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smoothened inhibitor

" in MedChemExpress (MCE) Product Catalog:

34

Inhibitors & Agonists

1

Isotope-Labeled Compounds

Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-16391
    Glasdegib
    5 Publications Verification

    PF-04449913

    		 Smo Cancer
    Glasdegib (PF-04449913) is a potent and orally bioavailable smoothened inhibitor. Glasdegib (PF-04449913) binds to human SMO (amino acids 181-787) with an IC50 of 4 nM .
    Glasdegib
  • HY-100535
    KAAD-Cyclopamine
    2 Publications Verification

    Cyclopamine-KAAD

    		 Smo Cancer
    KAAD-Cyclopamine, a hedgehog signaling inhibitor, is a smoothened antagonist .
    KAAD-Cyclopamine
  • HY-16587
    Saridegib

    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-13809
    BMS-833923

    XL-139

    		 Smo Apoptosis Cancer
    BMS-833923 (XL-139) is an orally biocompatible Smoothened (Smo) inhibitor with anti-tumor activity. It can inhibit the binding of BODIPY cyclopamine to SMO in a dose-dependent manner with an IC50 of 21 nM .
    BMS-833923
  • HY-B0877
    Halcinonide
    1 Publications Verification

    SQ-18566

    		 Smo Caspase RAR/RXR CDK Cardiovascular Disease Neurological Disease Inflammation/Immunology
    Halcinonide (SQ-18566) is an orally active Smoothened (Smo) agonist. Halcinonide activates the Hedgehog signaling pathway by binding to Smo and promoting its internalization and expression, thereby activating Gli transcription factors. Halcinonide not only stimulates cell proliferation, increases the expression of cyclin D2/CDK6 and inhibits the degradation of caspase-3, but also suppresses Bcl-2/Bax-mediated apoptosis, oxidative stress and inflammatory responses. Halcinonide activates RxRγ to upregulate the expression of myelin genes, thereby reducing cerebral infarction and improving behavioral deficits. Halcinonide has been used in studies related to multiple sclerosis and ischemic stroke .
    Halcinonide
  • HY-18366A
    RU-SKI 43 hydrochloride
    2 Publications Verification

    		 Hedgehog Cancer
    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-100036
    MK-4101

    		Smo Apoptosis Hedgehog Cancer
    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-18636
    LEQ506

    NVP-LEQ506

    		 Smo Cancer
    LEQ506 is a second-generation inhibitor of smoothened (Smo) with IC50s of 2 and 4 nM in human and mouse, respectively.
    LEQ506
  • HY-113965
    CUR61414
    1 Publications Verification

    		 Hedgehog Smo Apoptosis Inflammation/Immunology
    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-177291
    LAB687

    		Microsomal Triglyceride Transfer Protein (MTP) Smo Hedgehog LDLR Cardiovascular Disease Cancer
    LAB687 is a microsomal triglyceride transfer protein (MTP) inhibitor with an IC50 of 0.9 nM for apolipoprotein B (apoB) secretion in HepG2 cells. LAB687 also acts as a Smoothened (Smo) antagonist, with IC50 values of 2.48 μM and 3.42 μM against mouse and human Smo receptors, respectively. LAB687 reduces triglyceride and low-density lipoprotein cholesterol (LDL-C) levels, and inhibits the Hedgehog signaling pathway. LAB687 can be used in studies related to Hedgehog-dependent cancers .
    LAB687
  • HY-18366
    RU-SKI 43

    		Hedgehog Cancer
    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-115566
    S1PL-IN-1

    		LPL Receptor Smo Inflammation/Immunology
    S1PL-IN-31 (compound ) is an oral active sphingosine-1-phosphate (S1P) lyase inhibitor with the IC50 of 210 nM. S1PL-IN-31 is Smoothened receptor antagonist with the IC50 of 440 nM. S1PL-IN-31 can be used for study of experimental autoimmune encephalomyelitis .
    S1PL-IN-1
  • HY-145387
    MRT-81

    		Smo Cancer
    MRT-81 is a potent antagonist of human and rodent smoothened (Smo) receptors, with an IC50 value of 41 nM in the Shh-light2 cells. MRT-81 has potent hedgehog inhibiting activity. MRT-81 can be used for the research of cancer .
    MRT-81
  • HY-117407
    ALLO-2

    		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-147670
    TPB15

    		Hedgehog Smo Gli Apoptosis Cancer
    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-16587A
    Saridegib hydrochloride

    IPI 926 hydrochloride; Patidegib hydrochloride

    		 Smo Cancer
    Saridegib hydrochloride is a potent and specific inhibitor of Smoothened (Smo), a key signaling transmembrane protein in the Hedgehog (Hh) pathway.
    Saridegib hydrochloride
  • HY-147744
    AZD7254

    		Smo Cancer
    AZD7254 is an orally active Smoothened (SMO) inhibitor with an EC50 of 1.0 nM against sonic Hh protein (shh) .
    AZD7254
  • HY-147743
    SMO-IN-1

    		Smo Cancer
    SMO-IN-1 (Compound 15) is an orally active Smoothened (SMO) inhibitor with an EC50 of 89 nM against sonic Hh protein (shh) .
    SMO-IN-1
  • HY-117903A
    MRT-92

    		Smo Hedgehog Cancer
    MRT-92 is a Smoothened (Smo) antagonist (Ki=0.7 nM) with anticancer activity. MRT-92 inhibits Hedgehog signaling pathway and rodent cerebellar granule cell proliferation by blocking overlapping binding sites in the transmembrane domain of the Smoothened receptor (IC50=0.4 nM). MRT-92 can be used in the study of cerebellar glioma .
    MRT-92
  • HY-16391B
    Glasdegib hydrochloride

    PF-04449913 hydrochloride

    		 Smo Cancer
    Glasdegib hydrochloride is a potent and orally bioavailable smoothened inhibitor. Glasdegib hydrochloride (PF-04449913) binds to human SMO (amino acids 181-787) with an IC50 of 4 nM .
    Glasdegib hydrochloride
  • HY-16391A
    Glasdegib maleate

    PF-04449913 maleate

    		 Smo Cancer
    Glasdegib maleate (PF-04449913 maleate) is a potent and orally bioavailable smoothened inhibitor. Glasdegib maleate binds to human SMO (amino acids 181-787) with IC50value of 4 nM .
    Glasdegib maleate
  • HY-108508
    SMANT hydrochloride

    		Smo Hedgehog Cancer
    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-123752
    MS-0022

    		Hedgehog Smo Cancer
    MS-0022 is a Smoothened (SMO) antagonist. MS-0022 can inhibit the Hedgehog (Hh) signaling pathway. MS-0022 can be used in anti-tumor research .
    MS-0022
  • HY-162372
    Hedgehog IN-6

    		Hedgehog Smo Cancer
    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-150564
    SMO-IN-2

    		Smo Hedgehog Cancer
    SMO-IN-2 is a potent smoothened (SMO) inhibitor with an IC50 value of 123.4 nM for hedgehog (Hh) signaling pathway. SMO-IN-2 has antiproliferative activity against human medulloblastoma cell line Daoy. Anticancer activity .
    SMO-IN-2
  • HY-18287A
    MRT-83 hydrochloride

    		Smo Cancer
    MRT-83 (hydrochloride) is the potent antagonist of Smoothened (Smo) receptor. MRT-83 (hydrochloride) inhibits the Hedgehog (Hh) signaling pathway and BODIPY-cyclopamine binding to human Smo. MRT-83 (hydrochloride) has the potential for researching cancer disease .
    MRT-83 hydrochloride
  • HY-150567
    SMO-IN-3

    		Smo Hedgehog Cancer
    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-16391R
    Glasdegib (Standard)

    PF-04449913 (Standard)

    		 Smo Reference Standards Cancer
    Glasdegib (Standard) is the analytical standard of Glasdegib. This product is intended for research and analytical applications. Glasdegib (PF-04449913) is a potent and orally bioavailable smoothened inhibitor. Glasdegib (PF-04449913) binds to human SMO (amino acids 181-787) with an IC50 of 4 nM .
    Glasdegib (Standard)
  • HY-16391S1
    Glasdegib-d4

    PF-04449913-d4

    		 Isotope-Labeled Compounds Smo Cancer
    Glasdegib-d4 (PF-04449913-d4) is deuterium labeled Glasdegib. Glasdegib (PF-04449913) is a potent and orally bioavailable smoothened inhibitor. Glasdegib (PF-04449913) binds to human SMO (amino acids 181-787) with an IC50 of 4 nM .
    Glasdegib-d4
  • HY-159893
    SMO-IN-5

    		Smo Hedgehog Apoptosis Cancer
    SMO-IN-5 ((Compound 25(B31)) is a potent and competitive inhibitor of smoothened (SMO) that can inhibit Hedgehog (Hh) signaling. SMO-IN-5 interacts with Smo through hydrogen bonds, hydrophobic interactions, and electrostatic forces. SMO-IN-5 inhibits PC cell proliferation, migration, and induces apoptosis by suppressing Gli1 expression. SMO-IN-5 exhibits antitumor activity in pancreatic cancer. .
    SMO-IN-5
  • HY-108508R
    SMANT hydrochloride (Standard)

    		Reference Standards Smo Hedgehog Cancer
    SMANT hydrochloride (Standard) is the analytical standard of SMANT (hydrochloride) (HY-108508). This product is intended for research and analytical applications. 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 (Standard)
  • HY-182721
    Pipinib

    		PI4K Hedgehog Cancer
    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-100036R
    MK-4101 (Standard)

    		Smo Reference Standards Apoptosis Hedgehog Cancer
    MK-4101 (Standard) is the analytical standard of MK-4101 (HY-100036). This product is intended for research and analytical applications. 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 (Standard)
  • HY-183335
    SMO-IN-6

    		Smo Hedgehog Gli Apoptosis Caspase Cancer
    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

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