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Hedgehog signaling pathway

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50

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GMP Molecules

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-12848
    SAG
    Maximum Cited Publications
    37 Publications Verification

    Smo Cancer
    SAG is a potent Smoothened (Smo) receptor agonist (EC50=3 nM; Kd=59 nM). SAG activates the Hedgehog signaling pathway and counteracts Cyclopamine (HY-17024) inhibition of Smo .
    SAG
  • HY-17514
    Itraconazole
    Maximum Cited Publications
    24 Publications Verification

    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-12848B
    SAG hydrochloride
    Maximum Cited Publications
    37 Publications Verification

    Smo Cancer
    SAG hydrochloride is a potent Smoothened (Smo) receptor agonist (EC50=3 nM; Kd=59 nM). SAG hydrochloride activates the Hedgehog signaling pathway and counteracts Cyclopamine (HY-17024) inhibition of Smo .
    SAG hydrochloride
  • HY-113081
    1-Methyladenosine
    4 Publications Verification

    Endogenous Metabolite PPAR Hedgehog Cancer
    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-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-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-12848C
    SAG dihydrochloride
    Maximum Cited Publications
    37 Publications Verification

    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-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-B0508
    Ornidazole
    2 Publications Verification

    Ro 7-0207

    Bacterial Parasite Antibiotic Hedgehog Infection Cancer
    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-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-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-N6954
    Garcinone C
    2 Publications Verification

    ATM/ATR STAT CDK Hedgehog Inflammation/Immunology Cancer
    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-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-113081R

    Reference Standards Endogenous Metabolite PPAR Hedgehog Cancer
    1-Methyladenosine (Standard) is the analytical standard of 1-Methyladenosine. This product is intended for research and analytical applications. 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 . In Vitro:Compared to surrounding tumor tissues, 1-methyladenosine methylation in RNA is aberrantly elevated in hepatocellular carcinoma (HCC) cell lines and liver cancer stem cells (CSCs). Methylated 1-methyladenosine can promote cholesterol synthesis and activate the Hedgehog signaling pathway by enhancing the translation of PPARδ in liver CSCs, ultimately driving the self-renewal and tumorigenesis of liver cancer stem cells .
    1-Methyladenosine (Standard)
  • 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-177291

    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-P10875

    Hedgehog Cancer
    HL2-m5 is the inhibitor for the interaction between sonic hedgehog/patched (Shh/PTCH1) with Kd of 170 nM for Shh. HL2-m5 inhibits activation of Hedgehog signaling pathway and transcription of Gli-controlled gene with an IC50 of 230 nM .
    HL2-m5
  • HY-12848R

    Smo Reference Standards Cancer
    SAG (Standard) is the analytical standard of SAG. SAG is a potent Smoothened (Smo) receptor agonist (EC50=3 nM; Kd=59 nM). SAG activates the Hedgehog signaling pathway and counteracts Cyclopamine (HY-17024) inhibition of Smo .
    SAG (Standard)
  • 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-12848G

    Smo Cancer
    SAG (GMP) is SAG (HY-12848) in GMP grade. GMP-grade small molecules can be used as auxiliary reagents in cell therapy. SAG is a potent Smoothened (Smo) receptor agonist (EC50=3 nM; Kd=59 nM). SAG activates the Hedgehog signaling pathway and counteracts Cyclopamine (HY-17024) inhibition of Smo .
    SAG
  • 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-18366

    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-113081S1

    Isotope-Labeled Compounds Endogenous Metabolite PPAR Hedgehog Cancer
    1-Methyladenosine-d3 hydriodide is the deuterium labeled 1-Methyladenosine (HY-113081). 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-d3 hydriodide
  • HY-12848A

    Smo Cancer
    (Rac)-SAG is an isoform of SAG (HY-12848). SAG is a potent Smoothened (Smo) receptor agonist (EC50=3 nM; Kd=59 nM). SAG activates the Hedgehog signaling pathway and counteracts Cyclopamine (HY-17024) inhibition of Smo .
    (Rac)-SAG
  • 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-113081AS

    Isotope-Labeled Compounds Endogenous Metabolite PPAR Hedgehog Cancer
    1-Methyladenosine-d3 hydrochloride is the hydrochloride salt form of deuterium labeled 1-Methyladenosine (HY-113081). 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-d3 hydrochloride
  • 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-148440

    Hedgehog Smo Cancer
    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-B0508S1

    Ro 7-0207-13C2,15N2

    Isotope-Labeled Compounds Bacterial Parasite Antibiotic Hedgehog Infection
    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-13C2,15N2
  • HY-113081S

    Isotope-Labeled Compounds Endogenous Metabolite PPAR Hedgehog Cancer
    1-Methyl Adenosine-d3 is the deuterium labeled 1-Methyladenosine. 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-d3
  • 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
  • HY-18287A

    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-N0247R

    Reference Standards Smo Cancer
    Saikosaponin B1 (Standard) is the analytical standard of Saikosaponin B1. This product is intended for research and analytical applications. 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 (Standard)
  • HY-16587A

    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-159511

    Hedgehog Cancer
    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-123752

    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-150564

    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-150567

    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-116455

    Fluorescent Dye Cancer
    BRD-9526 is a potent and selective Sonic Hedgehog (Shh) pathway inhibitor with potential anti-cancer activity. The mechanism of BRD-9526 is similar in some ways to commonly used inhibitors such as cyclopamine, but is significantly different in other ways. The discovery of BRD-9526 may provide a useful probe for studying complex signaling pathways .
    BRD-9526
  • HY-W414581

    3ß,27-Dihydroxy-5-cholesten-7-one

    Biochemical Assay Reagents
    7-Keto-27-hydroxycholesterol (3?,27-Dihydroxy-5-cholesten-7-one) is an important bioactive compound that agonizes the activity of smoothened (SMO) protein in the Hedgehog (Hh) signaling pathway, which is essential for proper cell differentiation in embryonic tissues.
    7-Keto-27-hydroxycholesterol
  • HY-B0508S

    Ro 7-0207-d5

    Isotope-Labeled Compounds Bacterial Parasite Antibiotic Hedgehog Infection Cancer
    Ornidazole-d5 is deuterium 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-d5
  • HY-B0508R

    Ro 7-0207 (Standard)

    Reference Standards Bacterial Parasite Antibiotic Hedgehog Infection Cancer
    Ornidazole (Standard) is the analytical standard of Ornidazole. This product is intended for research and analytical applications. 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 (Standard)
  • HY-153500

    Hedgehog Others
    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-117903A

    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-118295

    Endogenous Metabolite Cancer
    Pyrimidine-indole hybrid is a compound that inhibits ciliogenesis and has the activity of antagonizing the Hedgehog signaling pathway by destabilizing microtubules. Pyrimidine-indole hybrid exerts its biological effects by inhibiting ciliogenesis and deconstructing the stable form of α-tubulin. Pyrimidine-indole hybrid has shown its unique mechanism of action in in vitro cell experiments and zebrafish embryo models, interfering with microtubule dynamics .
    Pyrimidine-indole hybrid
  • HY-N6954R

    Reference Standards ATM/ATR STAT CDK Hedgehog Inflammation/Immunology Cancer
    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-N9684

    EGFR GSK-3 Hedgehog Akt ERK Apoptosis Cancer
    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-182641

    SAG-Cl (cis-isomer)

    Gli Cardiovascular Disease
    SAG analog (cis-isomer) (SAG-Cl (cis-isomer)) (Compound 10b) is a Gli1 activator with an EC50 of 7.6 nM. SAG analog (cis-isomer) is non-toxic .
    SAG analog (cis-isomer)
  • HY-183335

    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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