D4476, 5 mg

A selective, potent, and cell-permeant inhibitor of casein kinase 1 (CK1) supplied by STEMCELL Technologies. The compound inhibits CK1 and CK1δ with IC50 values of 200 nM and 300 nM, respectively, and inhibits the transforming growth factor β1 (TGF-β1) type I receptor ALK5 with IC50 = 500 nM. It is described as an Activin/NODAL/TGF-β pathway inhibitor that also inhibits CK1, ALK5 and p38 MAPK. The molecular weight is 398.4 g/mol and the purity is ≥ 98%; the material is a crystalline solid.

In reprogramming research, D4476 has been used alongside forskolin to reprogram mouse somatic cells into pluripotent cells by acting as a chemical substitute for OCT4. In cancer research, published applications include inducing apoptosis of multiple myeloma cell lines and exhibiting anti-leukemic activity by selectively killing leukemia stem cells over normal hematopoietic stem and progenitor cells.

The product should be stored at -20°C as supplied, protected from prolonged exposure to light, and stored with a desiccant for long-term storage. Stock solutions can be prepared in DMSO at concentrations up to 75 mM or in absolute ethanol at up to 25 mM. The compound has low solubility in aqueous media; for cell culture use, stock solution should be diluted into culture medium immediately before use, with final DMSO concentration kept below 0.1% to avoid potential cell toxicity. Products are for research use only.