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SF1670 Sale

目录号 : GC10019

SF1670是一种有效的特异性PTEN(第10号染色体上缺失的磷酸酶和张力蛋白同源物)抑制剂。

SF1670 Chemical Structure

Cas No.:345630-40-2

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥431.00
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10mg
¥672.00
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50mg
¥2,741.00
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Sample solution is provided at 25 µL, 10mM.

Description

SF1670 is a potent and specific PTEN (phosphatase and tensin homolog deleted on chromosome 10) inhibitor[1]. SF1670 protects cells from oxygen-glucose deprivation-induced cell death[2]. SF1670 helps maintain the pluripotency of mouse embryonic stem cells (ESCs)[3].

In vitro, treatment of nucleus pulposus (NP) cells with SF1670 (0-5µM) for 3h significantly increased cell viability, inhibited PTEN expression, and activated Akt activity[4]. Pretreatment of neutrophils with SF1670 (125-500nM) for 30min dose-dependently enhanced fMLP-induced neutrophil polarization[5]. Treatment of MCF-7 cells with SF1670 (200nM) for 48h significantly inhibited curcumin-induced cell apoptosis and significantly upregulated p-AKT protein expression[6].

In vivo, SF1670 (3mg/kg) was intraperitoneally injected into mice with cerebral ischemia-reperfusion (I/R) injury, which attenuated the increase in thiobarbituric acid reactive substances (TBARS) induced by I/R and reversed the decrease in GSH levels and SOD activity[7].

References:
[1] Li F Q, Chen W B, Luo Z W, et al. Bone marrow mesenchymal stem cell-derived exosomal microRNAs target PI3K/Akt signaling pathway to promote the activation of fibroblasts[J]. World Journal of Stem Cells, 2023, 15(4): 248.
[2] Farajdokht F, Mohaddes G, Karimi-Sales E, et al. Inhibition of PTEN protects PC12 cells against oxygen-glucose deprivation induced cell death through mitoprotection[J]. Brain research, 2018, 1692: 100-109.
[3] Wang W, Lu G, Su X, et al. Pten-mediated Gsk3β modulates the naïve pluripotency maintenance in embryonic stem cells[J]. Cell Death & Disease, 2020, 11(2): 107.
[4] Fu H Y, Shen L, Gao X S, et al. SF1670 inhibits apoptosis and inflammation via the PTEN/Akt pathway and thus protects intervertebral disc degeneration[J]. European Review for Medical & Pharmacological Sciences, 2020, 24(17).
[5] Li Y, Prasad A, Jia Y, et al. Pretreatment with phosphatase and tensin homolog deleted on chromosome 10 (PTEN) inhibitor SF1670 augments the efficacy of granulocyte transfusion in a clinically relevant mouse model[J]. Blood, The Journal of the American Society of Hematology, 2011, 117(24): 6702-6713.
[6] Li M Z, Wang C R, Lin C L. Curcumin promotes apoptosis of breast cancer cells by down-regulating DJ-1-PTEN/PI3K/AKT signaling pathways[J]. Int. J. Clin. Exp. Med, 2019, 12: 8992-8998.
[7] Grewal A K, Singh N, Singh T G. Neuroprotective effect of pharmacological postconditioning on cerebral ischaemia–reperfusion-induced injury in mice[J]. Journal of Pharmacy and Pharmacology, 2019, 71(6): 956-970.

SF1670是一种有效的特异性PTEN(第10号染色体上缺失的磷酸酶和张力蛋白同源物)抑制剂[1]。SF1670能够保护细胞免受氧-葡萄糖剥夺诱导的细胞死亡[2]。SF1670有助于维持小鼠胚胎干细胞(ESC)的多能性[3]

在体外,SF1670(0-5µM)处理髓核(NP)细胞3h,显著提高了细胞活力,抑制了PTEN的表达,激活了Akt活性[4]。SF1670(125-500nM)预处理中性粒细胞30min,剂量依赖性地增强了fMLP诱导的中性粒细胞极化[5]。SF1670(200nM)处理MCF-7细胞48h,显著抑制了姜黄素引起的细胞凋亡,显著上调了p-AKT蛋白表达[6]

在体内,SF1670(3mg/kg)通过腹腔注射治疗脑缺血再灌注(I/R)损伤小鼠,减弱了I/R引起的硫代巴比妥酸反应物质(TBARS)的增加,逆转了GSH水平和SOD活性的下降[7]

实验参考方法

Cell experiment [1]:

Cell lines

Nucleus pulposus (NP) cells

Preparation Method

NP cells were treated with 0, 0.5, 1, 2, and 5μM SF1670 for 3h, and then cell viability was measured using the CCK-8 assay.

Reaction Conditions

0, 0.5, 1, 2, and 5µM; 3h

Applications

SF1670 treatment can improve the viability of NP cells, and the cell viability reached the highest level when treated with 2μM concentration.

Animal experiment [2]:

Animal models

Swiss albino male mice

Preparation Method

Six male mice in each group were randomly selected and divided into nine groups. All the animals were subjected to behavioral tests and biochemical estimations during the study. Group I was a sham surgery group, and group II was I/R control group. For the reperfusion intervention (i.e. pPoCo), pharmacological agents CGS21680 (0.5mg/kg; i.p.) (in group V, VI, IX) and SF1670 (3mg/kg; i.p.) (in group VII, VIII, IX) were administered 5min before reper fusion of 24h so that the drug would be in circulation at the time of onset of reperfusion.

Dosage form

3mg/kg; i. p.

Applications

SF1670 treatment attenuated the I/R-induced increase in thiobarbituric acid reactive substances (TBARS), and reversed the decrease in GSH levels and SOD activity.

References:
[1]Fu H Y, Shen L, Gao X S, et al. SF1670 inhibits apoptosis and inflammation via the PTEN/Akt pathway and thus protects intervertebral disc degeneration[J]. European Review for Medical & Pharmacological Sciences, 2020, 24(17).
[2]Grewal A K, Singh N, Singh T G. Neuroprotective effect of pharmacological postconditioning on cerebral ischaemia–reperfusion-induced injury in mice[J]. Journal of Pharmacy and Pharmacology, 2019, 71(6): 956-970.

化学性质

Cas No. 345630-40-2 SDF
化学名 N-(9,10-dioxo-9,10-dihydrophenanthren-2-yl)pivalamide
Canonical SMILES CC(C)(C(NC(C=C1C2=O)=CC=C1C3=C(C2=O)C=CC=C3)=O)C
分子式 C19H17NO3 分子量 307.34
溶解度 ≥ 15.37mg/mL in DMSO 储存条件 Desiccate at -20°C
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1 mM 3.2537 mL 16.2686 mL 32.5373 mL
5 mM 0.6507 mL 3.2537 mL 6.5075 mL
10 mM 0.3254 mL 1.6269 mL 3.2537 mL
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