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Enzymes(酶)

Enzymes are very efficient and specific catalyst proteins which react with 1 or few types of substrates in biochemical reactions and are responsible for bringing about almost all of the chemical reactions in living organisms. Enzymes speed up reactions by providing an alternative reaction pathway of lower activation energy. Without enzymes, reactions take place at a rate far too slow for the pace of metabolism which means that they speed up the chemical reactions in living things.

There are 2 types of enzymes, ones that help join specific molecules together to form new molecules & others that help break specific molecules apart into separate molecules. Enzymes play many important roles ouside the cell as well. One of the best examples of this is the digestive system. For instance, it is enzymes in your digestive system that break food down in your digestive system break food down into small molecules that can be absorbed by the body. Some enzymes in your digestive system break down starch, some proteins and others break down fats. The enzymes used to digest our food are extra-cellular since they are located outside our cells & enzymes inside our cells are intra-cellular enzymes. Enzymes are used in ALL chemical reactions in living things; this includes respiration, photosynthesis, movement growth, getting rid of toxic chemicals in the liver and so on. Enzymes are proteins that must have the correct structure to be active. They are very easily affected by heat, pH and heavy metal ions.

Ribonucleoprotein enzyme catalytic activity is located in the protein part but for some the catalytic activity is in the RNA part. A catalyst is any substance which makes a chemical reaction go faster, without itself being changed. A catalyst can be used over and over again in a chemical reaction and does not get used up.

Enzymes lower the amount of activation energy needed by binding to the reactants of the reaction they catalyze, thus speed up the reaction and can process millions of molecules per second. Enzymes are typically large proteins with high molecular weight that permit reactions to go at conditions that the body can tolerate.

Enzyme nomenclature is based on what the enzyme reacts with & how it reacts along with the ending ase.

Enzymes must get over the activation energy hurdle.

Enzymes change how a reaction will proceed which reduces the activation energy and makes it faster. The more we increase the enzyme concentration the faster the reaction rate for non-catalyzed reactions. Enzymes that are catalyzed reactions also increase reaction rate at higher level of concentration but up to a certain point called Vmax which means that the enzyme has reached its maximum point. The reaction is limited by both the concentrations of the enzyme and substrate. Enzymes as catalysts take part in reactions which provide an alternative reaction pathway. Enzymes do not undergo permanent changes and remain unchanged at the end of the reaction. They only change the rate of reaction, not the position of the equilibrium.Enzymes as catalysts are highly selective by only catalysing specific reactions due to the shapes of the enzyme’s molecule.

Enzymes contain a globular protein part called apoenzyme and a non-protein part named cofactor or prosthetic group or metal-ion-activator. Changes in temperature and pH have great influence on the intra- and intermolecular bonds that hold the protein part in their secondary and tertiary structures.

Examples of cofactors are 1. Prosthetic group that are permanently bound to the enzyme. 2. Activator group which are cations (positively charged metal ions) & temporarily bind to the active site of the enzyme. 3.Coenzymes, usually vitamins or made from vitamins which are not permanently bound to the enzyme molecule, but combine with the enzyme-substrate complex temporarily. Enzymes require the presence cofactors before their catalytic activity can be exerted. This entire active complex is referred to as the holoenzyme.

Without enzymes, our guts would take weeks to digest our food, our muscles, nerves and bones would not work properly and so on…

Main Enzyme category groups:

Oxidoreductases:
All enzymes that catalyse oxido-reductions belong in this class. The substrate oxidized is regarded as a hydrogen or electron donor. The classification is based on 'donor:acceptor oxidoreductase'. The common name is 'dehydrogenase', wherever this is possible; as an alternative, 'acceptor reductase' can be used. 'Oxidase' is used only where O2 is an acceptor. Classification is difficult in some cases, because of the lack of specificity towards the acceptor.

Transferases:
Transferases are enzymes that transfer a group, for example, the methyl group or a glycosyl group, from one compound (generally regarded as donor) to another compound (generally regarded as acceptor). The classification is based on the scheme 'donor:acceptor grouptransferase'. The common names are normally formed as 'acceptor grouptransferase' or 'donor grouptransferase'. In many cases, the donor is a cofactor (coenzyme) that carries the group to be transferred. The aminotransferases constitute a special case.

Hydrolases:
These enzymes catalyse the hydrolysis of various bonds. Some of these enzymes pose problems because they have a very wide specificity, and it is not easy to decide if two preparations described by different authors are the same, or if they should be listed under different entries. While the systematic name always includes 'hydrolase', the common name is, in most cases, formed by the name of the substrate with the suffix -ase. It is understood that the name of the substrate with this suffix, and no other indicator, means a hydrolytic enzyme. It should be noted that peptidases have recommended names rather than common names.

Lyases:
Lyases are enzymes that cleave C-C, C-O, C-N and other bonds by means other than by hydrolysis or oxidation. They differ from other enzymes in that two (or more) substrates are involved in one reaction direction, but there is one compound fewer in the other direction. When acting on the single substrate, a molecule is eliminated and this generates either a new double bond or a new ring. The systematic name is formed according to 'substrate group-lyase'. In common names, expressions like decarboxylase, aldolase, etc. are used. 'Dehydratase' is used for those enzymes that eliminate water. In cases where the reverse reaction is the more important, or the only one to be demonstrated, 'synthase' may be used in the name.

Ligases:
Ligases are enzymes that catalyse the joining of two molecules with concomitant hydrolysis of the diphosphate bond in ATP or a similar triphosphate. 'Ligase' is often used for the common name, but, in a few cases, 'synthase' or 'carboxylase' is used. 'Synthetase' may be used in place of 'synthase' for enzymes in this class.

Products for  Enzymes

  1. Cat.No. 产品名称 Information
  2. GC66360 Girentuximab Girentuximab (G250) 是一种嵌合单克隆抗体,可与碳酸酐酶 IX (CAIX) 结合,碳酸酐酶 IX 是一种在透明细胞肾细胞癌 (ccRCC) 中广泛表达的细胞表面糖蛋白。
  3. GC66033 Casein kinase 1δ-IN-1 Casein kinase 1δ-IN-1 (compound 822) 是酪蛋白激酶 1δ (CK1δ) 的抑制剂,抑制作用大于5%。Casein kinase 1δ-IN-1 可用于神经退行性疾病,如阿尔茨海默病的研究。
  4. GC66029 hCAI/II-IN-6 hCAI/II-IN-6 是一种具有口服活性的 human carbonic anhydrase (CA) 抑制剂。hCAI/II-IN-6 选择性地抑制 hCA II 和 hCA VII,对 hCA I,hCA II,hCA VII 和 hCA XII 的 Ki 值分别为 220,4.9,6.5 和 >50000 nM。hCAI/II-IN-6 在体内显示抗惊厥活性和抗最大电击 (MES) 活性。hCAI/II-IN-6 可以用于癫痫的研究。
  5. GC65998 Cathepsin C-IN-5 Cathepsin C-IN-5 (compound SF38) 是一种有效的、选择性的和具有口服活性的 组织蛋白酶 C 抑制剂,Cat C、Cat L、Cat S、Cat B、Cat K 的 IC50s 分别为 59.9 nM, 4.26 µM、>5 µM、>5 µM、>5 µM。Cathepsin C-IN-5 抑制骨髓和血液中的 Cat C 活性。Cathepsin C-IN-5 降低 NSP(中性粒细胞丝氨酸蛋白酶)的活化。Cathepsin C-IN-5 具有抗炎活性。
  6. GC65957 MMP13-IN-2 MMP13-IN-2 是一种有效、选择性和口服活性的 MMP-13 抑制剂。MMP13-IN-2 对 MMP-13 具有优异的效价 (IC50=0.036 nM),对 MMP-1、3、7、8、9、14 和 TACE 的选择性(大于 1500 倍)。MMP13-IN-2 在体外具有阻止软骨释放胶原蛋白的能力。MMP13-IN-2 具有胶原酶相关疾病研究的潜力。
  7. GC65938 Thrombin inhibitor 5 Thrombin inhibitor 5 (compound 385) 是一种凝血酶抑制剂,IC50 范围为 0.1 μM-1 μM。Thrombin inhibitor 5 可用于静脉血栓栓塞的研究。
  8. GC65668 5-Amino-8-hydroxyquinoline 5-氨基-8-羟基喹啉(5A8HQ)是一种潜在的抗癌候选药物,具有良好的蛋白酶体抑制活性
  9. GC65612 Acetazolamide sodium Acetazolamide sodium 是一种碳酸酐酶 (CA) IX 抑制剂,对 hCA IX 的 IC50 为 30 nM。Acetazolamide 具有利尿、抗高血压和抗淋球菌活性。
  10. GC52175 IQA A CK2 inhibitor
  11. GC65549 Indisulam Indisulam (E 7070) 是一种碳酸酐酶抑制剂,具有抗癌活性。Indisulam (E 7070) 是细胞周期 G1 期的靶向化合物。Indisulam (E 7070) 通过抑制 CDK2 和周期蛋白 E 的激活,引起 G1/S 转化被阻滞。Indisulam (E 7070) 通过募集 DCAF15 诱导 RBM39 降解来靶向剪接。
  12. GC65547 (1S,2R)-Alicapistat (1S,2R)-Alicapistat ((1S,2R)-ABT-957) 是一种具有口服活性的人钙激活中性蛋白酶 (calpains 1 和 2) 的选择性抑制剂,可能用于阿尔茨海默病 (AD) 的研究。 Alicapistat 可减轻羰基还原的代谢倾向,对 calpain 1 的 IC50 为 395 nM。
  13. GC65542 NSC-87877 disodium NSC-87877 disodium 是一种有效的Shp2 和Shp1 蛋白质酪氨酸磷酸酶抑制剂,IC50 值分别为0.318 μM 和0.355 μM。NSC-87877还抑制双特异性磷酸酶26 (DUSP26)。
  14. GC65533 SHP394 SHP394 是一种有效的,具有口服活性的,变构的选择性SHP2 抑制剂,IC50 为 23 nM。
  15. GC65432 LV-320 LV-320 是一种有效且非竞争性的 ATG4B 抑制剂,其 IC50 值为 24.5 μM,Kd 值为 16 μM。 LV-320 抑制 ATG4B 的酶促活性,阻断细胞自噬,并且在体内稳定,无毒且有活性。
  16. GC65394 7-BIA 7-BIA 是一种受体型蛋白酪氨酸磷酸酶 D (PTPRD) 抑制剂,IC50 值约为 1-3 μM。
  17. GC65308 SHIP2-IN-1 SHIP2-IN-1 是一种有效的 SHIP2 抑制剂,IC50 值为 2 µM。SHIP2-IN-1 可使 GSK3β 的 Ser9 位点磷酸化,抑制 GSK3β 的活化。SHIP2-IN-1 可用于阿尔滋海默症的研究。
  18. GC65307 S130 S130 是一种高亲和力、选择性的半胱氨酸蛋白酶 ATG4B 的抑制剂, IC50 值为 3.24 µM。S130 可以抑制自噬通量。
  19. GC65271 p-Hydroxyphenethyl trans-ferulate p-Hydroxyphenethyl trans-ferulate 具有抗高血糖 (酵母α-葡萄糖苷酶,IC50 19.24 ± 1.73 µmol L-1),抗氧化,抗炎活性。p-Hydroxyphenethyl trans-ferulate 具有抗癌活性和血清素能活性。
  20. GC65260 EDP-305 EDP-305 是一种口服有效且选择性的 farnesoid X 受体 (FXR) 激动剂,其 EC50 值为 34 nM (CHO 细胞嵌合性 FXR) 和 8 nM (HEK 细胞全长 FXR)。EDP-305 显示出强大而持久的抗纤维化作用。EDP-305 可用于原发性胆道胆管炎 (PBC) 和非酒精性脂肪性肝炎 (NASH) 研究。
  21. GC65157 Naphthol AS-BR Naphthol AS-BR 是组织化学中,酸性和碱性磷酸酶的底物。
  22. GC65153 KGP94 KGP94 是一种特异的 cathepsin L 抑制剂,IC50为 189 nM。KGP94 抑制转移癌的运动性和侵袭性,对人类细胞的毒性低 (GI50=26.9µM)。
  23. GC65098 ARL67156 triethylamine ARL67156 (FPL 67156) triethylamine 是一种 ecto-ATPase 抑制剂。ARL67156 triethylamine 是竞争性 NTPDase1 (CD39),NTPDase3 和 NPP1 抑制剂,Ki 分别为 11,18 和 12 μM。ARL67156 triethylamine 可用于钙化性主动脉瓣疾病、哮喘等疾病的研究。
  24. GC65097 ARL67156 trisodium hydrate ARL67156 (FPL 67156) trisodium hydrate 是一种 ecto-ATPase 抑制剂。ARL67156 trisodium hydrate 是竞争性 NTPDase1 (CD39),NTPDase3 和 NPP1 抑制剂,Ki 分别为 11,18 和 12 μM。ARL67156 trisodium hydrate 可用于钙化性主动脉瓣疾病、哮喘等疾病的研究。
  25. GC65025 BCI hydrochloride BCI hydrochloride ((E)-BCI hydrochloride) 是一种双重特异性磷酸酶 (DUSP) 的变构抑制剂。BCI hydrochloride 特异性抑制 DUSP6 和 DUSP1 的 EC50 分别为 13.3 和 8.0 μM。BCI hydrochloride 不抑制 DUSP5。
  26. GC65010 Bortezomib-d8 Bortezomib-d8 (PS-341-d8) 是 Bortezomib 的氘代物。Bortezomib (PS-341) 是一种可逆性和选择性的蛋白酶体 (proteasome) 抑制剂,通过靶向苏氨酸残基有效抑制 20S 蛋白酶体 (Ki=0.6 nM)。Bortezomib 破坏细胞周期、诱导细胞凋亡以及抑制核因子 NF-κB。Bortezomib 是第一种蛋白酶体抑制剂,具有抗癌活性。
  27. GC64992 YH-306 YH-306 是一种抗肿瘤剂。YH-306 通过 FAK 通路抑制结直肠肿瘤的生长和转移。 YH-306 显着抑制结直肠癌细胞的迁移和侵袭。YH-306 有效抑制不受抑制的增殖并诱导细胞凋亡 (apoptosis)。YH-306 抑制 FAK、c-Src、桩蛋白和 PI3K、Rac1 的激活以及 MMP2 和 MMP9 的表达。YH-306 还抑制肌动蛋白相关蛋白 (Arp2/3) 复合物介导的肌动蛋白聚合。
  28. GC64936 TD52 dihydrochloride TD52 dihydrochloride 是 Erlotinib 衍生物,一种具有口服活性的强效癌性蛋白磷酸酶 2A (CIP2A) 抑制剂。TD52 dihydrochloride 通过调节 CIP2A/PP2A/p-Akt 信号通路介导三阴性乳腺癌 (TNBC) 细胞的凋亡作用。TD52 dihydrochloride 通过干扰 Elk1 与 CIP2A 启动子的结合间接减少 CIP2A。TD52 dihydrochloride 具有小的 p-EGFR 抑制作用并具有抗癌活性。
  29. GC64734 Benzenesulphonamide Benzenesulphonamide (compound 1) 是一种有效的碳酸酐酶抑制剂。Benzenesulphonamide 显示出 CA II 抑制活性。
  30. GC64638 ALV1 ALV1 是一种有效的 Ikaros 和 Helios 降解剂。ALV1 能显著降低 IKZF1-4、CK1α (酪蛋白激酶 1α,CSNK1A1) 和核糖体蛋白 RPL4 的蛋白丰度。ALV1 对和 IKZF1/2/3 表现出相似的降解活性。ALV1 诱导 Helios/CRBN 二聚反应。ALV1 在很大程度上促进了 IL-2 的分泌。
  31. GC64607 Dazcapistat Dazcapistat 是一种有效的钙蛋白酶 (calpain) 抑制剂,对 calpain 1, calpain 2 和calpain 9 的 IC50 值为 <3 μM (详细信息请参见专利WO2018064119A1, compound 405)。
  32. GC64605 MY33-3 hydrochloride MY33-3 hydrochloride 是一种有效和选择性的蛋白酪氨酸磷酸酶 RPTPβ/ζ 抑制剂,IC50 值为 ~0.1 μM。MY33-3 hydrochloride 还抑制 PTP-1B (IC50 ~0.7 μM)。MY33-3 hydrochloride 可以减少乙醇消耗并缓解 Sevoflurane 引起的神经炎症和认知功能障碍。
  33. GC64556 PTP1B-IN-15 PTP1B-IN-15 是一种有效的选择性蛋白酪氨酸磷酸酶 1B (PTP1B) 抑制剂。PTP1B-IN-15具有研究II型糖尿病和肥胖症的潜力。
  34. GC64535 (S,S)-TAPI-1 (S,S)-TAPI-1 是 TAPI-1 的异构体。TAPI-1是一种 TACE (ADAM17) 抑制剂,可阻止多种细胞表面蛋白脱落。TAPI-1 也是金属蛋白酶 (MMP) 抑制剂。
  35. GC64519 Kaempferol-3,7-di-O-β-glucoside Kaempferol-3,7-di-O-β-glucoside (Kaempferol 3,7-diglucoside) 是一种黄酮醇,对 α-淀粉酶 (α-amylase)、α-葡萄糖苷酶 (α-glucosidase) 和乙酰胆碱酯酶 (Acetylcholinesterase) 具有酶抑制作用。Kaempferol-3,7-di-O-β-glucoside 保护分化神经元细胞 SH-SY5Y 免受 Amyloid β 肽诱导的损伤。Kaempferol-3,7-di-O-β-glucoside 具有用于研究阿尔茨海默氏症的潜力。
  36. GC64507 ML198 ML198 是一种葡萄糖脑苷脂酶 (GCase) 调节剂,EC50 为 0.4 μM。ML198 是葡萄糖脑苷脂酶的激活剂和非抑制性伴侣。ML198 可用于戈谢病的研究。
  37. GC64472 20S Proteasome-IN-1 20S Proteasome-IN-1 是一种 26S proteasome 抑制剂,详细信息请参考专利文献 WO2006128196A2 中的化合物 2。20S Proteasome-IN-1 具有用于癌症,免疫相关疾病,炎症,缺血性疾病,神经退行性疾病和其他疾病研究的潜力。
  38. GC64382 SGC-CK2-1 SGC-CK2-1 是一种高效、ATP 竞争性的 CK2 化学探针,对两种人 CK2 亚型 CK2α 和 CK2α' 具有选择性,IC50分别为 36 和 16 nM。SGC-CK2-1 可用于神经退行性疾病的研究。
  39. GC64376 GDC-1971 GDC-1971 (compound 199) 是 SHP2 的抑制剂。
  40. GC64338 LYP-IN-1 LYP-IN-1 是一种有效、选择性和特异性的 LYP 抑制剂,其 Ki,IC50 的值分别为 110 nM 和 0.259 μM。LYP-IN-1 对一些 PTPs 也有选择性,如 SHP1 (IC50=5 μM) 和 SHP2 (IC50=2.5 μM)。LYP-IN-1 在 T 细胞和肥大细胞中表现出高效的细胞活性。LYP-IN-1 可用于研究自身免疫性疾病。
  41. GC64282 LXE408 LXE408 是一种口服有效的,非竞争性的,动素体选择性蛋白酶体 (proteasome) 抑制剂。LXE408 抑制 L. donovani 蛋白酶体 (IC50=0.04 μM) 和 L. donovani (EC50=0.04 μM)。LXE408 具有较弱的透过血脑屏障能力。LXE408 具有用于内脏利什曼病 (VL) 研究的潜力。
  42. GC64213 GSK3494245 GSK3494245 (DDD01305143) 是一种有效的、具有口服活性的、选择性的可在夹在 β4 和 β5 亚基之间的位点结合寄生虫蛋白酶体 (proteasome) 的糜蛋白酶样活性抑制剂(对于 WT L.donovani蛋白酶体IC50=0.16μM)。GSK3494245 适度抑制人蛋白酶体的糜蛋白酶样活性 (IC50: 26S=13 µM;富集的 THP-1 提取物 IC50=40 µM)。GSK3494245 具有良好的生物安全特性。
  43. GC64202 Ganoderlactone D Ganoderlactone D 对酵母中的α-葡萄糖苷酶有抑制活性,IC50 为 41.7 μM。
  44. GC64161 Calcium glycerophosphate Calcium glycerophosphate 是肠道碱性磷酸酶 F3 的抑制剂 (intestinal alkaline phosphatase F3)。Calcium glycerophosphate是全肠外营养溶液中钙和磷的来源。
  45. GC64131 TMX-4116 TMX-4116 是酪蛋白激酶 1α (CK1α) 降解剂。TMX-4116 在 MOLT4、Jurkat 和 MM.1S 细胞中显示出对 CK1α 的降解偏好,DC50 小于 200 nM。TMX-4116 可用于多发性骨髓瘤的研究。
  46. GC64031 MP07-66 MP07-66 是一种 FTY720 类似物,没有免疫抑制作用,通过破坏 SET-PP2A 复合物导致 PP2A 重新激活,在慢性淋巴细胞白血病中显示出良好的抗肿瘤作用。
  47. GC64030 MY10 MY10 是一种有效和具有口服活性的的受体蛋白酪氨酸磷酸酶 (RPTPβ/ζ) 抑制剂。MY10 可以减弱了类似暴饮暴食的乙醇消耗和乙醇奖励。
  48. GC64005 FPFT-2216 FPFT-2216 是一种"分子胶水"化合物,可降解磷酸二酯酶 6D (PDE6D)、锌指转录因子 Ikaros (IKZF1)、Aiolos (IKZF3) 和酪蛋白激酶 1α (CK1α)。FPFT-2216 可用于癌症和炎症疾病的研究。
  49. GC63964 PR-39 TFA PR-39 TFA 是富含脯氨酸和精氨酸的天然抗菌肽,是一种非竞争性,可逆和变构的蛋白酶体 (proteasome) 抑制剂。PR-39 TFA 可逆地结合到蛋白酶体的 α7 亚基上,并通过泛素-蛋白酶体途径阻断 NF-κB 抑制剂 IκBα 的降解。PR-39 TFA 刺激小鼠的血管生成,抑制炎症反应并显着减小心肌梗死面积。
  50. GC63921 ABBV-CLS-484 ABBV-CLS-484 是一种具有亚纳摩尔活性的有效的 PTPN1 或 PTPN2 抑制剂。
  51. GC63856 Relacatib Relacatib (SB-462795) 是一种新的,有效的口服活性的人组织蛋白酶 K, L 和 V (cathepsins K, L, V) 的抑制剂,其Ki 值分别为 41, 68 和 53 pM。Relacatib 原位抑制人破骨细胞内源性组织蛋白酶 K 和人破骨细胞介导的骨吸收,IC50 值分别为 45 nM 和 70 nM。Relacatib 对体外人体组织骨吸收的抑制作用,以及对食蟹猴体内骨吸收有抑制作用。

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