1. NF-κB
  2. IKK
  3. IMD-0354

IMD-0354 (Synonyms: IKK2 Inhibitor V)

Cat. No.: HY-10172 Purity: 99.46%
Handling Instructions

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.

For research use only. We do not sell to patients.

IMD-0354 Chemical Structure

IMD-0354 Chemical Structure

CAS No. : 978-62-1

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 86 In-stock
Estimated Time of Arrival: December 31
5 mg USD 78 In-stock
Estimated Time of Arrival: December 31
10 mg USD 114 In-stock
Estimated Time of Arrival: December 31
50 mg USD 264 In-stock
Estimated Time of Arrival: December 31
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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

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.

IC50 & Target[1][2]

IKKβ

 

NF-κB

1.2 μM (IC50)

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].

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].

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (260.64 mM)

H2O : < 0.1 mg/mL (insoluble)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (6.52 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.5 mg/mL (6.52 mM); Suspended solution; Need ultrasonic

*All of the co-solvents are provided by MCE.
References
Cell Assay
[1]

HMC-1 cells (2×105 cells/mL) are incubated with various concentrations of IMD-0354 (0.1, 0.5, 1, 5 and 10 uM), STI571, or pyrrolidine dithiocarbamate (PDTC) for the indicated hours, and viable cell numbers are calculated with the use of the trypan blue dye exclusion test at each time point. Cells (2×105 cells/mL) are incubated in phenol red free α-MEM containing 10% FCS (for HMC-1 and IC-2 cells) or 5% FCS (for CBhCMCs), and antibiotics with or without various concentrations of IMD-0354 (0.1, 0.5, 1, 5 and 10 uM), STI571, or PDTC. IC-2WT cells and CBhCMCs are incubated in the presence of 100 ng/mL recombinant rat or recombinant human SCF. One hundred microliters of cell suspension is applied to each well of 96-well culture plates and are incubated for 24, 48, and 72 hours. Before 4 hours from the end of the culture, 10 μL of 5 mg/mL MTT dissolved in PBS is added to each well. The reaction is stopped with the addition of 100 μLof 10% SDS in 0.01 N HCl. Absorbance is measured at 577 nm with ImmunoMini NJ-2300[1].

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

Animal Administration
[3][4]

Mice[3]
MDA-MB-231 cells are suspended in PBS (5×106 cells/100 μL mouse) and s.c. injected to the back of female BALB/c nude mice at the age of 4 to 5 weeks. After growth, the tumor is removed surgically and 100 mg of each established tumor is transplanted to the back of other female nude mice at the age of 4 weeks under ether anesthesia. IMD-0354 is suspended in saline and 5 mg/kg body weight IMD-0354 (suspended in 100 μL/mouse) is given to each mouse by i.p. injection once a day for 28 days after the implantation. Saline is injected in nude mice as a control. Estimated tumor volume (mm3) and tumor weight (mg) are calculated.
Rats[4]
Eight-week-old male Lewis rats (180-220 g) are used. Endotoxin-induced uveitis (EIU) is induced with subcutaneous injection with 200 μg LPS from Escherichia coli that has been diluted in 200 μL PBS. At the same time, the rats are injected intraperitoneally with 30, 10, or 3 mg/kg of IMD-0354, diluted in 500 μL of 0.5% CMC. Control EIU rats are intraperitoneally administered 500 μL of CMC alone. Naïve rats are used as controls. All experiments are performed in triplicate with five animals in each group.

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

References
Molecular Weight

383.67

Formula

C₁₅H₈ClF₆NO₂

CAS No.

978-62-1

SMILES

O=C(NC1=CC(C(F)(F)F)=CC(C(F)(F)F)=C1)C2=CC(Cl)=CC=C2O

Shipping

Room temperature in continental US; may vary elsewhere

Purity: 99.46%

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Product Name:
IMD-0354
Cat. No.:
HY-10172
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IMD-0354

Cat. No.: HY-10172