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.
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- Fòrmula: C24H19BrN2O6
- Peso molecular:511.32
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
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Actividad biológica
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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) |
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.
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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Peso molecular 511.32
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Fòrmula 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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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
BLINK15 Related Classifications
HY-173348 Related Classifications
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