ZINC12409120

Research use only, not for human use.

ZINC12409120 (R-4584) is a selective ERK inhibitor.ZINC12409120 inhibits ERK with an IC50 of 5.0 μM.ZINC12409120 inhibits ERK activity by interfering with FGF23:α-Klotho interaction.

ZINC12409120 is a high selective ERK inhibitor. ZINC12409120 acts on disrupting FGF23:α-Klotho interaction to inhibit ERK activity with an IC50 of 5.0 μM.

FGF23 induces hypophosphatemia, mediated by ternary complex formed by FGF23, the FGF receptor (FGFR), and α-Klotho.ZINC12409120 (1 nM-0.1 mM; 5 h) inhibits ERK reporter activities mediated by FGF23 (1 μM), with an IC50 of 5 μM.ZINC12409120 (10 μM; 5 h) specificaly inhibits ERK activity mediated by FGF23:α-Klotho instead of EGF-mediated ERK activation, and exhibits no inhibitory effect on EGFR tyrosine kinase or EGF/EGFR interaction.ZINC12409120 has an half-life of 8.4 h, predicted by pkCSM64 .Cell Proliferation Assay Cell Line:Human embryonic kidney (HEK) 293T cells Concentration:1 nM-0.1 mM Incubation Time:5 hours Result:Inhibited FGF23-mediated ERK reporter activity in a dose-dependent manner, with an IC50 of 5 μM. And reduced FGF23-mediated ERK activities by 70%, as well.

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MAPK/ERK Signaling

ERK

ERK

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1010888-06-8

344.37

C20H16N4O2

>98% (HPLC)

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C(=O)(C1=NC(C2=C3C(NC=C3)=CC=C2)=NO1)N4CC=5C(CC4)=CC=CC5

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(-20℃)

With Ice Pack

≥ 2 years