SP 4206

Definition

ChEBI: N(2)-carbamimidoyl-N-{2-[4-(3-{4-[(5-carboxyfuran-2-yl)methoxy]-2,3-dichlorophenyl}-1-methyl-1H-pyrazol-5-yl)piperidin-1-yl]-2-oxoethyl}-D-leucinamide is a leucine derivative obtained by fpormal condensation of the secondary amino group of 5-({2,3-dichloro-4-[1-methyl-5-(piperidin-4-yl)-1H-pyrazol-3-yl]phenoxy}methyl)-2-furoic acid and the carboxy group of N-amidino-L-leucylglycine It is a member of guanidines, a furoic acid, a pyrazolylpiperidine, a glycine derivative, a dichlorobenzene and a D-leucine derivative.

Biological Activity

SP4206 is an IL-2/IL-2Rα interaction inhibitor. SP4206 binds with high affinity (Kd=70 nM) to IL-2 and blocks binding to its natural receptor IL-2Rα (Kd=10 nM)[1]. SP4206 binds the WT IL-2, IL-2 variant K35L/M39V, IL-2 variant P65A, and IL-2 variant V69A with EC50s of 68.8, 80.1, 117.0, and 10.4 nM, respectively[1].

References

[1]. Thanos CD, et al. Hot-spot mimicry of a cytokine receptor by a small molecule. Proc Natl Acad Sci U S A. 2006 Oct 17;103(42):15422-7.

Raw materials

Preparation Products