SW044248 是非典型拓扑异构酶 I 抑制剂，对NSCLC细胞具有选择性毒性。

SW044248 is a noncanonical Top1 inhibitor. It has selective toxicity for NSCLC cells.

The potency of JNJ-42041935 for inhibition of the structurally related enzyme FIH is assessed by methods similar to those described for PHD2. In brief, activity of FIH is determined using purified glutathione transferase-tagged full-length FIH amino acids 1 to 350 and a synthetic HIF-1α peptide corresponding to residues Asp788 to Leu822. Compounds are preincubated with 17.1 nM FIH for 30 min, followed by a 10-min incubation with 1 μM [2-14C]2-oxoglutarate, in the presence of 10 μM FeNH4SO4 in reaction buffer. The selectivity of JNJ-42041935 for inhibition of a range of other targets available for testing in commercial assays is also assessed at concentrations of 1 and 10 μM[1].

522650-83-5

C22H23N5O2S

421.52

DMSO:40 mg/mL
Powder: -20°C for 3 years
In solvent: -80°C for 2 years