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 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.

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17β-HSD10-IN-4

17β-HSD10-IN-4 構造式

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17β-HSD10-IN-4 関連抗体

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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

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製品説明

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

 

体外実験

17β-HSD10-IN-4 (Compound 14) (24 h) potently inhibits 17β-HSD10 activity in pCMV-Neo_17β-HSD10-transfected HEK-293 cells with an IC50 of 6.33 ± 0.15 μM[1].
17β-HSD10-IN-4 (10 h) exhibits favorable blood-brain barrier permeability with a Pe value of 4.75 ± 0.31 × 10-6 cm·s-1, qualifying it as CNS-permeable[1].

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

17β-HSD10-IN-4 関連抗体
体内実験

17β-HSD10-IN-4 (Compound 14) (10 mg/kg; i.p.; daily; 14 days) significantly improves cognitive function, restores mitochondrial function, attenuates Tau hyperphosphorylation, elevates BDNF levels, and reduces Aβ plaque load in APP/PS1 transgenic mice, without altering 17β-HSD10 protein levels[1].

MedChemExpress (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

分子式

C14H12N2O3S
SMILES

O=C1C2=C(C(C3=C1N=C(S3)NCCCO)=O)C=CC=C2
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

Please store the product under the recommended conditions in the Certificate of Analysis.
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17β-HSD10-IN-4 Related Classifications

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  • Do most proteins show cross-species activity?

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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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製品名:
17β-HSD10-IN-4
製品番号:
HY-182028
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