Sirtuin

信号通路图

研究领域

抑制剂选择性比较

特异性亚型抑制剂

Sirtuin产品

所有产品 Sirtuin抑制剂(11) Sirtuin激活剂(8) 新Sirtuin产品

产品目录	产品描述	文献引用	实验数据
S1541	Selisistat (EX 527) Selisistat (EX 527)是一种有效的，选择性SIRT1抑制剂，无细胞试验中IC50为38 nM，比作用于SIRT2和SIRT3选择性高200倍以上。Phase 2。	Blood, 2019, 133(3):266-279 Breast Cancer Res, 2019, 21(1):64 Cell Death Dis, 2019, 10(5):363	The eect of Melatonin, luzindole, and EX527 treatment on apoptotic index, infarct size, lactate dehydrogenase (LDH) release, and CK release in IR-injured hearts. Representative photomicrographs of in situ detection of apoptotic myocytes by TUNEL staining. Green ﬂuorescence shows TUNEL-positive nuclei; blue ﬂuorescence shows nuclei of total cardiomyocytes; original magniﬁcation 9x400. Sacle bar: 100 um.
S2804	Sirtinol Sirtinol是一种特异性SIRT1和SIRT2抑制剂，无细胞试验中IC50分别为131 μM和38 μM。	Mol Cell Endocrinol, 2018, 474:97-104 Biomed Pharmacother, 2018, 99:947-955 Mol Med Rep, 2018, 17(2):3212-3217	Effects of sirtinol on SIRT1 expression and HIF-1α. hMSCs were treated with sirtinol (100 uM) or equivalent concentration of DMSO (CTR) for 24 h and then exposed to 1% O2 for 6 h. All cells lysates were analyzed for SIRT1, HIF-1α, and tubulin by Western blot.
S1899	Nicotinamide (Vitamin B3) Nicotinamide (Vitamin B3) 是一种水溶性维生素，是NAD 和 NADP的活性成分，也是一种sirtuins抑制剂。	Mol Cell, 2019, 73(4):788-802 Cell Death Dis, 2019, 10(5):363 Pharmacol Res, 2019, 146:104281	Immunoprecipitation-western blot for analyzing acetylated Snail in Snail-transfected 293T cells (upper) and FaDu-Snail cells (lower) treated with a vehicle control (Ctrl), a HDAC inhibitor TSA 5 nM for 8 hr, a SIRT1 inhibitor NAM(Nicotinamide) 10 mM for 8 hr, or in combination.
S7845	SirReal2 SirReal2是一种有效的选择性Sirt2抑制剂，IC50为140 nM。	J Steroid Biochem Mol Biol, 2019, 185:27-38
S5914^New	AK 7 AK 7是具有血脑屏障渗透性的SIRT2抑制剂，IC50为15.5 μM。
S4900	Tenovin-6 Tenovin-6是p53转录活性的小分子激活剂。	Nat Biotechnol, 2015, 10.1038/nbt.3130
S7577	AGK2 AGK2是一个有效的选择性SIRT2抑制剂，IC50值为3.5 μM。对其他如SIRT1或SIRT3的抑制作用，在10倍以上的浓度时仍很微弱。	Life Sci, 2019, 230:68-75 Cell Physiol Biochem, 2018, 46(2):451-460 J Mol Cell Cardiol, 2018, 10.1016/j.yjmcc.2018.12.011	Masson trichrome staining of tubulointerstitium areas from Sham, UUO, UUO+AGK2 mice (original magnification: × 400).
S8245	Thiomyristoyl Thiomyristoyl是一种有效的、特异性SIRT2抑制剂，IC50为28 nM。它抑制SIRT1的IC50值为98 μM，而在浓度高达200 μM时，对SIRT3没有抑制作用。
S8460	Salermide Salermide是一种反向酰胺，在体外对Sirt1和Sirt2具有强的抑制作用。相对于Sirt1，Salermide对Sirt2的抑制更为有效。
S8627	OSS_128167 OSS-128167是一种特异性的SIRT6抑制剂，对SIRT6, SIRT1和SIRT2的IC50分别为89, 1578和751 μM。	J Neuroinflammation, 2019, 16(1):47
S8628	3-TYP 3-TYP是SIRT3的选择性抑制剂，相对于Sirt1和Sirt2来说，对Sirt3具有较高选择性。对SIRT1、SIRT2、SIRT3的IC50分别为88 nM、92 nM、16 nM。	Br J Haematol, 2019, 187(1):49-64 CNS Neurosci Ther, 2018, 10.1111/cns.13053 Biosci Trends, 2018, 12(6):605-612	Effects of HNK or 3‐TYP on surgery/anesthesia‐induced an increased expression of pro‐inflammatory cytokines in hippocampus. (A, E) Representative blots at postoperative 1 and 3 d, respectively. (B, F) MCP‐1 relative expression. (C, G) TNF‐α relative expression. (D, H) IL‐1β relative expression. The data are presented as the mean ±standard error of the mean for each group (n = 6 per group). *P < 0.05 vs the control group; #P < 0.05 vs the surgery+vehicle group; $P < 0.05 vs the honokiol group
S1129	SRT1720 HCl SRT1720 HCl是一种选择性的SIRT1激活剂，无细胞试验中EC50为0.16 μM，对SIRT2和SIRT3的作用弱230倍以上。	Cell Death Dis, 2019, 10(5):363 Neurobiol Aging, 2019, 80:127-137 Front Cell Neurosci, 2019, 10.3389/fncel.2018.00515	PAI-1 expression in HUVECs treated with drugs as indicated.(D) senescent HUVECs were treated with SRT1720, culturing for 24, 48 hours. PAI-1 mRNA and protein (E) levels were analyzed using real-time RT–PCR and Western blotting, respectively. The RNA and protein levels were normalized to the internal control β-actin. Data are presented as the mean±SEM of three independent experiments. P < 0.05 vs. corresponding control. P < 0.01 vs. corresponding control **P < 0.001 vs. corresponding control.
S5918^New	CAY10602 CAY10602是有效的SIRT1激活剂。
S4735	Salvianolic acid B Salvianolic acid B (Sal B)是一种抗氧化剂和自由基清除化合物，是从丹参中提取出来的最丰富的生物活性化合物。
S8270	SRT2183 SRT2183是sirtuin蛋白亚型SIRT1的小分子激活剂。
S7792	SRT2104 (GSK2245840) SRT2104 (GSK2245840)是一种选择性 SIRT1 活化剂，参与能量平衡的调节。Phase 2。	Mol Psychiatry, 2019, 10.1038/s41380-019-0352-1
S2391	Quercetin Quercetin是蔬菜水果和白酒中的天然黄酮类化合物，是一种体外重组Sirt1蛋白的激活剂同时也是PI3K抑制剂，IC50为2.4 – 5.4 μM。	Front Cell Neurosci, 2019, 13:316 NPJ Precis Oncol, 2019, 3:16 Clin Cancer Res, 2018, 10.1158/1078-0432	After starved in serum-free medium for 24h,A549 cells incubated with the indicated concentrations of Quercetin for 3h,followed by 20-minute stimolation of 100ng/ml EGF.
S2298	Fisetin Fisetin 是有效的Sirtuin活化化合物(STAC)，可以调节Sirtuin。	Alcohol Clin Exp Res, 2016, 40(10):2076-2084	Liver pathology and serum markers of liver injury in mice fed control (Ctrl), or ethanol (EtOH), or ethanol combined with fisetin (E/Fisetin) diet for 4 weeks. (A) Light microscopy with hematoxylin and eosin staining shows lipid accumulation (arrows) in the liver of mice after alcohol exposure, which was alleviated by fisetin administration. (B) Plasma alanine aminotransferase (ALT) and (C) aspartate aminotransferase (AST) activities. Infinity ALT and AST reagents were used formeasuring ALT and AST activities. Scale bar: 50 lm. Results are mean±SD (n = 3 to 6). Results for bars that do not share a letter differed significantly among groups (p < 0.05). Significant differences among groups are determined by analysis of variance followed by Tukey’s test.
S8481	SRT3025 HCl SRT3025是一种具有口服活性的SIRT1小分子激活剂。

产品目录	产品描述	文献引用	实验数据
S1541	Selisistat (EX 527) Selisistat (EX 527)是一种有效的，选择性SIRT1抑制剂，无细胞试验中IC50为38 nM，比作用于SIRT2和SIRT3选择性高200倍以上。Phase 2。	Blood,2019, 133(3):266-279 Breast Cancer Res,2019, 21(1):64 Cell Death Dis,2019, 10(5):363	The eect of Melatonin, luzindole, and EX527 treatment on apoptotic index, infarct size, lactate dehydrogenase (LDH) release, and CK release in IR-injured hearts. Representative photomicrographs of in situ detection of apoptotic myocytes by TUNEL staining. Green ﬂuorescence shows TUNEL-positive nuclei; blue ﬂuorescence shows nuclei of total cardiomyocytes; original magniﬁcation 9x400. Sacle bar: 100 um.
S2804	Sirtinol Sirtinol是一种特异性SIRT1和SIRT2抑制剂，无细胞试验中IC50分别为131 μM和38 μM。	Mol Cell Endocrinol,2018, 474:97-104 Biomed Pharmacother,2018, 99:947-955 Mol Med Rep,2018, 17(2):3212-3217	Effects of sirtinol on SIRT1 expression and HIF-1α. hMSCs were treated with sirtinol (100 uM) or equivalent concentration of DMSO (CTR) for 24 h and then exposed to 1% O2 for 6 h. All cells lysates were analyzed for SIRT1, HIF-1α, and tubulin by Western blot.
S1899	Nicotinamide (Vitamin B3) Nicotinamide (Vitamin B3) 是一种水溶性维生素，是NAD 和 NADP的活性成分，也是一种sirtuins抑制剂。	Mol Cell,2019, 73(4):788-802 Cell Death Dis,2019, 10(5):363 Pharmacol Res,2019, 146:104281	Immunoprecipitation-western blot for analyzing acetylated Snail in Snail-transfected 293T cells (upper) and FaDu-Snail cells (lower) treated with a vehicle control (Ctrl), a HDAC inhibitor TSA 5 nM for 8 hr, a SIRT1 inhibitor NAM(Nicotinamide) 10 mM for 8 hr, or in combination.
S7845	SirReal2 SirReal2是一种有效的选择性Sirt2抑制剂，IC50为140 nM。	J Steroid Biochem Mol Biol,2019, 185:27-38
S5914^New	AK 7 AK 7是具有血脑屏障渗透性的SIRT2抑制剂，IC50为15.5 μM。
S4900	Tenovin-6 Tenovin-6是p53转录活性的小分子激活剂。	Nat Biotechnol,2015, 10.1038/nbt.3130
S7577	AGK2 AGK2是一个有效的选择性SIRT2抑制剂，IC50值为3.5 μM。对其他如SIRT1或SIRT3的抑制作用，在10倍以上的浓度时仍很微弱。	Life Sci,2019, 230:68-75 Cell Physiol Biochem,2018, 46(2):451-460 J Mol Cell Cardiol,2018, 10.1016/j.yjmcc.2018.12.011	Masson trichrome staining of tubulointerstitium areas from Sham, UUO, UUO+AGK2 mice (original magnification: × 400).
S8245	Thiomyristoyl Thiomyristoyl是一种有效的、特异性SIRT2抑制剂，IC50为28 nM。它抑制SIRT1的IC50值为98 μM，而在浓度高达200 μM时，对SIRT3没有抑制作用。
S8460	Salermide Salermide是一种反向酰胺，在体外对Sirt1和Sirt2具有强的抑制作用。相对于Sirt1，Salermide对Sirt2的抑制更为有效。
S8627	OSS_128167 OSS-128167是一种特异性的SIRT6抑制剂，对SIRT6, SIRT1和SIRT2的IC50分别为89, 1578和751 μM。	J Neuroinflammation,2019, 16(1):47
S8628	3-TYP 3-TYP是SIRT3的选择性抑制剂，相对于Sirt1和Sirt2来说，对Sirt3具有较高选择性。对SIRT1、SIRT2、SIRT3的IC50分别为88 nM、92 nM、16 nM。	Br J Haematol,2019, 187(1):49-64 CNS Neurosci Ther,2018, 10.1111/cns.13053 Biosci Trends,2018, 12(6):605-612	Effects of HNK or 3‐TYP on surgery/anesthesia‐induced an increased expression of pro‐inflammatory cytokines in hippocampus. (A, E) Representative blots at postoperative 1 and 3 d, respectively. (B, F) MCP‐1 relative expression. (C, G) TNF‐α relative expression. (D, H) IL‐1β relative expression. The data are presented as the mean ±standard error of the mean for each group (n = 6 per group). *P < 0.05 vs the control group; #P < 0.05 vs the surgery+vehicle group; $P < 0.05 vs the honokiol group

产品目录	产品描述	文献引用	实验数据
S1129	SRT1720 HCl SRT1720 HCl是一种选择性的SIRT1激活剂，无细胞试验中EC50为0.16 μM，对SIRT2和SIRT3的作用弱230倍以上。	Cell Death Dis, 2019, 10(5):363 Neurobiol Aging, 2019, 80:127-137 Front Cell Neurosci, 2019, 10.3389/fncel.2018.00515	PAI-1 expression in HUVECs treated with drugs as indicated.(D) senescent HUVECs were treated with SRT1720, culturing for 24, 48 hours. PAI-1 mRNA and protein (E) levels were analyzed using real-time RT–PCR and Western blotting, respectively. The RNA and protein levels were normalized to the internal control β-actin. Data are presented as the mean±SEM of three independent experiments. P < 0.05 vs. corresponding control. P < 0.01 vs. corresponding control **P < 0.001 vs. corresponding control.
S5918^New	CAY10602 CAY10602是有效的SIRT1激活剂。
S4735	Salvianolic acid B Salvianolic acid B (Sal B)是一种抗氧化剂和自由基清除化合物，是从丹参中提取出来的最丰富的生物活性化合物。
S8270	SRT2183 SRT2183是sirtuin蛋白亚型SIRT1的小分子激活剂。
S7792	SRT2104 (GSK2245840) SRT2104 (GSK2245840)是一种选择性 SIRT1 活化剂，参与能量平衡的调节。Phase 2。	Mol Psychiatry, 2019, 10.1038/s41380-019-0352-1
S2391	Quercetin Quercetin是蔬菜水果和白酒中的天然黄酮类化合物，是一种体外重组Sirt1蛋白的激活剂同时也是PI3K抑制剂，IC50为2.4 – 5.4 μM。	Front Cell Neurosci, 2019, 13:316 NPJ Precis Oncol, 2019, 3:16 Clin Cancer Res, 2018, 10.1158/1078-0432	After starved in serum-free medium for 24h,A549 cells incubated with the indicated concentrations of Quercetin for 3h,followed by 20-minute stimolation of 100ng/ml EGF.
S2298	Fisetin Fisetin 是有效的Sirtuin活化化合物(STAC)，可以调节Sirtuin。	Alcohol Clin Exp Res, 2016, 40(10):2076-2084	Liver pathology and serum markers of liver injury in mice fed control (Ctrl), or ethanol (EtOH), or ethanol combined with fisetin (E/Fisetin) diet for 4 weeks. (A) Light microscopy with hematoxylin and eosin staining shows lipid accumulation (arrows) in the liver of mice after alcohol exposure, which was alleviated by fisetin administration. (B) Plasma alanine aminotransferase (ALT) and (C) aspartate aminotransferase (AST) activities. Infinity ALT and AST reagents were used formeasuring ALT and AST activities. Scale bar: 50 lm. Results are mean±SD (n = 3 to 6). Results for bars that do not share a letter differed significantly among groups (p < 0.05). Significant differences among groups are determined by analysis of variance followed by Tukey’s test.
S8481	SRT3025 HCl SRT3025是一种具有口服活性的SIRT1小分子激活剂。

Tags: Sirtuin activation | SIRT1 inhibition | SIRT1 activation | SIRT1 protein | SIRT1 cancer | SIRT1 activity | SIRT1 pathway | SIRT1 assay | Sirtuin protein | Sirtuin activity | SIRT activation | SIRT assay | Sirtuin cancer | Sirtuin pathway | SIRT1 phosphorylation | Sirtuin assay | SIRT2 cancer | SIRT pathway | SIRT2 protein | SIRT2 assay | SIRT1 inhibitor review