IC261

IC261 is a selective, ATP-competitive CK1 inhibitor, with IC₅₀s of 1 μM, 1 μM, 16 μM for Ckiδ, Ckiε and Ckiα1, respectively. IC50 & Target: IC50: 1 μM (Ckiδ), 1 μM (Ckiε), 16 μM (Ckiα1)^[1] In Vitro: IC261 is a selective, ATP-competitive CK1 inhibitor, with IC₅₀s of 1 μM, 1 μM, 16 μM for Ckiδ, Ckiε and Ckiα1, respectively. IC261 is less active on PKA, p34^cdc2, and p55^fyn (IC₅₀s > 100 μM)^[1]. IC261 induces mitotic arrest, spindle defects and centrosome amplification in AC1-M88 cells. IC261 (1?μM) increases G2/M cells after 12?h, and causes cell death at 24 h in AC1-M88 cells. IC261 (1?μM) also induces apoptosis in the extravillous trophoblast hybrid cells^[2]. IC261 (1.25 μM) suppresses the proliferation of several pancreatic tumour cell lines, including ASPC-1, BxPc3, Capan-1, Colo357, MiaPaCa-2, Panc1, Panc89, PancTu-1 and PancTu-2 cells. IC261 (1.25 μM) specifically enhances CD95-mediated apoptosis of pancreatic tumour cells^[3]. In Vivo: IC261 (20.5 mg/kg) inhibits tumor growth of PancTu-2 cells in SCID mice, downregulates several anti-apoptotic proteins, such as CK1δ/?, KRAS, and IL6 and upregulates p21, ATM, CHEK1 and STAT1 in mice^[3].