NS-0011
NS-0011 is a CDK5 inhibitor with a Kd value of 16 μM. NS-0011 binds to the nuclear export signal domain of CDK5, disrupts its interaction with CRM-1 and increases the accumulation of CDK5 in the nucleus. NS-0011 inhibits the proliferation of gastric cancer cells. NS-0011 suppresses the occurrence of gastric cancer xenograft tumors. NS-0011 is applicable to gastric cancer-related research.
For research use only. We do not sell to patients.
- CAS No.: 1076234-33-7
- Formula: C12H9ClF3N3O2
- Molecular Weight:319.67
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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
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
CDK5 16 μM (Kd) |
In Vitro
NS-0011 binds directly to purified recombinant CDK5 protein with a binding constant of 16 μmol/L[1].
NS-0011 (1-2 μmol/L; 24-80 h) accumulates CDK5 in the nucleus and completely inhibits proliferation of MGC-803 human gastric cancer cells at 2 μmol/L, an effect dependent on CDK5 expression[1].
NS-0011 (2 μmol/L; 48 h) specifically upregulates p16 expression in MGC-803 and SGC-7901 human gastric cancer cells at 2 μmol/L for 48 hours[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human gastric cancer MGC-803 cells
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Concentration:1-2 μmol/L (immunofluorescence; proliferation; proliferation with CDK5 siRNA)
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Incubation Time:24 h (immunofluorescence); up to 80 h (proliferation); up to 72 h (proliferation with CDK5 siRNA)
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Result:Caused clear accumulation of CDK5 in the nucleus of MGC-803 cells at 2 μmol/L for 24 h.
Inhibited MGC-803 cell proliferation in a dose-dependent manner: completely inhibited cell growth at 2 μmol/L over 80 h, while caused partial inhibition at 1 μmol/L.
Saw its antiproliferative effect largely reversed when CDK5 was depleted by siRNA.
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Cell Line:human gastric cancer MGC-803 and SGC-7901 cells
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Concentration:2 μmol/L
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Incubation Time:48 h
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Result:Significantly increased p16 protein levels in both MGC-803 and SGC-7901 cells.
Had no effect on the levels of p21, p27, or p57.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude mice (6-week-old male, immunocompromised, subcutaneous xenograft model via MGC-803 gastric cancer cell injection)[1]
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Dosage:2 μmol/L (pretreatment of cells); 4 μmol/L (in cell suspension for injection)
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Administration:in vitro pretreatment (48 hours); in-cell suspension injection
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Result:Significantly suppressed xenograft tumorigenesis, resulting in reduced maximum tumor diameter and reduced tumor weight compared to DMSO controls.
Chemical Information
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CAS No. 1076234-33-7
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Molecular Weight 319.67
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Formula C12H9ClF3N3O2
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SMILES
O=C1C(C)=C(C)C(N1NC2=NC(Cl)=C(C(F)(F)F)C=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.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
NS-0011 Related Classifications
HY-183235 Related Classifications
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