by computer simulation to have good blood-brain barrier penetration. Hedgehog IN-11 can be used for the study of glioblastoma (GBM).
    Hedgehog IN-11
  • 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-176056
    Hedgehog IN-9
    		Inhibitor
    Hedgehog IN-9 (Compound 1) is a Hedgehog inhibitor. Hedgehog IN-9 prevents GLI1 expression and enhances cellular BRD2 protein levels. Hedgehog IN-9 inhibits growth of medulloblastoma spheroid cells and can be used for synthesis of photoaffinity labeling probe.
    Hedgehog IN-9
  • HY-P992409
    MEDI-5304
    		Inhibitor
    MEDI-5304 is a hedgehog antibody inhibitor with human sonic hedgehog (SHH) KD of 5.13 pmol/L, and human Indian hedgehog (IHH) KD of 34.7 pmol/L. MEDI-5304 binds and neutralizes SHH and IHH, blocks downstream target gene transcription, inhibits osteoblast differentiation. MEDI-5304 can be used for the research of colon cancer.
    MEDI-5304
  • 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-182721
    Pipinib
    		Inducer
    Pipinib is an ATP-competitive and selective phosphatidylinositol 4-kinase IIIb (PI4KB) inhibitor with an IC50 of 2.2 μM. Pipinib reduces intracellular PI4P levels. Pipinib inhibits GLI-mediated transcription, the expression of Hedgehog target genes, and blocks the trafficking of Smoothened to cilia. Pipinib can be used in the research of basal cell carcinoma and medulloblastoma.
    Pipinib
  • 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-159511
    Hedgehog IN-7
    		Inhibitor
    Hedgehog IN-7 (Compound 8g), a purine derivative, acts as an inhibitor of Hedgehog, capable of reducing the expression of Hedgehog genes and inhibiting Hedgehog signaling. Hedgehog IN-7 has significant cytotoxicity and selectivity towards the Hedgehog pathway-dependent pancreatic cancer cell Mia-PaCa-2 cells and can be used in the research of pancreatic cancer.
    Hedgehog IN-7
  • HY-B0508S1
    Ornidazole-13C2,15N2
    		Inhibitor
    Ornidazole-13C2,15N2 is the 13C, 15N 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.
    Ornidazole-<sup>13</sup>C<sub>2</sub>,<sup>15</sup>N<sub>2</sub>
  • HY-117485
    CBR-096-4
    		Inhibitor
    CBR-096-4 is a derivative of Itraconazole (HY-17514). CBR-096-4 is an orally active antifibrotic agent with no CYP3A4 inhibitory activity. CBR-096-4 inhibits the formation of matrix-secreting activated myofibroblasts (MFBs) from multiple tissue types. CBR-096-4 inhibits Hedgehog reporter activity (GLI-LUC), VEGF-dependent growth, and αSMA-LUC reporter activity. CBR-096-4 can be used for research of fibrosis.
    CBR-096-4
  • 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-153500
    Hedgehog IN-4
    		Inhibitor
    Hedgehog IN-4 is a benzamide derivative and also an inhibitor of the Hedgehog signaling pathway, with an IC50 of 0.050 nM.
    Hedgehog IN-4
  • HY-108439R
    Neurodazine (Standard)
    		Activator
    Neurodazine (Standard) is the analytical standard of Neurodazine (HY-108439). This product is intended for research and analytical applications. Neurodazine is a neurogenic inducer, serve as a promoter of neurogenesisin pluripotent cells. Neurodazine promotes neurogenesis by activating Wnt and Shh signaling pathways..
    Neurodazine (Standard)
  • 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 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 (Standard)
Cat. No. Product Name / Synonyms Application Reactivity