Tyrosinase-IN-4

Tyrosinase-IN-4 (compound 34) is a potent tyrosinase inhibitor with potential applications in food preservation, skin-whitening agents, and the fields of food, cosmetics, agriculture, and medicine[1].

Tyrosinase-IN-40 (Compound 9r) is a competitive inhibitor of tyrosinase, boasting an IC50 value of 17.02 µM and a Ki value of 14.87 µM. This compound also exhibits antioxidant activity and can be utilized in studies related to melanin.

Tyrosinase-IN-41 (compound 7) is an inhibitor of tyrosinase with an IC50 value of 9.45 μM.

Tyrosinase-IN-42 is a tyrosinase inhibitor (IC50: 1.363 µM) that demonstrates anti-browning effects on fresh-cut apples. It exhibits the ability to scavenge DPPH and ABTS radicals, with IC50 values of 57.90 µM and 45.64 µM respectively, indicating its antioxidant activity.

Tyrosinase-IN-43 (Compound 12j) is a competitive tyrosinase inhibitor with an IC50 value of 10.49 μM for tyrosinase. It exhibits significant antioxidant activity and can be used in the study and treatment of pigmentation-related conditions such as melasma, freckles, age spots, and post-inflammatory hyperpigmentation.

Tyrosinase-IN-44 (Compound 3) is a tyrosinase inhibitor with IC50 values of 0.47 μM for monophenolase and 0.53 μM for diphenolase. It exhibits excellent glutathione peroxidase-like catalytic activity and DPPH radical scavenging activity. In banana and apple juice, Tyrosinase-IN-44 shows strong anti-browning activity by directly inhibiting polyphenol oxidase (PPO) and providing antioxidant effects. It is useful for redox regulation and food preservation.

Tyrosinase-IN-46 (Compound III19) is a tyrosinase inhibitor with IC50 values of 3.24 nM for L-dopa and 2.79 nM for L-tyrosine. It reduces melanin synthesis, exhibiting a significant anti-pigmentation effect. Tyrosinase-IN-46 is applicable in the study of pigmentation disorders.

Tyrosinase-IN-49 (Compound 12) is a potent mixed-type chalcone tyrosinase inhibitor, exhibiting an IC50 value of 0.19 μM. It demonstrates significant antioxidant potential by effectively scavenging DPPH and ABTS free radicals. The compound chelates the dinuclear copper ions at the active site of tyrosinase and reduces Cu2+ to Cu+, thereby decreasing the enzyme's catalytic activity. Tyrosinase-IN-49 has low cytotoxicity towards HEK293 cells and zebrafish embryos. Additionally, it exhibits anti-browning effects, improving food quality and serving as a potential agent in studies related to food preservation.

Tyrosinase-IN-47 (compound 6a) is a potent competitive inhibitor of tyrosinase with an IC50 of 1.43 µM and a Ki value of 0.1142 μM. It also exhibits inhibitory activity against α-Glucosidase (IC50= 36.26 μM) and acetylcholinesterase (IC50= 8.26 μM). Additionally, Tyrosinase-IN-47 has in vitro antioxidant activity, demonstrating effective scavenging abilities for DPPH (IC50= 4.75 μM) and ABTS (IC50= 0.04 μM). Furthermore, it prevents browning in freshly cut potato slices. This compound is applicable in pharmaceutical research.

Tyrosinase-IN-48 (Compound 3) is a potent and competitive chalcone-type inhibitor of tyrosinase, with an IC50 value of 0.49 μM. It exhibits significant antioxidant potential, effectively scavenging DPPH and ABTS free radicals. Tyrosinase-IN-48 chelates the dinuclear copper ions at the active center of tyrosinase and reduces Cu2+ to Cu+, thereby diminishing the enzyme's catalytic activity. It demonstrates low cytotoxicity to HEK293 cells and zebrafish embryos. Tyrosinase-IN-48 also possesses anti-browning properties, which can improve food quality and is applicable in studies related to food preservation.

1. 2,5-Dihydroxyacetophenone (Quinacetophenone) possess anti-anxiety, and neuroprotective qualities. 2. 2,5-Dihydroxyacetophenone (Quinacetophenone) reatment can induce a sustained activation of JNK, ERK1/2, and p38 MAPKs, it also can potentiate the pro-apoptotic and anti-proliferative effects of bortezomib in U266 cells. 3. 2,5-Dihydroxyacetophenone (Quinacetophenone) has anti-inflammatory activity in activated macrophages, raising the possibility that this compound has a therapeutic potential for inflammatory conditions. 4. 2,5-Dihydroxyacetophenone (Quinacetophenone) is an uncompetitive inhibitor of murine tyrosinase (K(I) 0.28mm), it strongly inhibits both melanogenesis and cellular tyrosinase activity in vitro in 3-isobutyl-1-methylxanthin-stimulated B16 mouse melanoma cells or in vivo in zebrafish and mouse models.

Tyrosinase-IN-35 (compound 6g), exhibiting a IC 50 value of 2.09 μM, serves as a more effective inhibitor of human tyrosinase compared to Kojic Acid (IC 50: 16.38 μM). At concentrations of 4 μM and 8 μM, this compound effectively lowers melanin levels in melanoma B16F10 cells in vitro.

3-(2,4-Dihydroxyphenyl)propanoic acid (Hydroumbellic acid) is a predicted metabolite generated by BioTransformer1 from the metabolism of 3-(2,4-dihydroxyphenyl)prop-2-enoic acid. It is produced by the abkar1 enzyme via a reduction-of-alpha-beta-unsaturated-compounds-pattern1 reaction in human gut microbiota.

CAY10761 is an inhibitor of ectonucleotide pyrophosphatase/phosphodiesterase 1 (ENPP1; IC50s = 467 and 429 μM for the human and snake venom enzymes, respectively).1,2 It also inhibits mushroom tyrosinase (Ki = 1.9 μM) and urease from jack bean, P. mirabilis, and B. pasteurii (IC50s = 0.093, <0.125, and 0.089 mM, respectively, at pH 8.2).3,4 |1. Khan, K.M., Fatima, N., Rasheed, M., et al. 1,3,4-Oxadiazole-2(3H)-thione and its analogues: A new class of non-competitive nucleotide pyrophosphatases/phosphodiesterases 1 inhibitors. Bioorg. Med. Chem. 17(22), 7816-7822 (2009).|2. Onyedibe, K.I., Wang, M., and Sintim, H.O. ENPP1, an old enzyme with new functions, and small molecule inhibitors - A STING in the tale of ENPP1. Molecules 24(22), E4192 (2019).|3. Ghani, U., and Ullah, N. New potent inhibitors of tyrosinase: Novel clues to binding of 1,3,4-thiadiazole-2(3H)-thiones, 1,3,4-oxadiazole-2(3H)-thiones, 4-amino-1,2,4-triazole-5(4H)-thiones, and substituted hydrazides to the dicopper active site. Bioorg. Med. Chem. 18(11), 4042-4048 (2010).|4. Amtul, Z., Rasheed, M., Choudhary, M.I., et al. Kinetics of novel competitive inhibitors of urease enzymes by a focused library of oxadiazoles/thiadiazoles and triazoles. Biochem. Biophys. Res. Commun. 319(3), 1053-1063 (2004).

1. N-trans-Feruloyltyramine (Feruloyltyramine)(NTF) has hepatoprotective effect. 2. NTF has antioxidative activity against Aβ(1-42)-induced neuronal death. 3. NTF is likely to inhibit COX enzymes, thereby suppressing P-selectin expression on platelets, is a platelet aggregation inhibitor. 4. NTF inhibits melanogenesis in a dose-dependent manner, NTF induces downregulation of tyrosinase resulted in suppression of melanin biosynthesis in murine B16 melanoma cells.

4-Ethylresorcinol has inhibitory activity against tyrosinase and acetylcholinesterase and can be used in biochemical experiments and drug synthesis.

4-Methylhistamine hydrochloride has been shown to inhibit the activity of copper-dependent enzymes such as tyrosinase and dopamine beta-hydroxylase and has also been shown to modulate the expression of genes involved in cell cycle regulation and apoptosis.

MtTMPK-IN-4 (compound 2), a para-piperidine, is a highly potent inhibitor of thymidylate kinase (MtTMPK) in Mycobacterium tuberculosis with an IC50 value of 6.1 μM, and exhibits remarkable tyrosinase inhibitory activity and potent antibacterial properties [1] [2].

4-Butylresorcinol (Butylresorcinol) is a potent inhibitor of tyrosinase(IC50 : 11.27 μM), and is used in cosmetics as a depigmenting agent.

Ac-[Nle4,D-Phe7]-α-MSH (4-10)-NH2, a melanotropin derivative and melanocyte-stimulating hormone, activates tyrosinase and demonstrates a thermoregulatory effect in rat models [1][2].

Tyrosinase-IN-22 (compound 4) serves as a potent inhibitor for tyrosinase substrates, namely L-tyrosine and L-dopa, exhibiting inhibitory concentrations (IC50s) of 60 nM and 30 nM, respectively. Additionally, it demonstrates significant antioxidant and anti-melanogenic properties, making it suitable for related research endeavors [1].

p-Anisic acid-d7 (4-Methoxybenzoic acid-d7) is the deuterium-labeled form of p-Anisic acid. The compound, also known as 4-Methoxybenzoic acid, serves as an orally administrable tyrosinase inhibitor and exhibits antioxidant, anxiolytic, anti-inflammatory, antitumor, antidiabetic, and preservative properties. In addition, p-Anisic acid is utilized as a preservative in the cosmetics industry.

2-Hydroxy-4-methoxybenzaldehyde (Standard) is a reference standard for research and analysis in studies involving 2-Hydroxy-4-methoxybenzaldehyde. 2-Hydroxy-4-methoxybenzaldehyde (4-Methoxysalicylaldehyde) is a chemical compound and an isomer of Vanillin. 2-Hydroxy-4-methoxybenzaldehyde(4-Methoxysalicylaldehyde) could be used to synthesis Urolithin M7. 2-hydroxy-4-methoxybenzaldehyde is a potent tyrosinase inhibitor from three East African medicinal plants, Mondia whitei, Rhus vulgaris Meikle, and Sclerocarya caffra Sond.

4-Butylresorcinol (Standard) is the standard substance of 4-Butylresorcinol, and it is applicable for quantitative analysis, quality control, and related research in biochemical experiments. 4-Butylresorcinol (Butylresorcinol) is a potent inhibitor of tyrosinase(IC50 : 11.27 μM), and is used in cosmetics as a depigmenting agent.