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
| 目录号 | 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。 |
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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| 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 (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。 |
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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| S7845 |
SirReal2SirReal2是一种有效的选择性Sirt2抑制剂，IC50为140 nM。 |
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| S6744New |
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。 |
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| S4900 |
Tenovin-6Tenovin-6是p53转录活性的小分子激活剂。 |
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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。 |
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| 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。 |
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| S8627 |
OSS_128167OSS-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。 |
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| 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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| 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。 |
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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| S8909New |
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。 |
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| S4735 |
Salvianolic acid BSalvianolic 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。 |
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| S8270 |
SRT2183SRT2183是sirtuin蛋白亚型SIRT1的小分子激活剂。 |
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| 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 |
QuercetinQuercetin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。 |
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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| 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 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.
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| S5918 |
CAY10602CAY10602是有效的SIRT1激活剂。 |
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| S8481 |
SRT3025 HClSRT3025是一种具有口服活性的SIRT1小分子激活剂。 |
| 目录号 | 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。 |
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 |
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 (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。 |
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 |
SirReal2SirReal2是一种有效的选择性Sirt2抑制剂，IC50为140 nM。 |
||
| S6744New |
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。 |
||
| S4900 |
Tenovin-6Tenovin-6是p53转录活性的小分子激活剂。 |
||
| 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。 |
||
| 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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| 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。 |
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.
|
|
| S8909New |
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。 |
||
| S4735 |
Salvianolic acid BSalvianolic 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 |
SRT2183SRT2183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。 |
||
| S2391 |
QuercetinQuercetin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。 |
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 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.
|
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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。 |
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