BLINK11
BLINK11 is a BBB-penetrant CDK5 inhibitor. BLINK11 lowers CDK5 activity for both complexes CDK5/p35 (IC50 = 17.09 nM) and CDK5/p25 (IC50 = 14.69 nM). BLINK11 offers anti-diabetic and neuroprotective benefits. BLINK11 lowers blood glucose, enhances cognition, and reduces neurodegeneration in T2D mice.
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- Fòrmula: C25H22Cl3N3O4
- Peso molecular:534.82
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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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CDK5/p35 17.09 nM (IC50) |
cdk9-cyclin T 83.43 nM (IC50) |
Cdk5/p25 14.69 nM (IC50) |
CDK1/Cly Y 39.34 nM (IC50) |
CDK2/ClyA2 83.43 nM (IC50) |
BLINK11 (50 nM-100 nM, 24 h) lowers CDK5 activity for both complexes CDK5/p35 (IC50 = 17.09 nM) and CDK5/p25 (IC50 = 14.69 nM)[1].
BLINK11 (50 nM-100 nM, 24 h) shows declined CDK5 activity in N2A cell lines overexpressing CDK5/p35 and CDK5/p25[1].
BLINK11 (100-500 μM, 7 h) shows the ability to traverse the BBB and access the central nervous system[1].
BLINK11 (25-500 μM, 24 h) maintains cell viability above 50% at all doses in HEK293T, HepG2, and N2A cell lines[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.
Reduced phospho-NF-H levels at higher dose.
Mitigated HFD-induced neurodegeneration through the inhibition of phosphorylation events involving NF-H and tau proteins.
Chemical Information
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Peso molecular 534.82
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Fòrmula C25H22Cl3N3O4
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SMILES
O=C(NC1=CC=CC(Cl)=C1Cl)C2=CC=CC=C2OCC(NC3=CC=C(N4CCOCC4)C(Cl)=C3)=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)
BLINK11 Related Classifications
HY-173347 Related Classifications
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