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Purity: ≥98%
IMD-0354 (IMD0354; IMD-0354) is a novel, potent and selective IKKβ inhibitor with potential anti-inflammatory activity. It prevents the NFκB (nuclear factor-kappaB) pathway from phosphorylating IκBα. Atopic dermatitis may benefit from treatment with IMD-0354. IMD-0354 (< 5 μM), inhibited NF-κB translocation to the nucleus and downregulated NF-κB expression in HMC-1 cells. IMD-0354 inhibited cell proliferation in a time- and dose-dependent manner, according to research done on HMC-1 cells. Additionally, it was noted that IMD-0354 reduced the proportion of HMC-1 cells in the S and G2/M phases and stopped the cell cycle at the G0/G1 phase.
| Targets |
NF-κB (IC50 = 1.2 μM)
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| ln Vitro |
IMD-0354 completely suppresses the growth factor-independent proliferation of mast cells in HMC-1 cells by impairing NF-κB activity. Cell proliferation is completely suppressed when the DNA-binding activity of NF-κB is inhibited by treatment with IMD-0354. IMD-0354 or STI571 are added to HMC-1 cells in escalating concentrations for 24, 48, and 72 hours; the number of cells and their viability are then assessed using the dye exclusion test and the MTT assay. Cell proliferation is inhibited by IMD-0354 in a time- and dose-dependent manner. When compared to STI571, IMD-0354 has a remarkable inhibitory effect, even at lower concentrations[1]. IMD0354 has an IC50 of 1.2±0.3 uM and inhibits TNF-αinduced NF-κB transcription activity[2].
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| ln Vivo |
In nude mice implanted with MDA-MB-231 tumors, a daily dose of 5 mg/kg IMD-0354 significantly inhibits tumor growth. Tumor progression is slowed down in mice receiving IMD-0354 treatment[3]. In rats treated with 30, 10, 3, or 0 mg/kg of IMD-0354, the number of infiltrating cells in the aqueous humor was 53.6±9.8×105, 72.5±17.0×105, 127.25±32.0×105, and 132.0±25.0×105 cells/mL, respectively. Rats treated with 30, 10, 3, and 0 mg/kg of IMD-0354, respectively, had total protein concentrations of 92.6±3.1 mg/mL, 101.5±6.8 mg/mL, 112.6±1.9 mg/mL, and 117.331.8 mg/mL in their aqueous humor[4].
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| Enzyme Assay |
IMD0354 inhibits TNF-α induced NF-κB transcription activity with an IC50 of 1.2±0.3 uM.
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| Cell Assay |
For the indicated hours, HMC-1 cells (2×105 cells/mL) are incubated with varying concentrations of IMD-0354 (0.1, 0.5, 1, 5, and 10 uM), STI571, or pyrrolidine dithiocarbamate (PDTC), and viable cell counts are determined using the trypan blue dye exclusion test at each time point. Cells (2×105 cells/mL) are incubated in phenol red-free -MEM containing 10% FCS (for HMC-1 and IC-2 cells) or 5% FCS (for CBhCMCs), antibiotics with or without varying concentrations of IMD-0354 (0.1, 0.5, 1, 5, and 10 uM), STI571, or PDTC. Recombinant rat or recombinant human SCF, 100 ng/mL, is added to the medium and is incubated with IC-2WT cells and CBhCMCs. Each well of 96-well culture plates receives 100 microliters of cell suspension, which is then left there for 24, 48, and 72 hours of incubation. 10 μL of 5 mg/mL MTT dissolved in PBS are added to each well prior to 4 hours from the culture's end. Once 100 L of 10% SDS in 0.01 N HCl are added, the reaction is stopped. ImmunoMini NJ-2300[1] is used to measure absorbance at 577 nm.
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| Animal Protocol |
Mice: Female BALB/c nude mice are injected s.c. with MDA-MB-231 cells suspended in PBS (5×106 cells/100 L mouse) when they are 4 to 5 weeks old. Following growth, the tumor is surgically removed, and at the age of 4 weeks, under ether anesthesia, 100 mg of each established tumor is transplanted to the back of additional female nude mice. Each mouse receives an intraperitoneal injection of 5 mg/kg body weight of IMD-0354 (suspended in 100 L/mouse) once daily for 28 days following the implantation. As a control, saline is injected into naked mice. Calculations are made for the estimated tumor weight (mg) and volume (mm3).
Rats: Lewis rats (180–220 g) that are eight weeks old are used. Endotoxin-induced uveitis (EIU) is brought on by injecting 200 μg of diluted Escherichia coli LPS in 200 l of PBS subcutaneously. IMD-0354, diluted in 500 μL of 0.5% CMC, is injected intraperitoneally into the rats at the same time in doses of 30, 10, or 3. 500 μL of CMC alone is intraperitoneally administered to control EIU rats. Control rats are naive rats. Five animals are used in each group for each experiment, which is carried out in triplicate. |
| References |
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| Molecular Formula |
C15H8CLF6NO2
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| Molecular Weight |
383.67
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| Exact Mass |
383.01
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| Elemental Analysis |
C, 46.96; H, 2.10; Cl, 9.24; F, 29.71; N, 3.65; O, 8.34
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| CAS # |
978-62-1
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| Appearance |
Solid powder
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| SMILES |
C1=CC(=C(C=C1Cl)C(=O)NC2=CC(=CC(=C2)C(F)(F)F)C(F)(F)F)O
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| InChi Key |
CHILCFMQWMQVAL-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H8ClF6NO2/c16-9-1-2-12(24)11(6-9)13(25)23-10-4-7(14(17,18)19)3-8(5-10)15(20,21)22/h1-6,24H,(H,23,25)
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| Chemical Name |
N-[3,5-bis(trifluoromethyl)phenyl]-5-chloro-2-hydroxybenzamide
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| Synonyms |
IKK2 Inhibitor V; IMD0354; IMD 0354; IMD-0354
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6064 mL | 13.0320 mL | 26.0641 mL | |
| 5 mM | 0.5213 mL | 2.6064 mL | 5.2128 mL | |
| 10 mM | 0.2606 mL | 1.3032 mL | 2.6064 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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