Tyrosinase

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).

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.

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

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.

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.

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.

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

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

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.

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.

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).

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

Temocapril is an inhibitor of tyrosine kinase.

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.

Swertiajaponin possesses antimicrobial activity.

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

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).

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.

Retusin is derived from the leaves of Talinum triangulare. Retusin Retusin can be used in studies about acting as pre- and postemergent herbicides.

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.

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

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.

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

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.

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.

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.

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

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

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-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.

(±)-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.

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

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.

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.

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

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.

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

(Z)-SU14813 is a novel tyrosine kinase inhibitor with anticardiogenic and antitumor activity that inhibits VEGFR-2, PDGFR-β, and FLT3 phosphorylation in xenograft tumors in a dose- and time-dependent manner.

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.

SU5214 is a modulator of tyrosine kinase signal transduction.

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

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].