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Cat. No.: HY-122859

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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 No.: 2252153-94-7
화학식: C₁₈H₂₀N₂O₂
분자량:296.37

보관:

Please store the product under the recommended conditions in the Certificate of Analysis.

ADA-07 Chemical Structure

CAS No.: 2252153-94-7

Amount: USD 0.00

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
순도&문서
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

IC₅₀ & Target

^[1]

TOPK

ERK1

ERK2

p38

JNK

AP-1

All ERK Isoforms :

All p38 MAPK Isoforms :

All JNK Isoforms :

All AP-1 Isoforms :

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.

Cell Cytotoxicity Assay^[1]

Cell Line:

JB6 P+ mouse epidermal cells, NHDF normal human dermal fibroblasts
Concentration:

1.25 μM; 2.5 μM; 5 μM; 10 μM
Incubation Time:

24 h; 48 h
Result:

Showed no cytotoxicity at concentrations less than 10 μM in both JB6 P+ mouse epidermal cells and NHDF normal human dermal fibroblasts.

Cell Proliferation Assay^[1]

Cell Line:

SCC12 human squamous cell carcinoma cells, A431 human epidermoid carcinoma cells
Concentration:

0.625 μM; 1.25 μM; 2.5 μM; 5 μM; 10 μM
Incubation Time:

several days
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.

Western Blot Analysis^[1]

Cell Line:

HaCaT human skin keratinocytes, JB6 P+ mouse epidermal cells
Concentration:

1.25 μM; 2.5 μM; 5 μM ; 60 kJ UVA/m², 2.9 kJ UVB/m² SUV
Incubation Time:

4 h (ADA-07 pre-incubation); 15 min (post-SUV exposure incubation)
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.

Western Blot Analysis^[1]

Cell Line:

SCC12 human squamous cell carcinoma cells, A431 human epidermoid carcinoma cells
Concentration:

1.25 μM; 2.5 μM; 5 μM
Incubation Time:

24 h
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; 28 weeks) completely prevents 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].
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.

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]
Dosage:

0.1 mg; 1 mg
Administration:

topical; 3 times weekly; 28 weeks
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.

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]
Dosage:

0.1 mg; 1 mg
Administration:

topical; 3 times weekly; 13 weeks
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

CAS No. 2252153-94-7
분자량 296.37
화학식 C₁₈H₂₀N₂O₂
SMILES

O=C1NC2=CC=C(C=C2C1=NO)C34CC5CC(CC(C5)C3)C4
선적

Room temperature in continental US; may vary elsewhere.
보관

Please store the product under the recommended conditions in the Certificate of Analysis.

순도&문서

Handling Instructions (2659 KB)

References

[1]. Gao G, et al. ADA-07 Suppresses Solar Ultraviolet-Induced Skin Carcinogenesis by Directly Inhibiting TOPK. Molecular cancer therapeutics. 2017 Sep;16(9):1843-1854.

Calculators

몰농도 계산기

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

MOQ

Minimum order quantity

100 mg

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Amount: USD 0.00

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
순도&문서
References

상품명:
Cat. No.:
수량:
MCE Japan Authorized Agent:

상품명:
CAS No.:
Species:
Purity:
수량:

ADA-07

All ERK Isoforms

All p38 MAPK Isoforms

All JNK Isoforms

All AP-1 Isoforms