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

Hedgehog Inhibitor

Hedgehog Inhibitors (67):

Cat. No. Product Name Effect Purity
  • 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.
  • 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.
  • 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.
  • 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.
  • 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.
  • 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] .
  • 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.
  • 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.
  • 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.
  • 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.
  • 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.
  • 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.
  • 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.
  • HY-13307
    JK184
    		Inhibitor 99.93%
    JK184 is a potent Hedgehog (Hh) pathway inhibitor with IC50 of 30 nM in mammalian cells.
  • HY-15398C
    3-epi-Vitamin D3
    		Inhibitor
    3-epi-Vitamin D3 (Epicholecalciferol) (Compound 4), a Vitamin D3 analogue, is a Hedgehog pathway inhibitor with an IC50 of 39.2 μM measured in U87MG cells.
  • HY-107551
    Hh Pathway-IN-1
    		Inhibitor 99.06%
    Hh Pathway-IN-1, a Hedgehog (Hh) pathway inhibitor, is a potent Gli antagonist. Hh Pathway-IN-1 inhibits Hh pathway functional with an IC50 value of 1.1 µM in C3H10T1/2 cells. Hh Pathway-IN-1 does not inhibit Wnt signaling. Hh Pathway-IN-1 shows anti-proliferative activity. Hh Pathway-IN-1 decreases the GLI1 mRNA expression. Hh Pathway-IN-1 inhibits colony formation in a dose-dependent manner.
  • HY-N0247
    Saikosaponin B1
    		Inhibitor 99.42%
    Saikosaponin B1 is a bioactive constituent of Radix Bupleuri. Saikosaponin B1 is an agonist of the 5-HT2C receptor with an EC50 of 147.41 μM. Saikosaponin B1 inhibits the Hedgehog (Hh) signaling pathway by targeting the transmembrane protein SMO. Sailosaponin B1 can reduce liver fibrosis. Saikosaponin B1 has anti-cancer activities thus can be studies in research for cancers such as Medulloblastoma (MB).
  • HY-158059
    DS-1-38
    		Inhibitor 99.57%
    DS-1-38 is an EYA1 antagonist that blocks Sonic Hedgehog (SHH) signaling. EYA1 is a haloacid dehalogenase phosphatase and transcription factor that regulates tumorigenesis and proliferation in SHH medulloblastoma (SHH-MB).
  • HY-122814
    Hedgehog IN-1
    		Inhibitor 99.0%
    Hedgehog IN-1 (Compound 7d) is an inhibitor for Hedgehog protein with IC50 of 70 nM.
  • 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.