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SRT1720 HCl

SRT1720 HCl是一種選擇性的SIRT1激活劑，無細胞試驗中EC50為0.16 μM，對SIRT2和SIRT3的作用弱230倍以上。SRT1720 還可誘導(dǎo)自噬。

SRT1720 HCl Chemical Structure

SRT1720 HCl Chemical Structure

CAS: 1001645-58-4

規(guī)格 價格 庫存 購買數(shù)量
10mM (1mL in DMSO) 1960.55 現(xiàn)貨
5mg 1400.82 現(xiàn)貨
50mg 7964.73 現(xiàn)貨
1g 31900 現(xiàn)貨
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常與SRT1720 HCl一起在實驗中被使用的化合物

Selisistat (EX 527)

SRT1720增加Pgrcre/+Rosa26mTmG/+小鼠的子宮內(nèi)膜異位病變，而Selisistat顯著減少子宮內(nèi)膜異位病變的數(shù)量。

Kim TH, et al.J Clin Endocrinol Metab. 2022 Feb 17;107(3):788-800.

Resveratrol

SRT1720增強依托泊苷和長春新堿誘導(dǎo)的細胞死亡，而Resveratrol則抑制ES細胞中的細胞死亡。

Sonnemann J, et al. J Cancer Res Clin Oncol. 2016 Jan;142(1):17-26.

Quercetin

Quercetin在對抗D-GalN/LPS對雄性Wistar大鼠的細胞毒性作用方面比SRT1720更有效。

Kemelo MK, et al. Eur Rev Med Pharmacol Sci. 2016;20(2):363-71.

Astragaloside IV

SRT1720 HCl和Astragaloside IV在calpain-1敲除中對血管內(nèi)皮功能障礙(VED)表現(xiàn)出相似的作用。

Zhao F, et al. Front Pharmacol. 2022 Aug 2;13:920977.

MDL-28170

SRT1720 HCl和MDL-28170治療可恢復(fù)人冠狀動脈內(nèi)皮細胞(HCAEC)中線粒體ROS水平的增加和膜電位的降低。

Zhao F, et al. Front Pharmacol. 2022 Aug 2;13:920977.

SRT1720 HCl相關(guān)產(chǎn)品

相關(guān)信號通路圖

Sirtuin Signaling Pathways

Sirtuin信號通路圖

細胞實驗數(shù)據(jù)示例

細胞系 實驗類型 給藥濃度 孵育時間 活性描述 文獻信息
MC3T3-E1 Function Assay 10 μM 60 min? attenuates the FGF-2-induced osteoprotegerin mRNA expression 25290095
MC3T3-E1 Function Assay 10 μM 60 min? suppresses the FGF-2-stimulated osteoprotegerin release 25290095
MDA-MB-231 Function Assay 5 μM 16 h induces lysosomal membrane permeabilization 25411356
MDA-MB-231 Function Assay 5 μM 8 h increases the number of acidic vesicular organelles 25411356
Neu Growth Inhibition Assay 0-20 μM 24 h reduces cell viability dose dependently 25411356
HCT116 Growth Inhibition Assay 0-20 μM 24 h reduces cell viability dose dependently 25411356
A459 Growth Inhibition Assay 0-20 μM 24 h reduces cell viability dose dependently 25411356
BT20 Growth Inhibition Assay 0-20 μM 24 h reduces cell viability dose dependently 25411356
HS578T Growth Inhibition Assay 0-20 μM 24 h reduces cell viability dose dependently 25411356
SUM149 Growth Inhibition Assay 0-20 μM 24 h reduces cell viability dose dependently 25411356
MDA-MB-231 Growth Inhibition Assay 0-20 μM 24 h reduces cell viability dose dependently 25411356
SKBR3 Growth Inhibition Assay 0-20 μM 24 h reduces cell viability dose dependently 25411356
T47D Growth Inhibition Assay 0-20 μM 24 h reduces cell viability dose dependently 25411356
MCF-7 Growth Inhibition Assay 0-20 μM 24 h reduces cell viability dose dependently 25411356
MCF10A Growth Inhibition Assay 0-20 μM 24 h reduces cell viability dose dependently 25411356
RAW264.7 Function Assay 1 μM 6 h upregulates the reduced SIRT1 protein or mRNA levels by high glucose 25793995
NRK-49F Function Assay 0–2?μM 36 h enhances STAT3 phosphorylation 26022003
NRK-49F Function Assay 0–2?μM 36 h enhances phosphorylation of EGFR and PDGFRβ? 26022003
NRK-49F Function Assay 0–2?μM 36 h increases expression of α-SMA and fibronectin dose dependently 26022003
SK-N-MC? Function Assay 3 μM 0-24 h activates caspase 3/7 26055805
SK-ES-1 Function Assay 10 μM 0-24 h activates caspase 3/7 26055805
WE-68 Function Assay 20 μM 0-24 h activates caspase 3/7 26055805
SK-N-MC? Apoptosis Assay 0-2.5 μM 24 h induces cell death in dose dependently 26055805
SK-ES-1 Apoptosis Assay 0-10 μM 24 h induces cell death in dose dependently 26055805
WE-68 Apoptosis Assay 0-24 μM 24 h induces cell death in dose dependently 26055805
MC3T3-E1 Function Assay 20 μM 1 h suppresses the TGF-β-induced phosphorylation of p44/p42 MAP kinase or SAPK/JNK 26136978
MC3T3-E1 Function Assay 10 μM? 12 h reduces the VEGF mRNA expression levels stimulated by TGF-β 26136978
MC3T3-E1 Function Assay 10 μM? 1 h reduces the TGF-β-stimulated VEGF release in dose- and time-dependent manner? 26136978
CACs? Function Assay 4?μM 30?min induces acute SIRT1 activation? 26254104
MC3T3-E1 Function Assay 10 μM 60 min? attenuates the FGF-2-induced osteoprotegerin mRNA expression 25290095
MC3T3-E1 Function Assay 10 μM 60 min? suppresses the BMP-4-stimulated VEGF release 24435444
MC3T3-E1 Function Assay 10 μM 60 min? suppresses the PGF2α-stimulated OPG release 24333336
MC3T3-E1 Function Assay 10 μM 60 min? reduces the PGF2α-stimulated phosphorylation of p44/p42 MAP kinase 24333336
MC3T3-E1 Function Assay 10 μM 60 min? attenuates the PGF2α-induced phosphorylation of both MEK1/2 and Raf-1 24333336
RPE Cell Viability Assay 5 μM 1 h attenuates OAβ-induced decrease of cell viability 24036938
9607 Cell Viability Assay 1 μM 36 h increases the cell viability compared with melatonin alone 23726949
9607 Function Assay 1 μM 36 h increases SIRT1 and decreased acetylated-p53 expression 23726949
RPMI.8226 Cell Viability Assay 7/10 μM 24 h decreases viability concentration dependently 21950728
U266 Cell Viability Assay 7/10 μM 24 h decreases viability concentration dependently 21950728
MM.1S Cell Viability Assay 7/10 μM 24 h decreases viability concentration dependently 21950728
KMS12 Cell Viability Assay 7/10 μM 24 h decreases viability concentration dependently 21950728
LR5 Cell Viability Assay 7/10 μM 24 h decreases viability concentration dependently 21950728
MM.1R Cell Viability Assay 7/10 μM 24 h decreases viability concentration dependently 21950728
Ina6 Cell Viability Assay 7/10 μM 24 h decreases viability concentration dependently 21950728
RPMI-8226 Apoptosis Assay 7/10 μM 24 h induces a significant increase in the Annexin V+/PI??apoptosis 21950728
MM.1R? Apoptosis Assay 7/10 μM 24 h induces a significant increase in the Annexin V+/PI??apoptosis 21950728
H411EC3 Function Assay 50/100 nM 6 h increases SIRT1 activity in the presence of TSA, PEPCK activity, mRNA levels of Pck1 and Pgc1α, and elevating glucose production 21212096
hepatocytes Function Assay 10 nM 6 h increases SIRT1 activity in the presence of TSA, PEPCK activity, mRNA levels of Pck1 and Pgc1α, and elevating glucose production 21212096
hepatocytes Function Assay 10 nM 6 h increases Hmgcr?and?Acc?gene expression 21212096
U2OS Function assay 0.10 uM Activation of SIRT1 in human U2OS cells assessed as decrease in p53 deacetylation level at 0.10 uM 18046409
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
DAOY qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells 29435139
BT-37 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells 29435139
MG 63 (6-TG R) qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells 29435139
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells 29435139
Rh30 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells 29435139
LAN-5 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells 29435139
Rh18 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells 29435139
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生物活性

產(chǎn)品描述 SRT1720 HCl是一種選擇性的SIRT1激活劑，無細胞試驗中EC50為0.16 μM，對SIRT2和SIRT3的作用弱230倍以上。SRT1720 還可誘導(dǎo)自噬。
靶點
SIRT1 [1]
(Cell-free assay)
0.16 μM(EC50)
體外研究(In Vitro)
體外研究活性

SRT1720抗最近的乙?；竿滴颯IRT2 (EC1.5為37 μM)和SIRT3 (EC1.5 > 300 μM)的最大激活率達781%。SRT1720在氨基末端催化區(qū)的變構(gòu)位點結(jié)合到SIRT1酶-肽底物復(fù)合物上，降低乙酰化底物的米氏常數(shù)值。用SRT1720處理一周后，飼喂的葡萄糖水平降低，處理三周后，飼喂的葡萄糖水平進一步降低，持續(xù)處理10周。SRT1720對用無糖食物喂養(yǎng)的鼠沒有作用效果，顯示出藥理學(xué)SIRT1的激活不會產(chǎn)生低血糖。用SRT1720處理4周，明顯降低高胰島素血癥，使升高的胰島素水平恢部分復(fù)正常SRT1720處理腓腸肌，通過測定檸檬酸合酶活性發(fā)現(xiàn)線粒體各項能力上升15%。[1]高濃度 SRT1720 (15 μM)誘導(dǎo)正常細胞活力輕微下降，約10-20%。SRT1720明顯抑制VEGF依賴的 MM 細胞遷移。[2]
激酶實驗 SIRT1熒光偏振實驗
在SIRT1 FP試驗中，使用從p53序列中得到的含20個氨基酸的肽段 (Ac-Glu-Glu-Lys(biotin)-Gly-Gln-Ser-Thr-Ser-Ser-His-Ser-Lys(Ac)-Nle-Ser-Thr-Glu-Gly-Lys(MR121或 Tamra)-Glu-Glu-NH2)。肽段N端與生物素相連，C端用熒光標記修飾。監(jiān)測酶活的反應(yīng)是酶活偶聯(lián)反應(yīng)，第一步反應(yīng)為SIRT1催化的脫乙酰反應(yīng)，第二步反應(yīng)為在新暴露的賴氨酸殘基處進行胰蛋白酶催化的分裂。為了突出底物和產(chǎn)物的多種區(qū)別，加入鏈酶親和素，反應(yīng)終止。FP測試的敏感性可用來鑒定SRT1720。進行熒光偏振反應(yīng)環(huán)境如下：0.5 μM 肽底物, 150 μM βNAD+, 0-10 nM SIRT1, 25 mM Tris-醋酸鹽（pH 為8）, 137 mM Na-Ac, 2.7 mM K-Ac, 1 mM Mg-Ac, 0.05% Tween-20, 0.1% Pluronic F127, 10 mM CaCl2, 5 mM DTT, 0.025% BSA, 及0.15 mM煙堿。 反應(yīng)在37oC溫育，加入煙堿終止反應(yīng)，加入胰蛋白酶分裂脫乙酰底物。加入鏈酶親和素在37oC溫育。在650 nm 和680nm 處測定熒光偏振。
細胞實驗 細胞系 人類血管內(nèi)皮細胞(HUVECs)
濃度 5 μM
孵育時間 2小時
方法

使用Transwell遷移實驗測定遷移率。通過基底膜的毛細血管樣管結(jié)構(gòu)形成試劑盒檢測體外血管生成。用于內(nèi)皮血管生成實驗，從Clonetics獲得的人類血管內(nèi)皮細胞（HUVEC），保存在含5% FBS的內(nèi)皮細胞生長培養(yǎng)基中。使用臺盼藍拒染法測定HUVEC細胞活力，觀察到用SRT1720處理的細胞死亡率小于5%。
實驗圖片 檢測方法 檢測指標 實驗圖片 PMID
Western blot

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