Deltafluorine 

Deltafluorine is a phosphodiesterase delta (PDEδ) inhibitor with an IC₅₀ of 27 nM, a K_D of 148 nM. Deltafluorine covalently modifies the specific glutamate residue p.E88 in the ligand binding site of PDEδ, interfering with its chaperone function. Deltafluorine inhibits signaling through the MAPK and Akt-mTOR pathway, reduces ERK1/2 expression. Deltafluorine reduces tumor volume in an autochthonous mouse model of Kras-driven lung adenocarcinoma. Deltafluorine can be used for the research of lung adenocarcinoma^[1].

Deltafluorine (Compound 22a) (60 μM; 0-7 days) covalently modifies purified PDEδ at residue p.E88 with >85% efficiency over 7 days in vitro, with a second-order rate constant of 5.4 M⁻¹ s^−1[1].
Deltafluorine (10 μM; 2 h) induces significant thermal stabilization of PDEδ in Jurkat cells with a ΔT_m of 16.6 ± 3.2 °C^[1].
Deltafluorine (5 μM; 0.25-4 h) reduces phosphorylation of ERK1/2 and S6 in PA-TU-8902 cells^[1].
Deltafluorine (5 μM; 0-120 h) inhibits the proliferation of PA-TU-8902 cells with 84 ± 2% growth inhibition^[1].
Deltafluorine (5 μM; 2 h) inhibits the MAPK and Akt-mTOR pathways in PA-TU-8902 cells^[1].

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

Deltafluorine (Compound 22a) (15 mg/kg; i.p.; daily; 21 days) treatment significantly reduces tumor growth in a highly aggressive Kras-driven lung adenocarcinoma mouse model^[1].

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

677.29

C₃₃H₄₂ClFN₄O₄S₂

CC1=NC(C)=C(CF)C=C1CN(S(=O)(C2=CC=C(S(=O)(N(C3CCCC3)CC4=CC=C(Cl)C=C4)=O)C=C2)=O)CC5CCNCC5

Room temperature in continental US; may vary elsewhere.

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

• [1]. Zhang R, et al. Targeting a Glutamic Acid in PDEδ with Fluoromethyl-Aryl Electrophiles Impairs K-Ras Signaling. J Med Chem. 2026;69(2):964-981.  [Content Brief]