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
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CDK5 16 μM (Kd) |
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.
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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