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Home >> Signaling Pathways >> Chromatin/Epigenetics >> Sirtuin

Sirtuin(Sirtuin蛋白)

Silent information regulator 2 (Sir2) proteins, also known as sirtuins, are a family of nicotine adenine dinucleotide (NAD) dependent protein deacetylases in organisms ranging from bacteria to humans that are characterized by the presence of a unique and highly conserved catalytic domain of approximately 260 amino acids. Sirtuins are divided into 5 classes, including Class I (subclasses Ia, Ib and Ic), Class II, Class III, Class IV (subclasses IVa and IVb) and Class U (Gram-positive bacteria specific). The catalytic domain of sirtuins is comprised of two bilobed globular domains, the large domain containing the NAD-binding pocket and the small domain binding the acetyl-lysine substrate.

  1. Cat.No. 产品名称 Information
  2. GC69950 SRT 1720 dihydrochloride SRT 1720 dihydrochloride 是选择性的和具有口服活性的 SIRT1 激活剂，EC50 为 0.10 μM，对 SIRT2 和 SIRT3 的作用较弱。
  3. GC69898 SIRT5 inhibitor 3 SIRT5 inhibitor 3 (compound 46) 是一种有效且具有竞争性的 SIRT5 抑制剂，IC50 为 5.9 μM。SIRT5 inhibitor 3 可抑制 SIRT5 去乙酰化。SIRT5 inhibitor 3 可用于癌症和神经退行性疾病的研究。
  4. GC69897 SIRT1-IN-2 SIRT1-IN-2 (compound 3h) 是一种有效且选择性的 SIRT1 （沉默信息调节因子1）抑制剂，其IC50 为 1.6 μM。
  5. GC69033 E1231 E1231 是一种具有口服有效的 Sirtuin 1 (SIRT1) (EC50=0.83 μM) 激活剂，可调节胆固醇和脂质代谢。E1231 与 SIRT1 和脱乙酰肝 X 受体-α (LXRα) 相互作用，并增加 ATP 结合盒转运蛋白 A1 (ABCA1) 的表达。E1231 还可以减少 ApoE-/- 小鼠模型中动脉粥样硬化斑块的形成。E1231 可用于胆固醇和脂质紊乱相关疾病的研究。
  6. GC68900 CrBKA CrBKA 是 SIRT6 的弱活性荧光小分子底物。
  7. GC67778 Sirtuin modulator 3 Sirtuin modulator 3 (compound 129) 是一种 N -苯基苯甲酰胺衍生物，作为 Sirtuin 调制剂。
  8. GC66026 SIRT2-IN-9 SIRT2-IN-9 (compound 12) 是 SRIT2 的选择性抑制剂，IC50 值为 1.3 μM。SIRT2-IN-9 抑制 MCF-7 乳腺癌细胞的增殖活性。SIRT2-IN-9 可用于癌症的研究。
  9. GC65581 MIND4-19 MIND4-19 是一种有效的 SIRT2 抑制剂，IC50 为 7.0 μM。MIND4-19 可用于亨廷顿氏舞蹈症 (Huntington's disease) 的研究。
  10. GC65030 Sirtuin modulator 2 Sirtuin modulator 2 (Compound 132) 是一种 sirtuin 调节剂，ED50 不超过 50 μM。
  11. GC65019 SRT 1460 SRT-1460 is a potent and selective activator of Sirtuin 1 (SIRT1) with EC1.5 of 2.9 μM. SRT-1460 reduces cell viability and growth of pancreatic cancer cells and induces apoptosis.
  12. GC64946 SRT 2183 SRT2183 is a small-molecule activator of the sirtuin subtype SIRT1, currently being developed by Sirtris Pharmaceuticals.
  13. GC64575 Et-29 Et-29 是一种有效的，选择性的 SIRT5 抑制剂 (Ki=40 nM)。
  14. GC64527 ADTL-SA1215 ADTL-SA1215 是一种调节三阴性乳腺癌自噬的特异性 SIRT3 小分子激活剂。
  15. GC64255 CHIC35 CHIC35 是 EX-527 的结构类似物，是 SIRT1 (IC50=0.124 µM) 的有效选择性抑制剂。CHIC35 对 SIRT1 的选择性远大于对 SIRT2 (IC50=2.8 µM) 和 SIRT3 (IC50>100 µM)。CHIC35 具有抗炎作用，可用于 CHARGE 综合征的研究。
  16. GC62886 Cannabisin F Cannabisin F 是一种 SIRT1 调制器。Cannabisin F 作为大麻籽木素酰胺，可用于抗炎、抗氧化研究。Cannabisin F 作为SIRT1/NF-κB 和 Nrf2 的调节因子，可能是一种潜在的神经退行性疾病的调节剂。
  17. GC62651 7-Chloro-4-(piperazin-1-yl)quinoline 7-Chloro-4-(piperazin-1-yl)quinolone 是药物化学中的重要支架。7-Chloro-4-（piperazin-1-yl）quinolone 是有效的 sirtuin 抑制剂，还抑制 5-羟色胺的摄取 (IC50 为 50 μM)。7-Chloro-4-(piperazin-1-yl)quinolone 对恶性疟原虫 D10 和 K1 菌株表现出抗疟疾活性，IC50 分别为 1.18 μM 和 0.97 μM。
  18. GC61279 SIRT-IN-3 SIRT-IN-3是一种有效的SIRT抑制剂，对SIRT1的IC50为17μM。SIRT-IN-3对SIRT1的选择性分别是SIRT-2和SIRT3的4倍和14倍(IC50forSIRT2=74μM;IC50forSIRT3=235μM)。
  19. GC60172 Gardenia yellow Crocin-I, a major member of the crocin family, has antidepressant activity and ameliorates the disruption of lipid metabolism and dysbiosis of the gut microbiota induced by chronic corticosterone in mice.
  20. GC39435 Scopolin A coumarin glucoside with anti-inflammatory activity
  21. GC37761 Tenovin-6 Hydrochloride A small molecule activator of p53
  22. GC37677 SRT 1720 A selective, potent SIRT1 activator
  23. GC36738 Nicotinamide riboside chloride A riboside form of nicotinamide
  24. GC44401 Nicotinamide riboside A riboside form of nicotinamide
  25. GC40900 Ganoderic Acid D An oxygenated triterpenoid
  26. GC34849 UBCS039 UBCS039 is the first synthetic SIRT6 activator with EC50 of 38 μM,induces a time-dependent activation of autophagy in several human tumor cell lines.
  27. GC34785 Sirt2-IN-1 Sirt2-IN-1(Compound9)是一种sirtuin2(Sirt2)抑制剂，IC50为163nM。
  28. GC34431 MC3482 MC3482是一种特异性sirtuin5(SIRT5)抑制剂。
  29. GC34187 Dihydrocoumarin (Hydrocoumarin) A coumarin with enzyme inhibitory activity
  30. GC33418 PROTAC Sirt2 Degrader-1 PROTACSirt2Degrader-1是一种基于SirReal的PROTAC，为Sirt2的降解剂，由一个高效、同种型选择性的Sirt2抑制剂，一个连接物和thalidomide(E3泛素化连接酶的配体)组成。PROTACSirt2Degrader-1对Sirt2的IC50值为0.25μM，而对Sirt1/Sirt3(IC50>100μM)无作用
  31. GC32745 OSS_128167 A SIRT6 inhibitor
  32. GC30922 SIRT2 Inhibitor II (AK-1) A SIRT2 inhibitor
  33. GC30733 SIRT-IN-1 SIRT-IN-1是SIRT1/2/3的有效抑制剂，其IC50值分别为15，10，33μM。
  34. GC30693 SIRT-IN-2 SIRT-IN-2是SIRT1/2/3的有效抑制剂，其IC50值分别为4，1，7nM。
  35. GC30251 SIRT5 inhibitor SIRT5 inhibitor 是一种有效的 Human Sirtuin 5 deacylase 抑制剂，IC50 为 0.11 μM.
  36. GC30204 Sirtuin modulator 1 A SIRT1 activator
  37. GC19013 3-TYP A SIRT3 inhibitor
  38. GC18228 CAY10602 A SIRT1 activator
  39. GC17724 Thiomyristoyl A potent and selective SIRT2 inhibitor
  40. GC15931 AGK7 An inactive control for AGK2
  41. GC14686 JFD00244 An inhibitor of SIRT2
  42. GC11716 SIRT1/2 Inhibitor IV Cell-permeable inhibitor of SIRT1 and SIRT2
  43. GC13062 JGB1741 A SIRT1 inhibitor
  44. GC17922 4'-bromo-Resveratrol A potent inhibitor of SIRT1 and SIRT3
  45. GC13942 SirReal2 A selective SIRT2 inhibitor
  46. GC17704 Triacetyl Resveratrol A resveratrol derivative with diverse biological activities
  47. GC17126 EX-527 R-enantiomer EX-527 R-对映异构体 ((R)-EX-527) 是 Selisstat 的 R-对映异构体。 Selisistat (EX-527) 是一种有效的选择性 SIRT1 抑制剂，IC50 为 98 nM。
  48. GC13417 EX-527 S-enantiomer EX-527 S-对映异构体 ((S)-EX-527) 是一种有效的选择性 SIRT1 抑制剂，IC50 为 98 nM。
  49. GC14817 Salermide A sirtuin inhibitor
  50. GC17881 AGK 2 AGK2 is a selective SIRT2 inhibitor, with an IC50 of 3.
  51. GC10676 AK-7 An inhibitor of SIRT2

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