IC 86621 is recognized as a strong inhibitor of DNA-dependent protein kinase (DNA-PK), with an IC50 value of 120 nM. It functions as a selective and reversible inhibitor that competes with ATP. IC 86621 impedes the repair of cellular DNA double-strand breaks (DSB) mediated by DNA-PK, with an EC50 of 68 µM. It enhances the antitumor activity induced by DSB without causing cytotoxicity and also shields rheumatoid arthritis (RA) T cells from apoptosis[1][2]. Moreover, IC 86621 is highly selective, showing minimal activity against other kinases including PI3K, Cdk2, Src, PKA, PKC, Chk1, CK1, ATM, and FKBP12[1]. Treatment with IC 86621, ranging from 0 to 100 nM for 24 hours, has been found to prevent apoptosis in T cells of patients with rheumatoid arthritis (RA). This protective effect was observed in CD4+CD45RO- T cells collected from both control individuals and RA patients, with concentrations of 0 nM, 50 nM, and 100 nM, effectively shielding RA T cells from programmed cell death[2].
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