ZINC12409120

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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.

For research use only. We do not sell to patients.

ZINC12409120 Chemical Structure

CAS No. : 1010888-06-8

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Description

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^[1].

IC₅₀ & Target

ERK

5 μM (IC₅₀)

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 IC₅₀ of 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].

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

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 IC₅₀ of 5 μM. And reduced FGF23-mediated ERK activities by 70%, as well.

Molecular Weight

344.37

Formula

C₂₀H₁₆N₄O₂

CAS No.

1010888-06-8

SMILES

O=C(N1CC2=C(C=CC=C2)CC1)C3=NC(C4=CC=CC5=C4C=CN5)=NO3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Liu SH, et al. Identification of Small-Molecule Inhibitors of Fibroblast Growth Factor 23 Signaling via In Silico Hot Spot Prediction and Molecular Docking to α-Klotho. J Chem Inf Model. 2022 Jul 22. [Content Brief]

ZINC12409120 Related Classifications

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Help & FAQs

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.

Keywords:

ZINC124091201010888-06-8ZINC 12409120ZINC-12409120ERKExtracellular signal regulated kinasesα-klohoHEK 293TFGFR1cepidermal growth factorEGFEGFRfibroblast growth factorselectivehypophosphatemiaInhibitorinhibitorinhibit

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