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.
Products for Sirtuin
- Cat.No. 产品名称 Information
- 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。
- 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。
- 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。
- 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。
- GC68900 CrBKA CrBKA 是 SIRT6 的弱活性荧光小分子底物。
- 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。
- 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。
- 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。
- GC65030 Sirtuin modulator 2 Sirtuin modulator 2 (Compound 132) 是一种 sirtuin 调节剂,ED50 不超过 50 μM。
- 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.
- GC64946 SRT 2183 SRT2183 is a small-molecule activator of the sirtuin subtype SIRT1, currently being developed by Sirtris Pharmaceuticals.
- GC64575 Et-29 Et-29 是一种有效的,选择性的 SIRT5 抑制剂 (Ki=40 nM)。
- 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。
- 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。
- 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。
- 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。
- 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)。
- 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.
- GC39435 Scopolin A coumarin glucoside with anti-inflammatory activity
- GC37761 Tenovin-6 Hydrochloride A small molecule activator of p53
- GC37677 SRT 1720 A selective, potent SIRT1 activator
- GC36738 Nicotinamide riboside chloride A riboside form of nicotinamide
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GC44401
Nicotinamide riboside
A riboside form of nicotinamide
- GC40900 Ganoderic Acid D An oxygenated triterpenoid
- 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.
- GC34785 Sirt2-IN-1 Sirt2-IN-1(Compound9)是一种sirtuin2(Sirt2)抑制剂,IC50为163nM。
- GC34431 MC3482 MC3482是一种特异性sirtuin5(SIRT5)抑制剂。
- GC34187 Dihydrocoumarin (Hydrocoumarin) A coumarin with enzyme inhibitory activity
- 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
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GC32745
OSS_128167
OSS_128167 is a potent selective silencing regulatory protein 6 (SIRT6) inhibitor with an IC50 of 89 μM. OSS_128167 can inhibit HBV transcription and replication, and has antiviral and anti-inflammatory effects.
- GC30922 SIRT2 Inhibitor II (AK-1) A SIRT2 inhibitor
- 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。
- 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。
- GC30251 SIRT5 inhibitor SIRT5 inhibitor 是一种有效的 Human Sirtuin 5 deacylase 抑制剂,IC50 为 0.11 μM.
- GC30204 Sirtuin modulator 1 A SIRT1 activator
- GC19013 3-TYP A SIRT3 inhibitor
- GC18228 CAY10602 A SIRT1 activator
- GC17724 Thiomyristoyl A potent and selective SIRT2 inhibitor
- GC15931 AGK7 An inactive control for AGK2
- GC14686 JFD00244 An inhibitor of SIRT2
- GC11716 SIRT1/2 Inhibitor IV Cell-permeable inhibitor of SIRT1 and SIRT2
- GC13062 JGB1741 A SIRT1 inhibitor
- GC17922 4'-bromo-Resveratrol A potent inhibitor of SIRT1 and SIRT3
- GC13942 SirReal2 A selective SIRT2 inhibitor
- GC17704 Triacetyl Resveratrol A resveratrol derivative with diverse biological activities
- 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。
- 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。
- GC14817 Salermide A sirtuin inhibitor
- GC17881 AGK 2 AGK2 is a selective SIRT2 inhibitor, with an IC50 of 3.
- GC10676 AK-7 An inhibitor of SIRT2