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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. 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。
  3. 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。
  4. GC64535 (S,S)-TAPI-1 A TACE inhibitor
  5. 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。
  6. GC64507 ML198 ML198 is a novel activator of glucocerebrosidase (GCase) with an IC50 of 0.4 μM and does not inhibit the enzyme's action, but can facilitate its translocation to the lysosome.
  7. 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。
  8. 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。
  9. GC64376 GDC-1971 GDC-1971 (compound 199) is a SHP2 inhibitor.
  10. 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。
  11. 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。
  12. 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。
  13. 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。
  14. 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。
  15. 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。
  16. GC64031 MP07-66 MP07-66, a FTY720 analogue, is devoid of immunosuppressive effects and shows promising antitumor effects in chronic lymphocytic leukemia by disruption of the SET-PP2A complex leading to PP2A reactivation.
  17. 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。
  18. 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。
  19. 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。
  20. GC63921 ABBV-CLS-484 ABBV-CLS-484 is a potent PTPN1 or PTPN2 inhibitor with a sub-nanomolar activity.
  21. 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。
  22. GC63788 BN82002 hydrochloride BN82002 hydrochloride 是 CDC25 phosphatase 家族的有效,选择性和不可逆的泛抑制剂。 BN82002 hydrochloride抑制 CDC25A,CDC25B2,CDC25B3,CDC25C CDC25A 和 25C-cat 的 IC50 值分别为 2.4、3.9、6.3、5.4 和 4.6 µM。 BN82002 hydrochloride 显示出比 CD45 酪氨酸磷酸酶高约 20 倍的选择性。
  23. GC63705 PTP1B-IN-3 diammonium PTP1B-IN-3 diammonium 是有效的,有选择性的 PTP1B 抑制剂,对 PTP1B 和 TCPTP 的 IC50 值均为 120 nM。PTP1B-IN-3 diammonium 具有抗糖尿病和抗癌作用。
  24. GC63661 Aderbasib Aderbasb (INCB007839) 是一种有效的、具有口服活性的、靶向特异性的低纳摩尔 ADAM10 和 ADAM17 抑制剂。Aderbasb 表现出强大的抗肿瘤活性,可用于癌症研究,包括弥漫性大 B 细胞非霍奇金淋巴瘤,HER2+ 乳腺癌,胶质瘤等。
  25. GC63621 Doxycycline Doxycycline(多西环素DOX)是一种四环素衍生物的广谱抗生素,通过干扰细菌核糖体30S亚基A位点上活化的氨基酰基tRNA的结合来抑制蛋白质合成。
  26. GC63487 RMC-4630 RMC-4630 (SHP2-IN-7) 是 一种 SHP2 抑制剂,来自专利 WO2018013597。
  27. GC63463 Casein Kinase inhibitor A86 Casein Kinase inhibitor A86 是一种有效且具有口服活性的酪蛋白激酶 1α (CK1α) 抑制剂。Casein Kinase inhibitor A86 还抑制 CDK7 (TFIIH) 和 CDK9 (P-TEFb)。Casein Kinase inhibitor A86 可诱导白血病细胞凋亡 (apoptosis),并具有有效的抗白血病活性。
  28. GC63451 Hex

    Hex 是烯醇酶 (enolase) 的抑制剂,其对 ENO2 和 ENO1 的 Ki 值分别为 74.4 nM 和 269.4 nM。

  29. GC63442 N-Caffeoyl O-methyltyramine N-Caffeoyl O-methyltyramine is a class of alkaloid isolated from Cuscuta reflexa with strong inhibitory activity against α-glucosidase with IC50 of 103.58 μM.
  30. GC63327 Fenvalerate-d5 Fenvalerate-d5 是 Fenvalerate 的氘代物。Fenvalerate 是一种有效的蛋白磷酸酶 2B (钙调神经磷酸酶;calcineurin) 抑制剂,对 PP2B-Aα 的IC50 为 2-4 nM。Fenvalerate 是拟除虫菊酯杀虫剂和杀螨剂。
  31. GC63322 MMP13-IN-3 An inhibitor of MMP-13
  32. GC63190 SHP389 SHP389 是 SHP2 的变构抑制剂,其对 SHP2 和 p-ERK 的 IC50 值均为 36 nM。
  33. GC63132 Otaplimastat Otaplimastat (SP-8203) 是一种基质金属蛋白酶 (MMP) 抑制剂,以竞争方式阻断 NMDA 受体介导的兴奋性毒性。Otaplimastat 还具有抗氧化活性。Otaplimastat 可用于脑缺血损伤的研究。
  34. GC63099 NCGC00092410 NCGC00092410 是一种有效,选择性和非糖性葡萄糖脑苷脂酶 (glucocerebrosidase, GC) 抑制剂,IC50 值为 31 nM。NCGC00092410 对相关水解酶没有活性。NCGC00092410 是一种 GC 分子伴侣,可提高突变型细胞株中葡萄糖脑苷脂酶的活性和溶酶体定位。NCGC00092410可用于戈谢病的研究。
  35. GC62984 Ganoderic acid Y Ganoderic acid Y 是一种 α-葡萄糖苷酶 (α-glucosidase) 抑制剂,对酵母 α-葡萄糖苷酶的 IC50 为170 μM。Ganoderic acid Y 通过阻止肠道病毒 71 (EV71) 的脱膜而抑制其复制。
  36. GC62948 Edaravone D5 Edaravone D5 是 Edaravone 的氘代标记物。Edaravone 是一种有效的自由基清除剂,能够抑制大鼠与 MMP-9 有关的脑出血。
  37. GC62943 DPM-1001 trihydrochloride DPM-1001 trihydrochloride 是一种有效的,特异性的,具有口服活性的,且非竞争性的蛋白酪氨酸磷酸酶 (PTP1B) 抑制剂,其 IC50 为 100 nM。DPM-1001 trihydrochloride 是特异性 PTP1B 抑制剂 MSI-1436 (IC50=600 nM) 的类似物。DPM-1001 trihydrochloride 具有抗糖尿病特性。
  38. GC62909 CPT-157633 CPT-157633 是一种二氟膦酰基甲基苯丙氨酸衍生物,是 PTP1B 抑制剂。 CPT-157633 可防止酗酒引起的葡萄糖耐受不良。
  39. GC62892 CDC25B-IN-2 BIA (TMBIM6 antagonist BIA), a potential TMBIM6 antagonist, is an inhibitor of the interaction between TMBIM6 (Transmembrane B cell lymphoma 2-associated X protein (BAX) inhibitor motif-containing 6) and mTORC2, which ultimately blocks AKT activation and cancer progression.
  40. GC62889 Cathepsin D and E FRET Substrate acetate Cathepsin D and E FRET Substrate acetate 为 cathepins D 和 E 的荧光底物 (fluorogenic substrate),而不是 B、H 或 I 的荧光底物,它的裂解发生在 Phe-Phe 酰胺键处。Cathepsin D and E FRET Substrate 是用于组织蛋白酶 D 和组织蛋白酶 E 的常规检测和机制研究的有用工具。(激发波长:328 nm; 发射波长:393 nm)
  41. GC62880 BTX161 BTX161 一种 Thalidomide 类似物,是一种有效的 CKIα 降解剂。BTX161 比 Lenalidomide更好地介导人类 AML 细胞中 CKIα 的降解,并激活 DNA损伤反应 (DDR) 和 p53,同时稳定 p53 拮抗剂 MDM2。
  42. GC62864 Benzolamide Benzolamide (CL11366) 是一种有效的碳酸酐酶 (CA) 抑制剂,抑制hCA I,hCA II,EcoCAγ 和 VchCAγ 的 Ki 值分别为15 nM,9 nM,94 nM 和 78 nM。Benzolamide 还抑制 CAS3,Ki 值为 54 nM。Benzolamide 可用于青光眼和癫痫的研究。
  43. GC62735 (E/Z)-GO289 (E/Z)-GO289 potently and selectively inhibits casein kinase 2 (CK2) at an IC50 of 7 nM in vitro kinase assay.
  44. GC49337 4-Acetamidobenzenesulfonamide A metabolite of asulam and sulfanilamide
  45. GC49211 O-desmethyl Brinzolamide (hydrochloride) An active metabolite of brinzolamide
  46. GC49210 N-desethyl Brinzolamide (oxalate) An active metabolite of brinzolamide
  47. GC49195 Indapamide-13C-d3 An internal standard for the quantification of indapamide
  48. GC49194 Metolazone-d7 An internal standard for the quantification of metolazone
  49. GC62687 Razuprotafib

    Razuprotafib (AKB-9778) 是 VE-PTP (HPTPß) 催化活性的有效选择性抑制剂 (IC50=17 pM),促进 TIE2 活化,增强 ANG1 诱导的 TIE2 活化,并刺激 TIE2 通路中信号分子的磷酸化,包括 AKT、eNOS 和 ERK。Razuprotafib 抑制结构相关磷酸酶 PTP1B,IC50 为 780 nM。除 HPTPΗ (IC50=36 pM) 和 HPTPγ (100 pM) 外,Razuprotafib 对 VE-PTP 具有良好的选择性。

  50. GC62677 Icerguastat Sephin-1 (NSC-65390) is a selective inhibitor of a holophosphatase, a small molecule that safely and selectively inhibits a regulatory subunit of protein phosphatase 1 in vivo. Sephin-1 (NSC-65390) selectively bounds and inhibits the stress-induced PPP1R15A.
  51. GC62634 GSK-2793660 GSK-2793660(游离碱)是一种口服的、不可逆的组织蛋白酶 C (CTSC) 抑制剂。

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