tyrosinase

Tyrosinase (Polyphenol oxidase), a rate-limiting enzyme encoded by the TYR gene, regulates melanin production and is primarily found in melanosomes synthesized by skin melanocytes [1].

Tyrosinase-IN-2 (compound 67) is a potent inhibitor of tyrosinase, a copper-containing metalloenzyme crucial for the rate-limiting step in melanin biosynthesis and enzymatic browning processes. This compound shows promise for research into skin whitening agents and food preservatives [1].

Tyrosinase-IN-19 (compound 9), a competitive tyrosinase inhibitor, exhibits potent antioxidant activities by neutralizing ROS, ABTS+, and DPPH radicals and demonstrates dose-dependent suppression of tyrosinase expression [1].

Tyrosinase-IN-15 (Compound 39), with an IC50 of 7.12 μM and a Ki of 11.8 μM, functions as a tyrosinase inhibitor [1].

Tyrosinase-IN-14 (compound 7m), a tyrosinase inhibitor, modulates the enzyme's secondary structure to diminish its catalytic function, exhibits low cytotoxicity, and possesses anti-browning properties that effectively prevent banana discoloration during storage [1].

Tyrosinase-IN-12(Non-competitive tyrosinase inhibitor) is a potent non-competitive tyrosinase inhibitor with an IC50 of 49.33 ± 2.64 µM and a Ki of 31.25 ± 0.25 µM. Tyrosinase-IN-12 has significant antioxidant and free radical scavenging activity (IC50:25.39 ± 0.77 µM), reducing reactive oxygen species (ROS) production. Tyrosinase inhibitor (Tyrosinase-IN-12) has significant antioxidant and free radical scavenging activity and reduces the production of reactive oxygen species (ROS) (IC50:25.39 ± 0.77 µM).Tyrosinase-IN-12 can be used for the study of browning of substances in food and fruits.

Tyrosinase-IN-13 (compound 3c), derived from Flurbiprofen, serves as a potent non-competitive inhibitor of tyrosinase with IC50 and Ki values of 68 μM and 36.3 μM, respectively. It exhibits cytotoxicity against several cancer cell lines, including hepatocellular carcinoma (HepG2), colorectal cancer (HT-29), and melanoma (B16F10) [1].

Arbutin (p-Arbutin)(β-Arbutin) is a glycosylated hydroquinone extracted from the bearberry plant in the genus Arctostaphylos and can inhibit tyrosinase and thus prevent the formation of melanin.

Methyl cinnamate, a tyrosinase inhibitor and a flavoring compound, has antimicrobial, antiadipogenic, vasorelaxant, and anti-inflammatory effects.

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

3-O-Ethyl-L-ascorbic acid is a cosmetic tyrosinase inhibitor with whitening ability and is a stabilized vitamin C derivative. It also has antioxidant properties.

Glycolic acid, an inhibitor of tyrosinase, suppresses melanin formation and is used in skincare products.

3,4-Dimethoxyphenol (4-Hydroxyveratrole) is an active biochemical.

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.

1. 2-Methoxycinnamic acid (o-Methoxycinnamic acid) can enhance inhibition of tyrosinase activity.

Taxifolin (Dihydroquercetin) is a flavonoid in many plants such as Taxus chinensis, Siberian larch, Cedrus deodara and so on.

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.

3,5-Dimethoxyphenol (Phloroglucinol dimethyl ether) as a marker of Taxus poisoning, being present in all species of Taxus. It has potent tyrosinase-inhibiting activity.

Aloin (Aloin-A)(mixture of A&B), a natural anthracycline from Aloe vera, is a tyrosinase inhibitor.

Benzylacetone (4-Phenyl-2-butanone) is an aromatic compound extracted from incense wood. Benzylacetone has appetite-enhancing and exercise-reducing properties. Benzylacetone has a strong and reversible anti-mushroom tyrosinase effect, with IC50 values of 2.8 mM and 0.6 mM for monophenolase and biphenolase effects, respectively.

DeoxyArbutin(IC50=50 nM) inhibits tyrosinase activity reversibly.

2-Ketoglutaric acid Sodium (AKG) is a key molecule in the TCA cycle. It can be produced from glutamate by oxidative deamination via glutamate dehydrogenase and as a product of pyridoxal phosphate-dependent transamination reactions (mediated by branched-chain amino acid transaminases) in which glutamate is a common amino donor.

2-Ketoglutaric acid is a key molecule in the tricarboxylic acid cycle,is also connected to glutamic acid and glutamine metabolisms through the transamination reactions.

D-Tyrosine, the D-isomer of tyrosine, acts as a negative regulator of melanin synthesis by inhibiting tyrosinase activity. Furthermore, D-Tyrosine also inhibits biofilm formation and induces the self-dispersal of biofilms, while not affecting bacterial growth.

1. Oxyresveratro can inhibit tyrosinase activity. 2. Oxyresveratro is useful to trauma models, as toxicity to glia could be beneficial by inhibiting reactive gliosis. 3. Oxyresveratrol (trans-Oxyresveratrol) has antioxidant activity, can reduce neuronal oxidative damage and protect hepatocytes against oxidative stress and mitochondrial dysfunction, which may be associated with activation of Nrf2.

Glabridin (KB-289522) may serve as an anti-inflammatory agent in diabetes-related vascular dysfunction, through regulating the synthesis and activity of iNOS under high-glucose levels; may possess a therapeutic effect on metabolic disorders( such as diabetes and hyperglycemia), by modulating glucose metabolism through AMPK in skeletal muscle cells. Glabridin may have potential as a chemopreventive agent against liver Y metastasis, by inhibiting the invasion of human HCC cells.

4-Chlorosalicylic acid (4-Chloro-2-hydroxybenzoic acid, 4-chloro salicylic acid) is antimicrobial compositions comprising a metal salt and a benzoic acid analog.

Hexylresorcinol (4-Hexylresorcinol) is a substituted dihydroxybenzene utilized topically as an antiseptic for minor skin infection treatment.

Monobenzone (Benoquin) is a Depigmenting Agent. The mechanism of action of monobenzone is as a Melanin Synthesis Inhibitor. The physiologic effect of monobenzone is by means of Depigmenting Activity.

Potassium iodide is used as the treatment of overactive thyroid and as protection of the thyroid gland from the influences of radiation from swallowed or inhaled radioactive iodine. It may be used after accidental exposure to radioactive iodine or before and after administration of medicine containing radioactive iodine.

Mizoribine (NSC-289637) belongs to the family of 1-Ribosyl-imidazolecarboxamides. Mizoribine has been investigated for the treatment of Rheumatoid Arthritis.

Isobarbaloin (Barbaloin-A) (Aloin) is a natural anthracycline from Aloe vera, is a tyrosinase inhibitor.

(+)-Isocorydine hydrochloride (Isocorydine HCl) is a eukaryote protein kinases Inhibitor.

Etarotene (Arotinoid ethyl sulphone) is an ethylsulfonyl derivative of aloe acid with differentiation-inducing and potentially antitumor activity.Etarotene is a collagenase inhibitor and can be used to study psoriasis.

KW-2450 Formate is an IGF-1R/IR tyrosine kinase inhibitor with antitumor effects that acts through inhibition of Aurora A and B kinases.KW-2450 Formate inhibits the growth of TNBC xenografts and induces tetraploid accumulation.

EHT 1610 (EHT 5372) is a potent inhibitor of DYRK, with an IC50 of 0.36 nM and 0.59 nM for DYRK1A and DYRK1B, respectively. EHT 1610 has an inhibitory effect on leukemia, regulating cell cycle and inducing cell apoptosis.

Calycosin (Cyclosin) acts as a selective estrogen receptor modulator. Calycosin induces apoptosis in human ovarian cancer SKOV3 cells by activating caspases and Bcl-2 family proteins. Calycosin suppresses breast cancer cell growth via ERβ-dependent regulation of IGF-1R, p38 MAPK and PI3K/Akt pathways. Calycosin has antineoplastic effects against osteosarcoma through inducing apoptosis showing in vitro and in vivo investigations. Calycosin was shown to induce angiogenesis in human umbilical vein endothelial cell cultures (HUVEC) in vitro. Calycosin may be an effective skin-lightening agent that regulates the expression of melanogenic enzymes. Calycosin exhibited tyrosinase inhibitory activity with an IC(50) value of 38.4 microM.

XMD16-5 is a TNK2 inhibitor. TNK2 genomic amplification has been associated with late-stage or metastatic lung and prostate Ys. Overexpression of TNK2 promoted metastasis in a mouse model of breast Y. TNK2 signaling is disrupted in breast, prostate and ga

Trifolirhizin exerts varying degrees of inhibition on tyrosinase-dependent melanin biosynthesis, and therefore, are candidates as skin-whitening agents.Trifolirhizin possesses potential anti-inflammatory and anti-cancer activities.Trifolirhizin shows in vitro inhibitory effects on the growth of human A2780 ovarian and H23 lung cancer cells. Trifolirhizin inhibits acetylcholine mediated airway smooth muscle (ASM) contraction or directly relaxes pre-contracted ASM independent of β 2 -adrenoceptors.

Benzoyloxypaeoniflorin (Benzoyloxypeoniflorin) is a natural product,contributes to improving blood circulation through their inhibitory effects on both platelet aggregation and blood coagulation.

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.

XMD8-87 (ACK1-B19) is a TNK2 inhibitor with activity in the inhibition of TNK2 phosphorylation. XMD8-87 and XMD16-5 potently inhibit phosphorylation of TNK2 truncation mutations found in solid tumor types.

SU-4942 is a regulator of tyrosine kinase signaling. It inhibits VEGF and endothelial cell growth factor (ECGF)-induced mitosis in endothelial cells (US5792783A).

ZAP-180013 is an inhibitor of zeta-chain-associated protein kinase 70 (ZAP70,IC50 : 1.8 μM).

SU5214 is a modulator of tyrosine kinase signal transduction.

Toceranib Phosphate (SU11654 phosphate), is a selective inhibitor of the tyrosine kinase activity of several members of the split kinase RTK family, including Flk-1 KDR, PDGFR

Kurarinol is a potent inhibitor of sortase A, with an IC50 value of 107.7 ± 6.6 μM. Kurarinol has extremely strong tyrosinase inhibitory activity, exerts varying degrees of inhibition on tyrosinase-dependent melanin biosynthesis, is a candidate as skin-whitening agents.

Viscumneoside III, a dihydroflavone O-glycoside, is a potent tyrosinase inhibitor with an IC50 of 0.5 mM, and has anti-angina pectoris properties.