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Hh

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97

Inhibitors & Agonists

1

Biochemical Assay Reagents

1

Peptides

1

Inhibitory Antibodies

11

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3

Recombinant Proteins

4

Isotope-Labeled Compounds

11

Antibodies

3

Oligonucleotides

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-17514
    Itraconazole
    20+ Cited Publications

    R51211

    Fungal Hedgehog Cytochrome P450 Autophagy Antibiotic Bacterial Infection Cancer
    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-17024
    Cyclopamine
    Maximum Cited Publications
    55 Publications Verification

    11-Deoxojervine

    Hedgehog Smo Endogenous Metabolite Cancer
    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-122632
    Ciliobrevin D
    4 Publications Verification

    Hedgehog Cancer
    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-121802
    Dynarrestin
    4 Publications Verification

    Hedgehog Cancer
    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-124899
    Hh-Ag1.5
    1 Publications Verification

    SAg1.5

    Hedgehog Metabolic Disease
    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-N0836
    Jervine
    3 Publications Verification

    11-Ketocyclopamine

    Hedgehog Smo Inflammation/Immunology Cancer
    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-12848C
    SAG dihydrochloride
    35+ Cited Publications

    Smo Cancer
    SAG dihydrochloride is a potent Smoothened (Smo) receptor agonist (EC50=3 nM; Kd=59 nM). SAG dihydrochloride activates the Hedgehog signaling pathway and counteracts Cyclopamine (HY-17024) inhibition of Smo .
    SAG dihydrochloride
  • HY-16587

    IPI-926; Patidegib

    Smo Cancer
    Saridegib is a potent and specific inhibitor of Smoothened (Smo), a key signaling transmembrane protein in the Hedgehog (Hh) pathway.
    Saridegib
  • HY-B0274
    Chlorprothixene
    2 Publications Verification

    Dopamine Receptor Histamine Receptor Bacterial Neurological Disease
    Chlorprothixene is a dopamine and histamine receptors antagonist with Kis of 18 nM, 2.96 nM, 4.56 nM, 9 nM and 3.75 nM for hD1, hD2, hD3, hD5 and hH1 receptors, respectively. Antipsychotic activity .
    Chlorprothixene
  • HY-B0274A
    Chlorprothixene hydrochloride
    2 Publications Verification

    Dopamine Receptor Histamine Receptor Bacterial Neurological Disease
    Chlorprothixene hydrochloride is a dopamine and histamine receptors antagonist with Kis of 18 nM, 2.96 nM, 4.56 nM, 9 nM and 3.75 nM for hD1, hD2, hD3, hD5 and hH1 receptors, respectively. Antipsychotic activity .
    Chlorprothixene hydrochloride
  • HY-N0247
    Saikosaponin B1
    2 Publications Verification

    Hedgehog Smo STAT Interleukin Related TNF Receptor Inflammation/Immunology Cancer
    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) .
    Saikosaponin B1
  • HY-13307
    JK184
    2 Publications Verification

    Hedgehog Cancer
    JK184 is a potent Hedgehog (Hh) pathway inhibitor with IC50 of 30 nM in mammalian cells.
    JK184
  • HY-100790
    Ciliobrevin A
    3 Publications Verification

    HPI-4

    Hedgehog Cancer
    Ciliobrevin A (HPI-4) is a hedgehog (Hh) signaling pathway inhibitor with median inhibitory concentration (IC50) less than 10 μM .
    Ciliobrevin A
  • HY-107560

    Histamine Receptor Inflammation/Immunology Cancer
    4-Methylhistamine hydrochloride is the dihydrochloride salt of 4-Methylhistamine (HY-W580721). 4-Methylhistamine hydrochloride is a potent and selective agonist of histamine 4 receptor (H4R) with a Ki of 50 nM. 4-Methylhistamine hydrochloride has a >100-fold selectivity for the hH4R over the other histamine receptor subtypes. 4-Methylhistamine hydrochloride can potently activate the hH4R (pEC50 = 7.4). 4-Methylhistamine hydrochloride can be used for the researches of cancer, inflammation and immunology, such as lung cancer and skin inflammation .
    4-Methylhistamine dihydrochloride
  • HY-124639

    CDK Cancer
    CDK9 inhibitor HH1 is a potent and selectively CDK9 inhibitor. CDK9 inhibitor HH1 inhibits the transcription of CDK. CDK9 inhibitor HH1 can be used in research of cancer .
    CDK9 inhibitor HH1
  • HY-111040

    Hedgehog Neurological Disease
    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-15412
    HhAntag
    1 Publications Verification

    Smo Cancer
    HhAntag is a specific, potent and orally active small molecule SMO antagonist of the Hh pathway .
    HhAntag
  • HY-150217A
    CpG ODN 10101 sodium
    2 Publications Verification

    ODN 10101 sodium

    Toll-like Receptor (TLR) Infection
    CpG ODN 10101 sodium, a synthetic oligodeoxynucleotide (ODN), is a toll-like receptor 9 (TLR9) agonist. CpG ODN 10101 sodium is a potent inducer of cytokine/chemokine expression ex vivo when used in combination with HH2(VQLRIRVAVIRA-NH2). CpG ODN 10101 sodium induces IFN- secretion from dendritic cells (DCs) and stimulates B-cells.CpG ODN 10101 sodium has antiviral and immunomodulatory properties that can influence chronic infection with HCV .
    CpG ODN 10101 sodium
  • HY-122590

    Gli Cancer
    Glabrescione B is the first compound that binds the Hedgehog (Hh) modulator Gli1. Glabrescione B impairs its activity by interfering with Gli1-DNA interaction. Glabrescione B inhibits the growth of Hedgehog-dependent tumor cells, the self-renewal ability, and clonogenicity of tumor-derived stem cells .
    Glabrescione B
  • HY-17514S

    R51211-d5

    Fungal Hedgehog Cytochrome P450 Autophagy Antibiotic Infection Cancer
    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 .
    Itraconazole-d5
  • HY-107551

    Hedgehog Gli Cancer
    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 .
    Hh Pathway-IN-1
  • HY-12317

    Smo Hedgehog Cancer
    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-120124

    SUVN-G3031

    Histamine Receptor Neurological Disease
    Samelisant (SUVN-G3031) is a potent and selective histamine H3 receptor (H3R) inverse agonist with good brain penetration and oral bioavailability. Samelisant has a similar binding affinity towards human (hH3R; Ki=8.7 nM) and rat (rH3R;Ki=9.8 nM) H3R indicating no inter-species differences. Samelisant can be used for the research of sleep-related disorders .
    Samelisant
  • HY-17514S1

    R51211-d3

    Antibiotic Autophagy Bacterial Cytochrome P450 Fungal Hedgehog Infection Cancer
    Itraconazole-d3 (R51211-d3) is the deuterium labeled Itraconazole (HY-17514) . 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-d3
  • HY-144881

    Histone Methyltransferase Inflammation/Immunology Cancer
    (S)-HH2853 (compound 200), a PYRIDINO five membered aromatic ring compound, is a potent EZH1/2 dual inhibitor with an IC50 of <100 nM for EZH2_Y641F. (S)-HH2853 has the potential to be used in the research of anti-tumor or autoimmune diseases .
    (S)-HH2853
  • HY-17514R

    R51211 (Standard)

    Reference Standards Fungal Hedgehog Cytochrome P450 Autophagy Antibiotic Bacterial Infection Cancer
    Itraconazole (Standard) is the analytical standard of Itraconazole. This product is intended for research and analytical applications. 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 (Standard)
  • HY-101188

    Histamine Receptor Infection
    INCB38579 is an orally active, highly brain penetrable, and selective histamine H4 receptor (HH4R) antagonist (hH4R IC50=4.8 nM, mH4R IC50=42 nM, rH4R IC50=32 nM). INCB38579 shows anti-inflammatory pain and anti-pruritic activities .
    INCB38579
  • HY-13459

    Smo Cancer
    PF-5274857 is a potent, selective, orally active and brain-penetrant antagonist of Smo, with an IC50 of 5.8 nM and Ki of 4.6 nM. PF-5274857 has potential for research of tumor types including brain tumors and brain metastasis driven by an activated Hh pathway .
    PF-5274857
  • HY-129250

    Histamine Receptor Neurological Disease
    AZD5213 is a selective and competitive human H3 receptor antagonist with a pKi value of 9.3 for hH3R. AZD5213 can be used for the research of sleep and cognitive regulation .
    AZD5213
  • HY-144882

    Histone Methyltransferase Inflammation/Immunology Cancer
    (R)-HH2853 is a mutant EZH2 inhibitor with an IC50 of <100 nM for EZH2-Y641F. (R)-HH2853 can be used for cancer and autoimmune diseases (WO2018045971A1; compound 201) .
    (R)-HH2853
  • HY-P99707

    Hh1

    Apoptosis Cancer
    Lilotomab (HH1) is a murine anti-CD37 monoclonal antibody. Lilotomab reduces clonogenic survival. Lilotomab shows anti-tumor activity .
    Lilotomab
  • HY-123781A

    Hedgehog Cancer
    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-121037

    EGM1

    Phosphodiesterase (PDE) Cancer
    Eggmanone (EGM1) is a potent and selective phosphodiesterase 4 (PDE4) antagonist with an IC50 of 72 nM for PDE4D3. Eggmanone shows approximately 40- to 50-fold selective for PDE4D3 over other PDEs. Eggmanone exerts its Hh-inhibitory effects through selective antagonism of PDE4, leading to protein kinase A activation and subsequent Hh blockade .
    Eggmanone
  • HY-120499

    Hedgehog Smo Cancer
    AZD8542 is an antagonist of Smoothened (SMO), playing an important role in oncology. AZD8542 is an Hedgehog (Hh) pathway antagonist on tumor progression with an emphasis on the role of the stroma compartment .
    AZD8542
  • HY-16475

    Hedgehog Cancer
    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-12316R
    20(S)-Hydroxycholesterol (Standard)
    3 Publications Verification

    20α-Hydroxycholesterol (Standard)

    Reference Standards Smo Endogenous Metabolite Cancer
    20(S)-Hydroxycholesterol (Standard) is the analytical standard of 20(S)-Hydroxycholesterol. This product is intended for research and analytical applications. 20(S)-hydroxyCholesterol (20α-Hydroxycholesterol) is an allosteric activator of the oncoprotein smoothened (Smo) that activates the hedgehog (Hh) signaling pathway with an EC50 of 3 μM in a gene transcription reporter assay using NIH3T3 cells .
    20(S)-Hydroxycholesterol (Standard)
  • HY-143400

    HSP Hedgehog Cancer
    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-17514S2

    R51211-d9

    Fungal Hedgehog Bacterial Autophagy Cytochrome P450 Antibiotic Infection
    Itraconazole-d9 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. Itraconazole is a oxysterol-binding protein (OSBP) inhibitor .
    Itraconazole-d9
  • HY-17024R

    11-Deoxojervine (Standard)

    Reference Standards Hedgehog Smo Endogenous Metabolite Cancer
    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-159503A

    3D185; Hh185

    FGFR c-Fms Cancer
    Segigratinib hydrochloride (3D185) is a potent inhibitor of FGFR1/2/3 and CSF-1R; The IC50 values for FGFR1, FGFR2, FGFR3 and CSF-1R are 0.5, 1.3, 3.6 and 3.8 nM, respectively. Segigratinib hydrochloride has antitumor activity .
    Segigratinib hydrochloride
  • HY-W111144

    Hedgehog Cancer
    T-1330 (Compound 45) is a Hh pathway inhibitor and reduces Gli1 expression .
    T-1330
  • HY-128656

    Histamine Receptor Neurological Disease Endocrinology
    LML134 (compound 18b) is an orally active and high selective Histamine 3 receptor (H3R) inverse agonist with Kis of 0.3 nM and 12 nM for hH3R cAMP and hH3R bdg. LML134 penetrates the brain rapidly, leading to high H3R occupancy, and disengages its target with a fast kinetic profile. LML134 has the potential for excessive sleep disorders .
    LML134
  • HY-159503

    3D185 free base; Hh185 free base

    FGFR c-Fms Cancer
    Segigratinib is a fibroblast growth factor receptor tyrosine kinase inhibitor, with antineoplastic effect .
    Segigratinib
  • HY-W580721

    Histamine Receptor Inflammation/Immunology Cancer
    4-Methylhistamine is a potent and selective agonist of histamine 4 receptor (H4R) with a Ki of 50 nM. 4-Methylhistamine has a >100-fold selectivity for the hH4R over the other histamine receptor subtypes. 4-Methylhistamine can potently activate the hH4R (pEC50 = 7.4). 4-Methylhistamine can be used for the researches of cancer, inflammation and immunology, such as lung cancer and skin inflammation .
    4-Methylhistamine
  • HY-161333

    Histamine Receptor Inflammation/Immunology
    ADS031, a histamine H3R antagonist, displays 12.5 nM affinity at the hH3R and the highest inhibitory activity against AChE (IC50 = 1.537 μM) .
    ADS031
  • HY-117407

    Smo Cancer
    ALLO-2 is a potent drug-resistant Smoothened (Smo) mutant antagonist that inhibits Smo agonist Hh-Ag1.5-induced luciferase expression in TM3-Gli-Luc cells with IC50 of 6 nM .
    ALLO-2
  • HY-108507

    Smo Cancer
    MRT-10 is a seven-transmembrane receptor smoothened (Smo) antagonist with an IC50 of 0.65 μM in the micromolar range in various Hedgehog (Hh) assays. MRT-10 binds to the Smo receptor at the level of the Bodipycyclopamine binding site. MRT-10 can be used for the research of cancer .
    MRT-10
  • HY-117376

    UAB30

    RAR/RXR Cancer
    (all-E)-UAB30 (UAB30) is an retinoid X receptor (RXR) selective agonist.(all-E)-UAB30 shows anti-proliferation activity for MyLa, HuT 78, and HH cells with the IC50 of 34.7, 5.1, and 22.4 μM respectively .
    (all-E)-UAB30
  • HY-107408

    Hedgehog Gli Metabolic Disease Cancer
    SANT 2 is a potent Hh-signaling pathway antagonist. SANT 2 interferes with the expression of Gli1. SANT 2 causes developmental delay in medaka embryos. 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-13654

    Smo Hedgehog Cancer
    IPI-269609 is an orally effective Smoothed (SMO) inhibitor that targets the Hedgehog (Hh) signaling pathway. IPI-269609 specifically reduces the ALDH-bright (high aldehyde dehydrogenase activity) cell subset, which is considered the "cancer stem cells" in pancreatic cancer. IPI-269609 significantly inhibits the migration and colony formation of pancreatic cancer cells. IPI-269609 effectively inhibits pancreatic cancer metastasis in a mouse model. IPI-269609 can be used for pancreatic cancer research .
    IPI-269609

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