D-64406
(5-Hydroxy-1H-2-indolyl)(1H-2-indolyl)-methanone

Yellow solid. PROTECT FROM LIGHT. PACKAGED UNDER INERT GAS. A cell-permeable bis (1H-2-indolyl)-1-methanone compound that acts as a highly selective, ATP-competitive inhibitor of platelet-derived growth factor (PDGF) receptor tyrosine kinase (IC₅₀ = 200 nM in Swiss 3T3 cells for PDGFR; IC₅₀ = 90 nM in vitro and 200 nM in PAE cells for PDGFb-R; IC₅₀ = 1 µM for PDGFa-R). Also potently inhibits Flt3 (Fms-like tyrosine kinase 3) activity (IC₅₀ = 300 nM for hPDGFb-R-mFlt3 & 100 nM in EOL-1 cells). Shown to be only weakly active towards Cdk2/cyclin E, EGFR, ErbB2, FGFR-1, GRK2, JAK-2, PKB/Akt, PKC_a,e,i, and c-Src kinases (IC₅₀ > 10 µM). Sensitizes 32D cells to radiation-induced apoptosis. Inhibits DNA synthesis in stimulated-Swiss 3T3 cells (≤ 30 µM), and proliferation of TEL-Flt3-transfected BA/F3 cells (IC₅₀ < 300 nM). Purity: ≥97% by HPLC.

Ref.: Mahboobi, S., et al. 2002. J. Med. Chem. 45, 1002. Teller, S., et al. 2002. Leukemia 16, 1528.