tyrosinase-in-1

Tyrosinase-IN-1 (compound 90) 是有效的酪氨酸酶抑制剂。酪氨酸酶是一个很前途的靶点，酪氨酸酶抑制剂可用作美白剂和食品防腐剂，因此在食品、化妆品、农业和医药等领域具有广阔的应用前景。

Tyrosinase-IN-16对酪氨酸酶具有抑制作用。

Tyrosinase-IN-12(Non-competitive tyrosinase inhibitor) 是一种有效的非竞争性酪氨酸酶抑制剂，IC50 值为 49.33 ± 2.64 µM，Ki 值为31.25 ± 0.25 µM。Tyrosinase-IN-12 具有显著的抗氧化和自由基清除活性，减少活性氧 (ROS) 的产生（IC50:25.39 ± 0.77 µM)。Tyrosinase-IN-12 可用于研究食品和水果中物质的褐变。

Tyrosinase-IN-13 (compound 3c)为Flurbiprofen的衍生物，具有非竞争性酪氨酸酶抑制活性（IC50=68 μM；Ki=36.3 μM），并对肝细胞癌（HepG2）、结直肠癌（HT-29）及黑色素瘤（B16F10）细胞表现出细胞毒性。

Tyrosinase-IN-14 (compound 7m) 是一种针对酪氨酸酶的抑制剂, 它通过改变酪氨酸酶的二级结构来降低其催化活性。此化合物的细胞毒性较低, 并且在水果抗褐变方面显示出活性。特别是，Tyrosinase-IN-14 在抑制香蕉储藏期间的褐变方面表现出了有效性。

Tyrosinase-IN-19 是竞争性酪氨酸酶抑制剂，对ROS、ABTS+ 及DPPH 自由基展现显著的抗氧化活性。该化合物通过剂量依赖性方式有效抑制酪氨酸酶表达。

Tyrosinase-IN-15 (Compound 39)为酪氨酸酶抑制剂，具有IC50值为7.12 μM及Ki值为11.8 μM。

Tyrosinase-IN-17 (Compound 5b), characterized as a lipophilic, skin-permeable, and non-cytotoxic tyrosinase inhibitor (pIC 50 = 4.99), is suited for research into melanin-related diseases, including melanoma and melanogenesis [1].

Tyrosinase-IN-11 是一种有效的酪氨酸酶 (tyrosinase) 抑制剂，对 L-酪氨酸酶和 L-多巴的 IC50值分别为 50 nM 和 64 nM。Tyrosinase-IN-11 具有显着的抗氧化活性和低细胞毒性。Tyrosinase-IN-11 具有用于皮肤色素沉着过度研究的潜力。

Tyrosinase-IN-10 是一种部分竞争性酪氨酸酶 (tyrosinase) 抑制剂，其 IC50为 1.6 μM，可抑制人黑素瘤细胞裂解物中的酪氨酸酶活性。

2,5-Dihydroxyacetophenone (Quinacetophenone) 是从熟地黄中分离出的一种天然产物，通过阻断 ERK1 2和 NF-κB 信号通路，抑制活化巨噬细胞中炎症介质的产生。

Trans-caffeic acid（Trans-咖啡酸）可作为高灵敏的荧光探针检测食物中的漆酶（laccase），还可以刺激胚芽组织的生长。

hTYR AbTYR-IN-1 是一种 hTYR AbTYR 双重抑制剂，对 hTYR 和 AbTYR 具有抑制作用， IC50 分别为 5.4 μM 和 3.52 μM。hTYR AbTYR-IN-1 可用于研究人类色素沉着过度和黑色素瘤。

Noroxyhydrastinine exhibits potent melanogenesis-inhibitory activities, it inhibits melanogenesis, at least in part, by inhibiting the expression of protein levels of tyrosinase, TRP-1, and TRP-2 in α-MSH-stimulated B16 melanoma cells.

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).

N-trans-Feruloyltyramine (Feruloyltyramine) 是从大麻中分离得到的一种生物碱，是COX1和COX2的抑制剂，具有抗氧化和抗炎活性。

Tyrosinase-IN-2 (compound 67) 是一种有效的酪氨酸酶抑制剂。酪氨酸酶是一种含铜金属酶，负责黑色素生物合成和酶促褐变中的限速催化步骤。Tyrosinase-IN-2 具有研究皮肤美白剂和食品防腐剂的潜力。

Tyrosinase-IN-4 (compound 34) 是一种有效的酪氨酸酶抑制剂。酪氨酸酶是一种有前途的靶点，酪氨酸酶抑制剂可用作皮肤美白剂和食品防腐剂。 Tyrosinase-IN-4 在食品、化妆品、农业和医药等领域具有应用潜力[1]。

Tyrosinase-IN-5 (compound 16c) is a highly effective inhibitor of tyrosinase, exhibiting an IC50 value of 0.02 μM. This compound efficiently suppresses melanogenesis while posing minimal toxicity to cells [1].

Tyrosinase-IN-3 (compound 54) is a powerful tyrosinase inhibitor, an enzyme involved in the key catalytic step of melanin biosynthesis and enzymatic browning. As a copper-containing metalloenzyme, tyrosinase plays a crucial role in these processes. The compound shows promise for studying skin whitening agents and food preservatives [1].

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

Gnetol 是从买麻藤的根中分离出来的一种酚类。它是酪氨酸酶抑制剂，对鼠酪氨酸酶的 IC50为 4.5 μM，可抑制黑色素的生物合成。它有效抑制 COX-1和 HDAC，具有抗氧化、抗增殖、抗癌和保肝活性，还具有浓度依赖性的 α-淀粉酶、α-葡萄糖苷酶和脂肪形成活性。

Tyrosinase elastase-IN-1，一种来源于悬钩子叶的三萜类化合物，具有抑制酪氨酸酶和弹性蛋白酶活性的功能。

5-epi-Arvestonate A是一种从(Seriphidium transiliense)绢毛菊中提取的倍半萜化合物，能够通过激活(MITF)小眼相关转录因子和酪氨酸酶家族基因来促进黑色素的产生。此外，5-epi-Arvestonate A还能通过JAK STAT信号通路，抑制永生化人角化细胞(HaCaT)中IFN-γ趋化因子的表达。