Sirtuin
信号通路图
研究领域
抑制剂选择性比较
Sirtuin产品
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S1541 |
Selisistat (EX 527)Selisistat (EX 527, SEN0014196) 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。 |
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.
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| S1396 |
Resveratrol (SRT501)Resveratrol (SRT501, trans-Resveratrol)具有广泛靶点，包括环氧酶（如COX, IC50=1.1 μM）、脂肪氧合酶(LOC, IC50=2.7 μM)、sirtuins和其他蛋白质。它是一种天然的植物抗毒素，具有抗癌，抗炎，降血糖和其他有益心血管的作用。Resveratrol可诱导线粒体自噬、细胞自噬和自噬依赖性的凋亡。 |
Cellular senescence and SIRT1 phosphorylation was monitored in PAECs (P2) incubated in DMEM containing HDL (50 mg/L), LDL (50 mg/L), or resveratrol (100 μM) for 24 hours. |
|
| S2804 |
SirtinolSirtinol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。 |
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.
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| S1899 |
Nicotinamide (NSC 13128)Nicotinamide (NSC 13128, Niacinamide, Vitamin PP, Nicotinic acid amide, Vitamin B3, NSC 27452)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。 |
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. |
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| E1150New |
SIRT7 inhibitor 97491在SIRT7相关的癌症中，SIRT7 inhibitor 97491以剂量依赖性的方式降低SIRT7的去乙酰化酶活性，通过p53修饰以及对caspase通路影响，激活凋亡。 |
||
| S9903New |
NRD167NRD167 是一种有效的选择性 SIRT5 抑制剂。 |
||
| S8000 |
Tenovin-1Tenovin-1 可防止MDM2介导的p53的降解，涉及泛素化途径，并通过导致SirT1和SirT2蛋白脱乙酰基活性的降低而发挥作用。Tenovin-1 也是 dihydroorotate dehydrogenase (DHODH) 的抑制剂。 |
The SIRT1 inhibitor (tenovin-1) partially blocked the protective effect of γ-man in L02 cells. The effect of tenovin-1 on expression and acetylation level of PGC-1α (B) in L02 cells treated with or without γ-man.
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| S7845 |
SirReal2SirReal2是一种有效的选择性Sirt2抑制剂，IC50为140 nM。 |
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| S4900 |
Tenovin-6Tenovin-6 是p53转录活性的小分子激活剂并可抑制 dihydroorotate dehydrogenase (DHODH)。Tenovin-6 也是 SirT1 和 SirT2 的抑制剂。 |
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| S2176 |
Tenovin-3Tenovin-3 是一种 SIRT2 的抑制剂。Tenovin-3 能够增加MCF-7细胞中的 p53 的水平。 |
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| S7577 |
AGK2AGK2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。 |
Masson trichrome staining of tubulointerstitium areas from Sham, UUO, UUO+AGK2 mice (original magnification: × 400).
|
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| S8245 |
ThiomyristoylThiomyristoyl (TM)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 |
SalermideSalermide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_128167OSS_128167 (SIRT6-IN-1)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。OSS_128167 在HBV的转录和复制中起到抗病毒的作用。 |
||
| S5914 |
AK 7AK 7是具有血脑屏障渗透性的SIRT2抑制剂，IC50为15.5 μM。 |
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| S8628 |
3-TYP3-TYP (3-(1H-1,2,3-triazol-4-yl) pyridine) 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。 |
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
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| S6744 |
InauhzinInauhzin是具有细胞透性的SIRT1抑制剂，IC50为0.7-2 μM，可通过抑制SIRT1脱乙酰活性重新激活p53。 |
||
| S1129 |
SRT1720 HClSRT1720 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。SRT1720 还可诱导自噬。 |
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.
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| S3262 |
ScopolinScopolin 是一种从 Arabidopsis thaliana (Arabidopsis) 中分离的香豆素，它通过激活 SIRT1 介导的信号级联反应来减轻肝脏脂肪变性，SIRT1介导的信号通路是脂质稳态的有效调节剂。 |
||
| S2935 |
Nicotinamide Riboside ChlorideNicotinamide Riboside Chloride是烟酰胺核糖(NR)的氯化物盐形式。NR是维生素B3的衍生物，可作为作为NAD或NAD+的前体。 |
||
| S4735 |
Salvianolic acid BSalvianolic acid B (Sal B, Lithospermate B, Lithospermic acid 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。 |
||
| S3168 |
cis-Resveratrolcis-Resveratrol (cis-RESV, cRes, (Z)-Resveratrol) 是Resveratrol的顺式异构体。Resveratrol 是一种天然的酚类化合物，具有抗氧化、抗炎、保护心脏和抗癌的特性。Resveratrol 是 pregnane X receptor (PXR) 的抑制剂，也是 Nrf2 和 SIRT1 的激活剂，并可能诱导凋亡。Resveratrol 还可抑制多种靶标，包括 5-lipoxygenase (LOX)、cyclooxygenase (COX)、IKKβ、DNA polymerases α和δ，IC50分别为2.7 μM、<1 μM、1 μM、3.3 μM和5 μM。 |
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| S8270 |
SRT2183SRT2183是sirtuin蛋白亚型SIRT1的小分子激活剂。 |
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| S8909 |
UBCS039UBCS039是第一个合成的SIRT6激活剂，EC50为38 μM，在多种人类肿瘤细胞系中均可诱导自噬的时间依赖性激活。 |
||
| 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。 |
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| S2391 |
Quercetin (NSC 9221)Quercetin (NSC 9221, Sophoretin, C.I. 75720)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。Quercetin 可诱导凋亡和保护性的自噬。Phase 4。 |
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 |
FisetinFisetin 是有效的Sirtuin活化化合物(STAC)，可以调节Sirtuin。 |
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 sharea letter differed significantly among groups (p < 0.05). Significant differences among groups are determined by analysis of variance followed by Tukey’s test.
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| S5918 |
CAY10602CAY10602是有效的SIRT1激活剂。 |
||
| S8481 |
SRT3025 HClSRT3025是一种具有口服活性的SIRT1小分子激活剂。 |
||
| S6880 |
SRT-1460SRT-1460 是一种有效的 Sirtuin 1 (SIRT1) 的选择性激活剂，其EC1.5值为2.9 μM。SRT-1460 可降低胰腺癌细胞的细胞活性、减少增殖并诱导凋亡。 |
||
| S2347 |
Quercetin DihydrateQuercetin (Sophoretin) 是一种多酚类黄酮，存在于多种植物性食品中，例如苹果，洋葱，浆果和红酒，由于其神经系统和抗癌作用而被用于许多不同的文化中。Quercetin (Sophoretin) 作为天然类黄酮，是重组SIRT1和PI3K抑制剂的刺激物，对PI3Kγ，PI3Kδ和PI3Kβ的IC50分别为2.4μM，3.0μM和5.4μM。 |
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. |
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S1541 |
Selisistat (EX 527)Selisistat (EX 527, SEN0014196) 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。 |
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.
|
|
| S1396 |
Resveratrol (SRT501)Resveratrol (SRT501, trans-Resveratrol)具有广泛靶点，包括环氧酶（如COX, IC50=1.1 μM）、脂肪氧合酶(LOC, IC50=2.7 μM)、sirtuins和其他蛋白质。它是一种天然的植物抗毒素，具有抗癌，抗炎，降血糖和其他有益心血管的作用。Resveratrol可诱导线粒体自噬、细胞自噬和自噬依赖性的凋亡。 |
Cellular senescence and SIRT1 phosphorylation was monitored in PAECs (P2) incubated in DMEM containing HDL (50 mg/L), LDL (50 mg/L), or resveratrol (100 μM) for 24 hours. |
|
| S2804 |
SirtinolSirtinol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。 |
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 (NSC 13128)Nicotinamide (NSC 13128, Niacinamide, Vitamin PP, Nicotinic acid amide, Vitamin B3, NSC 27452)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。 |
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. |
|
| E1150New |
SIRT7 inhibitor 97491在SIRT7相关的癌症中，SIRT7 inhibitor 97491以剂量依赖性的方式降低SIRT7的去乙酰化酶活性，通过p53修饰以及对caspase通路影响，激活凋亡。 |
||
| S9903New |
NRD167NRD167 是一种有效的选择性 SIRT5 抑制剂。 |
||
| S8000 |
Tenovin-1Tenovin-1 可防止MDM2介导的p53的降解，涉及泛素化途径，并通过导致SirT1和SirT2蛋白脱乙酰基活性的降低而发挥作用。Tenovin-1 也是 dihydroorotate dehydrogenase (DHODH) 的抑制剂。 |
The SIRT1 inhibitor (tenovin-1) partially blocked the protective effect of γ-man in L02 cells. The effect of tenovin-1 on expression and acetylation level of PGC-1α (B) in L02 cells treated with or without γ-man.
|
|
| S7845 |
SirReal2SirReal2是一种有效的选择性Sirt2抑制剂，IC50为140 nM。 |
||
| S4900 |
Tenovin-6Tenovin-6 是p53转录活性的小分子激活剂并可抑制 dihydroorotate dehydrogenase (DHODH)。Tenovin-6 也是 SirT1 和 SirT2 的抑制剂。 |
||
| S2176 |
Tenovin-3Tenovin-3 是一种 SIRT2 的抑制剂。Tenovin-3 能够增加MCF-7细胞中的 p53 的水平。 |
||
| S7577 |
AGK2AGK2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。 |
Masson trichrome staining of tubulointerstitium areas from Sham, UUO, UUO+AGK2 mice (original magnification: × 400).
|
|
| S8245 |
ThiomyristoylThiomyristoyl (TM)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 |
SalermideSalermide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_128167OSS_128167 (SIRT6-IN-1)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。OSS_128167 在HBV的转录和复制中起到抗病毒的作用。 |
||
| S5914 |
AK 7AK 7是具有血脑屏障渗透性的SIRT2抑制剂，IC50为15.5 μM。 |
||
| S8628 |
3-TYP3-TYP (3-(1H-1,2,3-triazol-4-yl) pyridine) 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。 |
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
|
|
| S6744 |
InauhzinInauhzin是具有细胞透性的SIRT1抑制剂，IC50为0.7-2 μM，可通过抑制SIRT1脱乙酰活性重新激活p53。 |
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S1129 |
SRT1720 HClSRT1720 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。SRT1720 还可诱导自噬。 |
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.
|
|
| S3262 |
ScopolinScopolin 是一种从 Arabidopsis thaliana (Arabidopsis) 中分离的香豆素，它通过激活 SIRT1 介导的信号级联反应来减轻肝脏脂肪变性，SIRT1介导的信号通路是脂质稳态的有效调节剂。 |
||
| S2935 |
Nicotinamide Riboside ChlorideNicotinamide Riboside Chloride是烟酰胺核糖(NR)的氯化物盐形式。NR是维生素B3的衍生物，可作为作为NAD或NAD+的前体。 |
||
| S4735 |
Salvianolic acid BSalvianolic acid B (Sal B, Lithospermate B, Lithospermic acid 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。 |
||
| S3168 |
cis-Resveratrolcis-Resveratrol (cis-RESV, cRes, (Z)-Resveratrol) 是Resveratrol的顺式异构体。Resveratrol 是一种天然的酚类化合物，具有抗氧化、抗炎、保护心脏和抗癌的特性。Resveratrol 是 pregnane X receptor (PXR) 的抑制剂，也是 Nrf2 和 SIRT1 的激活剂，并可能诱导凋亡。Resveratrol 还可抑制多种靶标，包括 5-lipoxygenase (LOX)、cyclooxygenase (COX)、IKKβ、DNA polymerases α和δ，IC50分别为2.7 μM、<1 μM、1 μM、3.3 μM和5 μM。 |
||
| S8270 |
SRT2183SRT2183是sirtuin蛋白亚型SIRT1的小分子激活剂。 |
||
| S8909 |
UBCS039UBCS039是第一个合成的SIRT6激活剂，EC50为38 μM，在多种人类肿瘤细胞系中均可诱导自噬的时间依赖性激活。 |
||
| 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。 |
||
| S2391 |
Quercetin (NSC 9221)Quercetin (NSC 9221, Sophoretin, C.I. 75720)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。Quercetin 可诱导凋亡和保护性的自噬。Phase 4。 |
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 |
FisetinFisetin 是有效的Sirtuin活化化合物(STAC)，可以调节Sirtuin。 |
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 sharea letter differed significantly among groups (p < 0.05). Significant differences among groups are determined by analysis of variance followed by Tukey’s test.
|
|
| S5918 |
CAY10602CAY10602是有效的SIRT1激活剂。 |
||
| S8481 |
SRT3025 HClSRT3025是一种具有口服活性的SIRT1小分子激活剂。 |
||
| S6880 |
SRT-1460SRT-1460 是一种有效的 Sirtuin 1 (SIRT1) 的选择性激活剂，其EC1.5值为2.9 μM。SRT-1460 可降低胰腺癌细胞的细胞活性、减少增殖并诱导凋亡。 |
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S2347 |
Quercetin DihydrateQuercetin (Sophoretin) 是一种多酚类黄酮，存在于多种植物性食品中，例如苹果，洋葱，浆果和红酒，由于其神经系统和抗癌作用而被用于许多不同的文化中。Quercetin (Sophoretin) 作为天然类黄酮，是重组SIRT1和PI3K抑制剂的刺激物，对PI3Kγ，PI3Kδ和PI3Kβ的IC50分别为2.4μM，3.0μM和5.4μM。 |
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. |
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