ZINC12409120 是一种高选择性的ERK抑制剂。ZINC12409120 通过干扰FGF23:α-Klotho的相互作用而抑制 ERK 活性，IC50为 5.0 μM。
| 生物活性 | ZINC12409120 is a high selectiveERKinhibitor. ZINC12409120 acts on disruptingFGF23:α-Klothointeraction to inhibitERKactivity with anIC50of 5.0 μM[1]. |
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体外研究
(In Vitro) | FGF23 induces hypophosphatemia, mediated by ternary complex formed by FGF23, the FGF receptor (FGFR), and α-Klotho[1].
ZINC12409120 (1 nM-0.1 mM; 5 h) inhibits ERK reporter activities mediated by FGF23 (1 μM), with an IC50of 5 μM[1].
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[1].
ZINC12409120 has an half-life of 8.4 h, predicted by pkCSM64 (http://biosig.unimelb.edu.au/pkcsm/)[1].
Cell Proliferation Assay[1] | 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 IC50of 5 μM. And reduced FGF23-mediated ERK activities by 70%, as well. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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