ADA-07
ADA-07 is a TOPK inhibitor with activity at the ATP-binding pocket that does not inhibit MEK1 activity. ADA-07 suppresses solar ultraviolet (SUV)-induced phosphorylation of ERK1/2, p38, and JNKs, and inhibits AP-1 activity. ADA-07 attenuates tumor incidence, multiplicity, and volume in SUV-exposed SKH-1 hairless mice. ADA-07 can be used for the research of solar ultraviolet-induced skin carcinogenesis.
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- CAS. Nr.: 2252153-94-7
- Formel: C18H20N2O2
- Molecular Weight:296.37
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
TOPK |
ERK1 |
ERK2 |
p38 |
JNK |
AP-1 |
In Vitro
ADA-07 binds directly to the ATP-binding pocket of TOPK via hydrogen bonding with Gly118 and Gly119[1].
ADA-07 binds TOPK in an ATP-competitive manner[1].
ADA-07 (2.5 mg; overnight) binds to endogenous TOPK and MEK1/2 present in HaCaT human skin keratinocyte lysates[1].
ADA-07 (0.5-5 μM; 30 min) potently and selectively inhibits the kinase activity of active human recombinant TOPK, but does not inhibit active human recombinant MEK1[1].
ADA-07 (1.25-10 μM; 24-48 h) is non-cytotoxic to JB6 P+ mouse epidermal cells and NHDF normal human dermal fibroblasts at concentrations below 10 μM after 24 or 48 h of incubation[1].
ADA-07 (1.25-5 μM; 4 h pre-incubation) dose-dependently inhibits SUV-induced phosphorylation of ERK1/2, p38, JNKs, and c-Jun in HaCaT human skin keratinocytes and JB6 P+ mouse epidermal cells[1].
ADA-07 (1.25-5 μM; 24 h) dose-dependently inhibits basal phosphorylation of ERK1/2, p38, JNKs, and c-Jun in SCC12 human squamous cell carcinoma cells and A431 human epidermoid carcinoma cells[1].
ADA-07 (1.25-5 μM; 1 h pre-incubation) dose-dependently inhibits SUV-induced AP-1 transactivation in JB6 P+ mouse epidermal cells stably expressing an AP-1 luciferase reporter[1].
ADA-07 (1.25-10 μM; 1-2 weeks) dose-dependently inhibits EGF-induced neoplastic transformation of JB6 P+ mouse epidermal cells in an anchorage-independent growth assay[1].
ADA-07 (0.625-10 μM; several days) dose-dependently suppresses the proliferation of SCC12 human squamous cell carcinoma cells and A431 human epidermoid carcinoma cells in a crystal violet staining assay[1].
ADA-07 (1.25-5 μM; 24 h) suppresses AP-1 activity in control A431 human epidermoid carcinoma cells in a dose-dependent manner, but has minimal effect on AP-1 activity in TOPK-knockdown A431 cells, confirming that ADA-07 acts by targeting TOPK[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:JB6 P+ mouse epidermal cells, NHDF normal human dermal fibroblasts
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Concentration:1.25 μM; 2.5 μM; 5 μM; 10 μM
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Incubation Time:24 h; 48 h
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Result:Showed no cytotoxicity at concentrations less than 10 μM in both JB6 P+ mouse epidermal cells and NHDF normal human dermal fibroblasts.
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Cell Line:SCC12 human squamous cell carcinoma cells, A431 human epidermoid carcinoma cells
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Concentration:0.625 μM; 1.25 μM; 2.5 μM; 5 μM; 10 μM
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Incubation Time:several days
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Result:Decreased cell proliferation strongly in both SCC12 and A431 cells in a dose-dependent manner, with significant inhibition observed starting at 1.25 μM.
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Cell Line:HaCaT human skin keratinocytes, JB6 P+ mouse epidermal cells
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Concentration:1.25 μM; 2.5 μM; 5 μM ; 60 kJ UVA/m2, 2.9 kJ UVB/m2 SUV
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Incubation Time:4 h (ADA-07 pre-incubation); 15 min (post-SUV exposure incubation)
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Result:Suppressed SUV-induced phosphorylation of ERK1/2, p38, and JNKs in a dose-dependent manner in both HaCaT and JB6 P+ cells.
Suppressed SUV-induced phosphorylation of c-Jun in a dose-dependent manner in both cell lines.
Showed no significant changes in phosphorylated or total TOPK protein levels.
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Cell Line:SCC12 human squamous cell carcinoma cells, A431 human epidermoid carcinoma cells
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Concentration:1.25 μM; 2.5 μM; 5 μM
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Incubation Time:24 h
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Result:Blocked phosphorylation of ERK1/2, p38, and JNKs in a dose-dependent manner in both SCC12 and A431 cells.
Attenuated phosphorylation of c-Jun in a dose-dependent manner in both cell lines.
Showed no significant changes in phosphorylated or total TOPK protein levels.
In Vivo
ADA-07 (0.1-1 mg; topical; 3 times weekly; 13 weeks) significantly suppresses established SUV-induced skin carcinogenesis in SKH-1 hairless mice by inhibiting SUV-induced phosphorylation of ERK1/2, p38, and JNKs and reducing cell proliferation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:SKH-1 hairless mice (female, 6-8 weeks old, mean body weight 25 g, chronic solar ultraviolet-induced skin carcinogenesis early-stage prevention model)[1]
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Dosage:0.1 mg; 1 mg
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Administration:topical; 3 times weekly; 28 weeks
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Result:Completely inhibited SUV-induced papilloma formation.
Reduced SUV-induced epidermal thickness.
Decreased PCNA expression (a marker of cell proliferation).
Suppressed SUV-induced phosphorylation of ERK1/2, p38, and JNKs in mouse skin.
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Animal Model:SKH-1 hairless mice (female, 6-8 weeks old, mean body weight 25 g, chronic solar ultraviolet-induced skin carcinogenesis late-stage prevention model)[1]
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Dosage:0.1 mg; 1 mg
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Administration:topical; 3 times weekly; 13 weeks
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Result:Substantially suppressed SUV-induced tumor incidence.
Significantly reduced tumor volume and multiplicity.
Decreased SUV-induced epidermal thickness.
Inhibited SCC formation.
Decreased PCNA expression.
Suppressed SUV-induced phosphorylation of ERK1/2, p38, and JNKs in mouse skin.
Chemical Information
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CAS. Nr. 2252153-94-7
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Molecular Weight 296.37
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Formel C18H20N2O2
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SMILES
O=C1NC2=CC=C(C=C2C1=NO)C34CC5CC(CC(C5)C3)C4
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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