Cas No.: | 978-62-1 |
Chemical Name: | N-(3,5-Bis(trifluoromethyl)phenyl)-5-chloro-2-hydroxybenzamide |
Synonyms: | IMD-0354;IMD 0354;N-[3,5-bis(trifluoromethyl)phenyl]-5-chloro-2-hydroxybenzamide;IKK-2 Inhibitor V;N-(3,5-Bis-trifluoromethylphenyl)-5-chloro-2-hydroxybenzamide;IMD0354;N-(3,5-bis(trifluoromethyl)phenyl)-5-chloro-2-hydroxybenzamide;76145IS906;Benzamide, N-(3,5-bis(trifluoromethyl)phenyl)-5-chloro-2-hydroxy-;Benzamide, N-[3,5-bis(trifluoromethyl)phenyl]-5-chloro-2-hydroxy-;CHILCFMQWMQVAL-UHFFFAOYSA-N;IKK2 Inhibitor V;Kinome_1864;C15H8ClF6NO2;MLS0 |
SMILES: | ClC1C([H])=C([H])C(=C(C=1[H])C(N([H])C1C([H])=C(C(F)(F)F)C([H])=C(C(F)(F)F)C=1[H])=O)O[H] |
Formula: | C15H8ClF6NO2 |
M.Wt: | 383.6729 |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | IMD-0354 is a selective IKKβ inhibitor which inhibits NF-κB activity. IMD0354 inhibits TNF-α induced NF-κB transcription activity with an IC 50 of 1.2±0.3 uM. |
In Vivo: | Daily administration with 5 mg/kg IMD-0354 significantly suppresses tumor expansion in nude mice implanted with established MDA-MB-231 tumors. In mice treated with IMD-0354, tumor progression is restrained[3]. The number of infiltrating cells in aqueous humor is 53.6±9.8×105, 72.5±17.0×105, 127.25±32.0×105, and 132.0±25.0×105 cells/mL in rats treated with 30, 10, 3, or 0 mg/kg of IMD-0354, respectively. The total protein concentrations of aqueous humor are 92.6±3.1 mg/mL, 101.5±6.8 mg/mL, 112.6±1.9 mg/mL, and 117.33±1.8 mg/mL in rats treated with 30, 10, 3, and 0 mg/kg of IMD-0354, respectively[4]. |
In Vitro: | IMD-0354 inhibits NF-κB activity in HMC-1 cells, resulting in complete repression of growth factor-independent proliferation of mast cells. When the DNA-binding activity of NF-κB is inhibited by treatment with IMD-0354, cell proliferation is completely suppressed. HMC-1 cells are incubated with increasing concentrations of IMD-0354 or STI571 for 24, 48, and 72 hours, and numbers and viability of cells are determined by a dye exclusion test and an MTT assay. IMD-0354 suppresses cell proliferation in a time- and dose-dependent manner. The inhibitory effect of IMD-0354 is remarkable, even at lower concentrations, when compared with that of STI571[1]. IMD0354 inhibits TNF-α induced NF-κB transcription activity with an IC 50 of 1.2±0.3 uM[2]. |