TDI6245

TDI6245 (compound 5) potently inhibits purified AURKA with an IC₅₀ of 21.64 nM^[1].
TDI6245 (48 hours) inhibits the growth of NIH/3T3 mouse embryonic fibroblast cells with an IC₅₀ of 4.67 μM after 48 hours of incubation^[1].
TDI6245 (1 mM; 60 min) binds to the β5 active site of recombinant Plasmodium falciparum 20S proteasome in an antiparallel β-sheet conformation, forming critical hydrogen bonds with residues Ser21, Ala49, Asp153, Ser157, and Ser27 to mediate potent inhibition^[2].
TDI6245 (3 days) inhibits the growth of JIMT-1 breast cancer cells with an IC₅₀ of 60.84 μM after 3 days of incubation^[1].
TDI6245 (3 days) inhibits the growth of MDA-MB-231 triple-negative breast cancer cells with an IC₅₀ of 60.84 μM after 3 days of incubation^[1].
TDI6245 (3 days) inhibits the growth of MDA-MB-453 triple-negative breast cancer cells with an IC₅₀ of 2.947 μM after 3 days of incubation^[1].
TDI6245 (48 hours) inhibits the growth of MDA-MB-231 triple-negative breast cancer cells with an IC₅₀ of 49.78 μM after 48 hours of incubation^[1].
TDI6245 potently inhibits recombinant Plasmodium falciparum 20S proteasome with an IC₅₀ of 0.11 μM, and exhibits 283-fold and 62-fold selectivity over human constitutive 20S proteasome and human immunoproteasome, respectively^[2].
TDI6245 (72 h) inhibits Plasmodium falciparum 3D7 laboratory strain growth in vitro with an EC₅₀ of 0.038 μM after 72 h incubation^[2].
TDI6245 (72 h) inhibits growth of Plasmodium falciparum clinical isolates from Tororo, Uganda ex vivo with a geometric mean EC₅₀ of 84.2 nM after 72 h incubation^[2].
TDI6245 (72 h) inhibits Plasmodium falciparum Dd2 wild-type strain growth with an EC₅₀ of 0.042 μM, β5^A49S mutant strain growth with an EC₅₀ of 0.85 μM, and β6^A117D mutant strain growth with an EC₅₀ of 0.52 μM after 72 h incubation^[2].

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