2. Signaling Pathways
  3. Metabolic Enzyme/Protease
  4. UGT
  5. UGT Inhibitor

UGT Inhibitor

UGT Inhibitors (18):

Cat. No. Product Name Effect Purity
  • HY-N0235
    Bakuchiol
    		Inhibitor 99.25%
    Bakuchiol is a phytoestrogen that can be obtained from psoralen seeds. Bakuchiol has been proven to be a non-competitive inhibitor of multiple enzymes, including UDP-glucuronosyltransferase 2B7 (UGT2B7) and human carboxylesterase 2 (hCE2) , with IC50s values of 40.9 μM and 7.28 μM, respectively. Bakuchiol exhibits significant research and application potential in areas such as anti-inflammatory, antibacterial, antitumor therapies, as well as drug metabolism regulation.
  • HY-111832
    1,2,3,6-Tetragalloylglucose
    		Inhibitor 99.08%
    1,2,3,6-Tetragalloylglucose (TEgG) is a competitive inhibitor of UDP-glucuronyltransferase UGT1A1, targeting the competitive substrate binding site of UGT1A1. 1,2,3,6-Tetragalloylglucose inhibits UGT1A1-mediated β-estradiol 3-glucuronidation and SN-38 glucuronidation with IC50 of 6.01 μM and 4.31 μM, respectively, and binds to UGT1A1 with Ki of 3.55 μM. 1,2,3,6-Tetragalloylglucose also induces tumor cell apoptosis, inhibit cell proliferation, activates caspase-3 and induces DNA fragmentation in HL-60 cells. 1,2,3,6-Tetragalloylglucose also inhibits HIV integrase and reverse transcriptase, and inhibits HCV protease.
  • HY-131703
    UGT8-IN-1
    		Inhibitor 99.94%
    UGT8-IN-1 is a brain penetrable and orally active inhibitor of ceramide galactosyltransferase enzyme (UGT8). UGT8-IN-1 can be used in the study for lysosomal storage disorders.
  • HY-N0762
    Isobavachin
    		Inhibitor 99.88%
    Isobavachin is an orally active, blood-brain barrier-penetrating prenylated flavonoid present in Psoralea corylifolia. Isobavachin inhibits human CYP2B6, CYP2C9, CYP2C19, UGT1A1, UGT1A9, and UGT2B7. Isobavachin suppresses MAPK activation, NF-κB nuclear translocation, overexpression of iNOS/COX-2, FcεRI-mediated signaling pathways, and RANKL-induced osteoclastogenesis. Isobavachin induces autophagy, cytotoxicity, neuronal differentiation, and NRF2 activation; it alleviates oxidative damage, inflammatory responses, apoptosis, iron accumulation, mitochondrial biogenesis, and mast cell degranulation. Isobavachin is applicable to research related to liver injury, inflammatory diseases, osteoporosis, liver cancer, prostate cancer, glioma, periodontitis-induced bone loss, and Alzheimer's disease.
  • HY-122163
    MK-3901
    		Inhibitor
    MK-3901 is a selective P2X3 receptor antagonist with an IC50 of 24 nM. MK-3901 inhibits UGT1A1 (with an IC50 of 1 μM) and CYP2C9 (with an IC50 of 5.7 μM). MK-3901 activates PXR. MK-3901 induces hyperbilirubinemia. MK-3901 can be used for the research of inflammatory pain.
  • HY-B0811
    Salicylamide
    		Inhibitor 99.92%
    Salicylamide is an inhibitor of microsomal UDP-glucuronosyltransferase. Salicylamide is an analgesic and anti-pyretic agent.
  • HY-107850
    Pregnanediol
    		Inhibitor 99.97%
    Pregnanediol (NSC 1612) is a Progesterone (HY-N0437) metabolite. Pregnanediol does not affect the transcriptional activity of UGT1A1 enhancer-promoter complex of WT and variant type. pregnanediol inhibits glucuronidation activity of G71R-UGT1A1. Pregnanediol is a cause of breast milk jaundice in carriers of G71R.
  • HY-137083
    Trifluoperazine N-Glucuronide
    		Inhibitor
    Trifluoperazine N-Glucuronide (UGT1A4), as one of the human UGT1A isoforms, is expressed in the liver. Trifluoperazine N-Glucuronide catalyzes the imipramine and trifluoperazine Nglucuronide formation.
  • HY-160250
    UGT1A1-IN-1
    		Inhibitor 99.27%
    UGT1A1-IN-1 is a UGT1A1 inhibitor and fluorescent probe (Ex=370 nm, Em=520 nm), with an IC50 of 1.33 μM and a Ki of 5.02 μM. UGT1A1-IN-1 is selectively glucuronidated by UGT1A1 at the bilirubin homologous binding site, and its PET effect is blocked along with this reaction, triggering fluorescence changes. UGT1A1-IN-1 can serve as a substitute for bilirubin to detect UGT1A1 activity and perform high-throughput screening of UGT1A1 modulators.
  • HY-N0859
    Schisanhenol
    		Inhibitor 99.99%
    Schisanhenol (Schizanhenol), a lignan, is an orally active antioxidant. Schisanhenol reduces AChE activity, increases SIRT1 and PGC-1α expression, and decreases phosphorylated Tau (Ser 396) levels. Schisanhenol increases SOD and glutathione peroxidase activity, decreases malondialdehyde (MDA) content, and inhibits UGT2B7 activitY. Schisanhenol attenuates ox-LDL-induced apoptosis, intracellular reactive oxygen species generation, and cytotoxicity in endothelial cells. Schisanhenol inhibits LDL oxidation, brain mitochondrial and membrane peroxidative damage, and brain mitochondrial swelling and disintegration. Schisanhenol can be used for the research of Alzheimer’s disease, atherosclerosis, brain ischemia, and age-related brain deterioration.
  • HY-N2413
    Gomisin D
    		Inhibitor 99.56%
    Gomisin D is an orally active lignan that binds to PDGFRβ with a Kd of 10 μM. By targeting PDGFRβ to regulate signaling pathways, Gomisin D inhibits the activation and proliferation of hepatic stellate cells and promotes their apoptosis, thereby ameliorating hepatic fibrosis. Gomisin D exhibits multiple activities such as photoprotection, antimelanogenesis, antioxidant effects, and hypoglycemic activity. Gomisin D can be used in studies related to diabetes, Alzheimer's disease, and hepatic fibrosis.
  • HY-145668
    Cyclopentenyl uracil
    		Inhibitor 99.84%
    Cyclopentenyl uracil, a non-cytotoxic inhibitor of uridine kinase, effectively blocks the salvage of circulating uridine by host and tumor tissues in the intact mouse.
  • HY-130046
    16-Epiestriol
    		Inhibitor 99.04%
    16-Epiestriol (16-epi-Estriol; 16β,17β-Estriol) is a natural stereoisomer of estriol and an anti-inflammatory agent that targets UGT. The Ki values of 16-Epiestriol against human UGT1A10 and UGT2B7 are 98.1 μM and 162 μM, respectively. As a glucuronidation substrate, 16-Epiestriol can be modified at the 3-OH, 16-OH and 17-OH sites by various UGT enzymes; in liver microsomes, the modification mainly occurs at the 16-OH and 17-OH sites, while reactions take place at all three sites in intestinal microsomes. 16-Epiestriol acts on the phase II inflammatory process by blocking edema mediated by prostaglandins and leukocyte infiltration. It lacks glycogenic activity or any effect on blood glucose levels, and serves as an important candidate molecule in the research of inflammatory diseases.
  • HY-N4267
    Yangambin
    		Inhibitor 98.27%
    Yangambin is a PAF receptor antagonist and UGT1A1/UGT1A3 inhibitor, with an IC50 of 29.7 μM and a Ki of 17.1 μM against human UGT1A1, and an IC50 of 56.5 μM and a Ki of 66.8 μM against human UGT1A3. Yangambin blocks PAF-mediated responses, inhibits LTB4-mediated neutrophil infiltration, and suppresses inflammatory events and anaphylactic contraction. Yangambin acts as a central nervous system inhibitor to reduce spontaneous activity, and also exhibits analgesic, anticonvulsant, antileishmanial, vasodilatory and hypotensive effects. Yangambin blocks voltage-gated Ca2+ channels, reduces the production of NO, TNF-α, IL-6 and PGE2 in cells, increases the production of IL-10, and exerts a protective effect against cardiovascular injury. Yangambin can be used in research related to allergies, cutaneous leishmaniasis, central nervous system diseases and cardiovascular diseases.
  • HY-100319
    UK-157147
    		Inhibitor
    UK-157147 is a substrate for UDP-glucuronosyltransferases (UGT1A1) with a Km value of 105 μM.
  • HY-N0859R
    Schisanhenol (Standard)
    		Inhibitor
    Schisanhenol (Standard) (Schizanhenol (Standard)) is the analytical standard of Schisanhenol (HY-N0859). This product is intended for research and analytical applications. Schisanhenol, a lignan, is an orally active antioxidant. Schisanhenol reduces AChE activity, increases SIRT1 and PGC-1α expression, and decreases phosphorylated Tau (Ser 396) levels. Schisanhenol increases SOD and glutathione peroxidase activity, decreases malondialdehyde (MDA) content, and inhibits UGT2B7 activitY. Schisanhenol attenuates ox-LDL-induced apoptosis, intracellular reactive oxygen species generation, and cytotoxicity in endothelial cells. Schisanhenol inhibits LDL oxidation, brain mitochondrial and membrane peroxidative damage, and brain mitochondrial swelling and disintegration. Schisanhenol can be used for the research of Alzheimer’s disease, atherosclerosis, brain ischemia, and age-related brain deterioration.
  • HY-N0235R
    Bakuchiol (Standard)
    		Inhibitor
    Bakuchiol (Standard) is the analytical standard of Bakuchiol. This product is intended for research and analytical applications. Bakuchiol is a phytoestrogen that can be obtained from psoralen seeds. Bakuchiol has been proven to be a non-competitive inhibitor of multiple enzymes, including UDP-glucuronosyltransferase 2B7 (UGT2B7) and human carboxylesterase 2 (hCE2) , with IC50s values of 40.9 μM and 7.28 μM, respectively. Bakuchiol exhibits significant research and application potential in areas such as anti-inflammatory, antibacterial, antitumor therapies, as well as drug metabolism regulation.
  • HY-N3989
    Haplopine
    		Inhibitor 99.49%
    Haplopine is a substance with anti-inflammatory, antioxidant and photoactivated antibacterial activities. It also acts as an inhibitor of UGT1A7 and a photoactivated restriction endonuclease inhibitor. Haplopine inhibits the mRNA/protein expression of IL-6, TSLP, GM-CSF, G-CSF, IL-4, IL-13 and COX-2, while upregulating the mRNA/protein expression of SOD, CAT and HO-1. Haplopine inhibits the glucuronidation reaction catalyzed by UGT1A7 through competitive hydrophobic binding. Haplopine exerts photoactivated restriction endonuclease inhibitory effects by binding to DNA. Haplopine exhibits photoactivated activity against methicillin-resistant Staphylococcus aureus. Haplopine alleviates symptoms of atopic dermatitis. Haplopine can be used in research related to atopic dermatitis and methicillin-resistant Staphylococcus aureus infections.