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  3. DHPS-IN-2

DHPS-IN-2 is an allosteric deoxyhypusine synthase (DHPS) inhibitor with an IC50 of 70 nM and a Kd of 26.4 μM. DHPS-IN-2 significantly suppresses melanoma cell migration and invasiveness in vitro and exhibits potent anti-tumor efficacy in an A375 cell zebrafish xenograft model. DHPS-IN-2 can be used for the study of melanoma.

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DHPS-IN-2

DHPS-IN-2 Chemical Structure

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Description

DHPS-IN-2 is an allosteric deoxyhypusine synthase (DHPS) inhibitor with an IC50 of 70 nM and a Kd of 26.4 μM. DHPS-IN-2 significantly suppresses melanoma cell migration and invasiveness in vitro and exhibits potent anti-tumor efficacy in an A375 cell zebrafish xenograft model. DHPS-IN-2 can be used for the study of melanoma[1].

In Vitro

DHPS-IN-2 (Compound 7C16) inhibits A375 and B16 cell proliferation with IC50 of 4.0 and 14.4 μM, and has a low cytotoxicity towards normal HaCaT cells (CC50 = 16.6 μM)[1].
DHPS-IN-2 (1-10 μM) significantly inhibits the invasion and migration abilities of A375 cells[1].
DHPS-IN-2 (1-10 μM, 24 h) inhibits melanoma proliferation by modulating the expression of melanoma-associated proteins (elF5A-Hyp) in A375 cells[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: A375 cells
Concentration: 1, 5 and 10 μM
Incubation Time: 24 h
Result: Significantly reduced the level of eIF5A-Hyp.
Reduced the melanoma markers GP-100 and tyrosinase.
Did not affect the total expression of DHPS protein.
In Vivo

DHPS-IN-2 (Compound 7C16) (15.6 μM, 7 days) exhibits potent anti-melanoma activity in zebrafish xenograft models[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: A375 cells were fluorescently labeled with CM-DiI and Xenograft via microinjection into the yolk sac of 2 dpf wild-type AB strain zebrafish[1]
Dosage: 15.6 μM
Administration: 7 days
Result: Exhibited superior antitumor efficacy at lower concentrations.
Molecular Weight

406.22

Formula

C17H15IN2O2

SMILES

IC1=CC=C(C=C1)CC2=NN=C(CC3=CC=CC=C3OC)O2

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Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation
References
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DHPS-IN-2 Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
DHPS-IN-2
Cat. No.:
HY-175828
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