BLINK15
BLINK15 is a BBB-penetrant CDK5 inhibitor. BLINK15 lowers CDK5 activity for both complexes CDK5/p35 (IC50 = 29.34 nM) and CDK5/p25 (IC50 = 12.08 nM). BLINK15 offers anti-diabetic and neuroprotective benefits. BLINK15 lowers blood glucose, enhances cognition, and reduces neurodegeneration in T2D mice.
For research use only. We do not sell to patients.
- Formula: C24H19BrN2O6
- Molecular Weight:511.32
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
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CDK9/Cyclin T 74.63 nM (IC50) |
CDK1/Cly Y 35.84 nM (IC50) |
CDK2/ClyA2 44.12 nM (IC50) |
CDK5/p35 29.34 nM (IC50) |
Cdk5/p25 12.08 nM (IC50) |
In Vitro
BLINK15 (50 nM-100 nM, 24 h) lowers CDK5 activity for both complexes CDK5/p35 (IC50 = 29.34 nM) and CDK5/p25 (IC50 = 12.08 nM)[1].
BLINK15 (50 nM-100 nM, 24 h) shows declined CDK5 activity in N2A cell lines overexpressing CDK5/p35 and CDK5/p25[1].
BLINK15 (25-500 μM, 24 h) maintains cell viability above 50% at all doses in HEK293T, HepG2, and N2A cell lines[1].
BLINK15 (100-500 μM, 7 h) shows the ability to traverse the BBB and access the central nervous system[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:High-fat diet (HFD)-fed (3-4 weeks), four-week-old male C57BL/6J mice (n=40)[1]
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Dosage:20 mg/kg/day, 40 mg/kg/day
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Administration:Intraperitoneal injection (i.p.), 20 days, 3 months after HFD-fed for 3-4 weeks
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Result:Demonstrated rescued symptoms caused by T2D including gaining of body weight, glucose tolerance test (GTT) and insulin tolerance test (ITT) level.
Alleviated cognitive impairment including rescued muscle strength and prevent anxiety, showing mitigated adverse effects of HFD level.
Rescued memory and spatial learning impairments in T2D mouse models with 40 mg/kg/day dosage but no effect with 20 mg/kg/day.
Significantly reduced CDK5 activity even in the presence of p25.
Chemical Information
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Molecular Weight 511.32
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Formula C24H19BrN2O6
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SMILES
O[C@](C1=C(N2CC3=CC=CC=C3)C=CC(Br)=C1)(CC(C4=CC([N+]([O-])=O)=C(OC)C=C4)=O)C2=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Neurotoxicity Study
This protocol assesses in vitro neurotoxicity by combining neuronal viability, mitochondrial/metabolic activity, neurite outgrowth, and optional neuronal network function readouts. Calcein-AM or resazurin/PrestoBlue readouts estimate viable or metabolically active cells; βIII-tubulin immunofluorescence detects neuronal morphology and neurite networks; TMRE detects mitochondrial membrane potential; and MEA recordings detect functional changes in neuronal network activity.
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
BLINK15 Related Classifications
HY-173348 Related Classifications
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