2. Metabolic Enzyme/Protease NF-κB Immunology/Inflammation Neuronal Signaling Cell Cycle/DNA Damage
  3. 17β-HSD Reactive Oxygen Species (ROS) Tau Protein Amyloid-β CDK Mitochondrial Metabolism
  4. 17β-HSD10-IN-4

17β-HSD10-IN-4 是一种具有脑穿透性的选择性 17β-HSD10 抑制剂，其 IC50 为 6.33 μM。\n

17β-HSD10-IN-4 可与 17β-HSD10 的催化三联体形成关键相互作用，从而在功能上抑制该酶，且不会改变其蛋白水平。17β-HSD10-IN-4 可恢复线粒体功能、降低 ROS 水平、增加 ATP 生成并抑制细胞色素 c 释放。17β-HSD10-IN-4 可减弱 CDK5/p25 的激活、减少 Tau 蛋白过度磷酸化与 Aβ 斑块负荷，并恢复脑源性神经营养因子水平。17β-HSD10-IN-4 可改善认知功能，可用于阿尔茨海默病的相关研究。

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17β-HSD10-IN-4

17β-HSD10-IN-4 Chemical Structure

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17β-HSD10-IN-4 相关抗体

Top Publications Citing Use of Products

查看 CDK 亚型特异性产品:

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CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85 CDK10 CDK15 CDK17 CDK18 CDK20 PITSLRE

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

17β-HSD10-IN-4 is a selective brain-penetrant 17β-HSD10 inhibitor with an IC50 of 6.33 μM.

17β-HSD10-IN-4 forms key interactions with the 17β-HSD10 catalytic triad to functionally inhibit the enzyme, without altering its protein levels. 17β-HSD10-IN-4 restores mitochondrial function, reduces ROS levels, increases ATP production, and suppresses cytochrome c release. 17β-HSD10-IN-4 attenuates CDK5/p25 activation, reduces Tau hyperphosphorylation, Aβ plaque load and restores brain-derived neurotrophic factor levels. 17β-HSD10-IN-4 improves cognitive function.17β-HSD10-IN-4 can be used for the research of Alzheimer's disease[1].
IC50 & Target[1]

17β-HSD10

6.33 μM (IC50)

Cdk5/p25

 

体外研究
(In Vitro)

17β-HSD10-IN-4 (Compound 14)(24 h) 可在转染 pCMV-Neo_17β-HSD10 的 HEK-293 细胞中强效抑制 17β-HSD10 的活性，其 IC50 为 6.33 ± 0.15 μM[1]。
17β-HSD10-IN-4 (10 h) 具有良好的血脑屏障通透性，其 Pe 值为 4.75 ± 0.31 × 10-6 cm·s-1，符合中枢神经系统通透性的标准[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

17β-HSD10-IN-4 相关抗体:
体内研究
(In Vivo)

17β-HSD10-IN-4 (Compound 14) (10 mg/kg；腹腔注射；每日一次；连续 14 天) 可显著改善 APP/PS1 转基因小鼠的认知功能，恢复线粒体功能，减轻 Tau 蛋白过度磷酸化，提升 BDNF 水平，并使 Aβ 斑块负荷降低，且不会改变 17β-HSD10 蛋白水平[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6 (B6) APPswe/PSEN1dE9 (APP/PS1) transgenic (male, 6 months old)[1]
Dosage: 10 mg/kg
Administration: i.p.; daily; 14 days
Result: Improved spatial learning and memory, with treated mice spending 29 seconds in the target quadrant during the Morris water maze probe trial, demonstrating reduced escape latency, increased platform crossings, and goal-directed swimming trajectories.
Reduced cerebral reactive oxygen species (ROS) levels by 24% and increased ATP content by 76% in APP/PS1 mouse brain cells; suppressed cytochrome c release to near wild-type levels.
Reduced cortical phosphorylated Tau (p-Tau) levels by 32% and cortical p-Tau/Tau ratio by 18%; reduced hippocampal p-Tau levels by 18% and hippocampal p-Tau/Tau ratio by 11%; reduced CDK5 overexpression by 13% in the cortex and 7% in the hippocampus.
Increased cortical brain-derived neurotrophic factor (BDNF) levels by 58% compared to untreated APP/PS1 mice, restoring levels to near wild-type values.
Reduced cerebral Aβ plaque load by approximately two-thirds (plaque burden was one-third of that in untreated APP/PS1 mice).
Showed no significant change in 17β-HSD10 protein expression relative to untreated APP/PS1 mice.
分子量

288.32

Formula

C14H12N2O3S
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

17β-HSD10-IN-4 相关分类

  • 摩尔计算器

  • 稀释计算器

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

17β-HSD10-IN-417β-HSDReactive Oxygen Species (ROS)Tau ProteinAmyloid-βCDKMitochondrial Metabolism17beta-HSD17β-hydroxysteroid dehydrogenases17 beta-hydroxysteroid dehydrogenaseβ-amyloid peptideAβAbetaCyclin dependent kinaseAlzheimer's diseasemitochondrial functionCDK5/p25blood-brain barrier17β-HSD10brain-derived neurotrophic factorATPreactive oxygen speciescytochrome cTau hyperphosphorylationInhibitorinhibitorinhibit

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