KZ-02
KZ-02 is an orally active dual MEK1/Pim-1 kinase inhibitor, with an IC50 of 1.07 nM against MEK1 and an IC50 of 1.34 μM against Pim-1. KZ-02 reduces the phosphorylation levels of ERK and Cdc25C, and promotes the proteasomal degradation of Pim-1 protein. KZ-02 inhibits cancer cell growth and exerts anti-tumor effects. KZ-02 can be used in the research of colorectal cancer.
For research use only. We do not sell to patients.
- CAS No.: 1801756-14-8
- Formula: C15H11F2IN4O3S
- Molecular Weight:492.24
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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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Biological Activity
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MEK1 1.07 nM (IC50) |
PIM1 1.34 μM (IC50) |
KZ-02 (0.01-1000 nmol/L; 24-72 h) potently inhibits Colo205 human colorectal cancer cell proliferation with an IC50 of 0.015 nmol/L at 48 h, which is 1033-fold more potent than AZD6244[1].
KZ-02 (1-1000 nmol/L; 2 h, unspecified) inhibits MEK and Pim-1 activity in Colo205 and HT29 human colorectal cancer cells by decreasing ERK and Cdc25C phosphorylation, reducing Pim-1 protein levels, and inhibiting phosphorylation of Pim-1 downstream targets P21Cip1/Waf1, P27Kip1, and Bad[1].
KZ-02 (10 nmol/L; 2 h) increases Pim-1 mRNA levels in Colo205 and HT29 human colorectal cancer cells following 2 h of treatment at 10 nmol/L[1].
KZ-02 (10 nmol/L; 2 h) decreases Pim-1 protein levels in Colo205 and HT29 human colorectal cancer cells by promoting proteasome-dependent degradation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Colo205 and HT29 human colorectal cancer cells
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Concentration:1, 10, 100 and 1000 nM
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Incubation Time:Pretreatment for 2 hours, then 48 hours
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Result:Decreased Pim-1 protein levels and inhibited phosphorylation of ERK (a MEK substrate) and Cdc25C (a Pim-1 substrate) in both cell lines at 10 nM for 2 h.
Decreased Pim-1 protein levels and phosphorylation of P21Cip1/Waf1 (Thr145), P27Kip1 (Thr198), and Bad (Ser112) in Colo205 cells at 1-1000 nM.
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Cell Line:Colo205 and HT29 human colorectal cancer cells
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Concentration:10 nM
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Incubation Time:Pretreatment for 2 hours, then 48 hours
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Result:Significantly increased Pim-1 mRNA levels in both Colo205 and HT29 cells, similar to the effect of AZD6244.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c (male, ~20 g, subcutaneously injected with 1×107 Colo205 human colon cancer cells)[1]
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Dosage:1 mg/kg
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Administration:p.o.; once daily; 20 days
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Result:Inhibited Colo205 xenograft growth by 56.6%.
Showed no apparent effect on mouse body weight during treatment.
Chemical Information
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CAS No. 1801756-14-8
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Molecular Weight 492.24
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Formula C15H11F2IN4O3S
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SMILES
O=C(C1=CC2=C(C(F)=C1NC3=CC=C(C=C3F)I)N=NS2)NOCCO
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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)
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