- 抑制劑
- 化合物庫
- 抗體
- 生物試劑
- qPCR
- 2x SYBR Green qPCR Master Mix
- 2x SYBR Green qPCR Master Mix(Low ROX)
- 2x SYBR Green qPCR Master Mix(High ROX)
- 蛋白實驗
- Protein A/G免疫沉淀磁珠
- Anti-DYKDDDDK Tag免疫磁珠
- Anti-DYKDDDDK Tag親和凝膠
- Anti-Myc免疫磁珠
- Anti-HA免疫磁珠
- 磁力架
- Poly DYKDDDDK Tag多肽
- 細胞核與細胞漿蛋白抽提試劑盒
- 免疫磁珠
- 蛋白酶抑制劑Cocktail
- 蛋白酶抑制劑Cocktail(DMSO儲液)
- 磷酸酶抑制劑Cocktail
- 新產(chǎn)品
- 聯(lián)系我們
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
CAS: 1001645-58-4
產(chǎn)品質(zhì)控
批次：
純度：
99.61%
99.61
常與SRT1720 HCl一起在實驗中被使用的化合物
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。
SRT1720 HCl相關(guān)產(chǎn)品
| 相關(guān)靶點 | SIRT1 SIRT2 SIRT3 SIRT6 SIRT5 | 點擊展開 |
|---|---|---|
| 相關(guān)產(chǎn)品 | Selisistat (EX 527) Sirtinol Quercetin Fisetin 3-TYP AGK2 OSS_128167 SRT2104 (GSK2245840) SirReal2 Thiomyristoyl Salvianolic acid B SRT2183 UBCS039 Salermide SRT3025 HCl AK 7 Inauhzin NRD167 CAY10602 | 點擊展開 |
| 相關(guān)化合物庫 | 激酶抑制劑庫 FDA藥物庫 天然產(chǎn)物庫 已知活性藥物庫-I 高選擇性抑制劑庫 | 點擊展開 |
相關(guān)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(PMID) |
|---|---|---|---|---|---|
| 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 | ||
| 點擊查看更多細胞系數(shù)據(jù) | |||||
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 |
|
| 體外研究(In Vitro) | ||||||
| 體外研究活性 | SRT1720抗最近的乙酰化酶同系物SIRT2 (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 |
| |||||