Tyrosinase

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

Glycyrrhisoflavone is a tyrosinase inhibitor with anti-inflammatory effects. Glycyrrhisoflavone inhibits α-glucosidase and monoamine oxidase.

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.

Methyl rosmarinate is a noncompetitive tyrosinase inhibitor isolated from Rabdosia serra, with an IC50 of 0.28 mM for mushroom tyrosinase. It exhibits antioxidative and antifungal activities, and also inhibits tyrosinase, α±-glucosidase, and matrix metalloproteinase-1 (MMP-1).

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.

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.

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

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

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.

Aloesin is a C-glycosylated chromone compound found in aloe (Liliaceae) that inhibits tyrosinase (IC50 = 0.9 mM), an enzyme responsible for catalyzing the first step of the conversion of tyrosine to melanin.

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.

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

5-Feruloylquinic acid (5-FQA) is a potent Sirt1 agonist and a potential lead compound for further testing in the drug development process for aging-associated diseases.

1. Mulberroside has nephroprotective, hypoglycemic, and antidiabetic effects. 2. Mulberroside A is a glycosylated stilbene of oxyresveratrol; thus, the deglycosylation of Mulberroside A resulted in enhanced inhibition of melanogenesis. 3. Mulberroside A has anti-inflammatory antiapoptotic effects. by decreasing the expressions of tumor necrosis factor-α (TNF-α), interleukin (IL)-1β, and IL-6 and inhibiting the activation of NALP3, caspase-1, and nuclear factor-κB and the phosphorylation of extracellular signal-regulated protein kinases, the c-Jun N-terminal kinase, and p38.

lavendustin C (NSC 666251) is a potent inhibitor of epidermal growth factor (EGF) receptor-associated tyrosine kinase.

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

Licraside is a tyrosinase inhibitor with an IC50 of 0.072 mM for monophenolase and can be used in studies about antibrowning and depigmenting agents.

Gnetol competitivity inhibits butyrylcholinesterase (IC50: 1.3 uM). Gnetol has a strong inhibitory effect on murine tyrosinase activity. Gnetol significantly suppresses melanin biosynthesis in murine B16 melanoma cells. It is active in the inhibition of a

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

Wilforlide A (3-Epiabruslactone A) is a natural product, separated from the ethanolic extract of tripterygium wilfordii. High-dose wilforlide A has obvious anti-inflammatory effect, but has no significant immune suppressive activity.

Temocapril is an inhibitor of tyrosine kinase.

α-Arbutin (4-hydroxyphenyl-D-lucopyranoside) is a synthetic and functional active ingredient for skin lightening.

Kojic acid is a fungal metabolite that inhibits tyrosinase, an enzyme involved in melanin synthesis, with an IC50 value of 30.6 μM for mushroom tyrosinase.

Swertiajaponin possesses antimicrobial activity.

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.

ethyl rosmarinate inhibit the activity of tyrosinase, α-glucosidase, and matrix metalloproteinase-1 (MMP-1).

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

Isosilybin A is a partial PPARγ agonist, it significantly induced ABCA1 protein expression, it inhibited both monophenolase (IC50=1.7-7.6μM) and diphenolase (IC50=12.1-44.9μM) of tyrosinase. Isosilybin A shows anti-angiogenic efficacy, it has anti-prostate cancer (PCA) activity that is mediated via cell cycle arrest and apoptosis induction.

Isoastilbin is a dihydroflavonol glycoside compound found in Rhizoma Smilacis glabrae and Astragalus membranaceus. Isoastilbin inhibits glucosyltransferase (GTase) with an IC50 value of 54.3 μg mL and possesses anti-acne and tyrosinase inhibition properties. Additionally, isoastilbin demonstrates neuroprotective, antioxidation, antimicrobial, and anti-apoptotic properties, indicating potential for Alzheimer's disease research.

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.

Mirificin (BCP10902) is an active ingredient in Tongmai formula (TMF) which is a well-known Chinese medicinal preparation. Anti-oxidant.

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.

P505-15 Acetate is a selective inhibitor of spleen tyrosine kinase that acts by suppressing leukocyte immune function and inflammation and leading to a reduction in arthritis score and attenuated histological damage.

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.

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.

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.

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

Lavendustin B is a Tyrosine Kinase Inhibitor and an inhibitor of HIV-1 integrase (IN) interaction with its cognate cellular cofactor, lens epithelium-derived growth factor (LEDGF p75).

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.

Pinocembrin chalcone is an inhibitor of tyrosinase with antimutagenic effects. Pinocembrin chalcone can be used in studies about the prevention of gastric ulcers.

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.

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

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.

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.

3',4'-Dihydroxyacetophenone (Qingxintong) is an active constituent of Chinese medicine. It is platelet aggregation Inhibitor and also has anti-arrhythmia activity.

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.

(±)-Taxifolin ((±)-Dihydroquercetin) is the racemate of Taxifolin, a flavonoid with anti-tyrosinase and anti-fibrotic activity, commonly found in onion, silymarin, French maritime pine bark, and Douglas fir bark. It inhibits collagenase with an IC50 value of 193.3 μM and acts as a free radical scavenger with antioxidant capacity.