ugt1a1

Cremophor EL is a nonionic surfactant. cremophor EL inhibits cellular metabolism and suppresses UGT1A1-mediated rhodopsin glucuronidation.

UGT1A1-IN-1 (compound 2) acts as a non-competitive inhibitor of UGT1A1, effectively inhibiting the 1-O-glucuronidation process mediated by UGT1A1 with a Ki value of 5.02 μM. This compound binds to the same ligand-binding site on UGT1A1 as bilirubin and additionally functions as a 'turn-on' fluorescent probe substrate for UGT1A1 [1].

Cabotegravir (S GSK1265744) (GSK744, GSK1265744) is a long-acting HIV integrase inhibitor and inhibits the HIV-1 integrase catalyzed strand transfer reaction (IC50: 3.0 nM).

Hesperetin belongs to the flavanone class of flavonoids. Hesperetin, in the form of its glycoside hesperidin, is the predominant flavonoid in lemons and oranges.

Mertansine is a tubulin inhibitor and an antibody-conjugable maytansinoid alkaloid. The IC50 of Mertansine against HCT-15 and A431 cells is 0.750 and 0.04nM.

1. Corylifol A (Corylinin) displays cytotoxic activity against HepG2 and Hep3B hepatocellular carcinoma cell lines, with IC50 values of 4.6 and 13.5 ug ml, respectively. 2. Corylifol A and Biochanin A can be the potential uncouplers of neuronal nitric oxide synthase-postsynaptic density protein-95. 3. Corylifol A and bavachin are strong inhibitors of UDP-glucuronosyltransferase 1A1 (UGT1A1) with the inhibition kinetic parameters (Ki) values lower than 1 uM.4. Corylifol A and bakuchiol are naturally occurring potent inhibitors of hCE2, with low Ki values ranging from 0.62uM to 3.89 uM. 5. Corylifol A shows an inhibitory effect on IL-6-induced STAT3 promoter activity in Hep3B cells with IC50 values of 0.81 ± 0.15 uμ, it also inhibits STAT3 phosphorylation induced by IL-6 in Hep3B cells, suggests that corylifol A has antiinflammatory activity.

Licochalcone A is a flavonoid isolated from the famous Chinese medicinal herb Glycyrrhiza uralensis Fisch with obvious anti-cancer effects.

RO6889678 is HBV inhibitor with a complex ADME profile.

Naringenin-7-O-β-D-glucuronide, a metabolite of the flavonoid naringenin, is predominantly synthesized through the action of UDP-glucuronosyltransferase (UGT) isoforms UGT1A1, UGT1A3, UGT1A6, and UGT1A9.

Carlinoside could be a worthy choice to intervene hyperbilirubinemia due to liver dysfunction. Carlinoside upregulates Nrf2 gene expression, increases its nuclear translocation and stimulates UGT1A1 promoter activity.

(R,S)-Carvedilol glucuronide is a racemic mixture of the carvedilol metabolites (R)-carvedilol glucuronide and (S)-carvedilol glucuronide. (R)-Carvedilol glucuronide is formed via glucuronidation of (R)-carvedilol by the UDP-glucuronosyltransferase (UGT) isoforms UGT1A1 and UGT2B4. (S)-Carvedilol glucuronide is formed via glucuronidation of (S)-carvedilol by UGT2B4 and UGT2B7.

1,2,3,6-Tetragalloylglucose (TeGG) has antioxidative activity, it also shows the most potent anticomplement activity (IC50 = 34 microM). 1,2,3,6-Tetragalloylglucose is also a potent inhibitor of UDP glucuronosyltransferase 1 A1 (UGT1A1, Ki = 1.68 μM).

Raloxifene 6-glucuronide, a primary metabolite of Raloxifene, is mediated predominantly by UGT1A1 and UGT1A8.

MAT2A-IN-20 (Compound A49) is an inhibitor of methionine adenosyltransferase 2A (MAT2A) with an IC50 of ≤50 nM. It also inhibits human UGT1A1 with an IC50 of 28.45 μM. Additionally, MAT2A-IN-20 exhibits antitumor activity in mouse models.

UK-157147 is a substrate for UGT1A1 (Km: 105 μM).

Jaceosidin has anti-oxidative activity. Jaceosidin has anti-inflammatory activity, also a microglial inhibitor with anti-neuroinflammation activity. aceosidin has anticancer activity, modulates the ERK ATM Chk1 2 pathway, leading to inactivation of the Cd