| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
IKKβ-IN-5 (compound LP46) (0-2 μM, 48 hours) exhibited potent antiproliferative activity in RKO and HCT116 cells and low toxicity in NCM460 cells [1]. IKKβ-IN-5 (0.75-3.0 μM, 48 hours) affected IKKβ phosphorylation and the protein expression of its downstream target IκBα in RKO and HCT116 cells by directly inhibiting IKKβ phosphorylation [1]. IKKβ-IN-5 (0.75-3.0 μM, 7 days) had a long-term antiproliferative effect in RKO and HCT116 cells [1]. IKKβ-IN-5 (0.75-3.0 μM, 48 hours) exerts its antiproliferative effect through a dual mechanism (including inducing G2/M phase cell cycle arrest and activating autophagy) even in the presence of inflammatory stimulation, and can block NF-κB pathway activation, thereby inhibiting downstream inflammatory responses in RKO and HCT116 cells [1]. IKKβ-IN-5 (3 μM, 48 hours) can directly counteract the IKKβ-mediated pro-inflammatory and anti-autophagy effects in IKKβ knockdown or overexpression colorectal cancer cells [1].
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: HCT116, RKO, and NCM460 cells Tested Concentrations: 0, 0.4 0.8, 1.2, 1.6 and 2.0 μM Incubation Duration: 48 h Experimental Results: Exhibited potent inhibitory activity, with IC50 values of 3.94 μM for RKO and 2.59 μM for HCT116. Showed significantly lower toxicity in NCM460 cells, with an IC50 of 21.25 μM. Western Blot Analysis[1] Cell Types: RKO and HCT116 cells Tested Concentrations: 0.75, 1.5, and 3 μM Incubation Duration: 48 h Experimental Results: Significantly reduced phosphorylation of both IKKβ and IκBα in a dose-dependent manner. Induced greater inhibition of IKKβ phosphorylation. Had no significant impact on either the expression or phosphorylation of TAK1 or MAP3K1. Cell Proliferation Assay[1] Cell Types: RKO and HCT116 cells Tested Concentrations: 0.75, 1.5, and 3 μM Incubation Duration: 7 days Experimental Results: Observed Dose-dependent suppression of colony formation. Demonstrated superior efficacy at the highest dose. Cell Cycle Analysis[1] Cell Types: RKO and HCT116 cells Tested Concentrations: 0.75, 1.5, and 3 μM Incubation Duration: 48 h Experimental Results: Revealed a significant accumulation of RKO and HCT116 cells in the G2/M phase. Cell Proliferation Assay[1] Cell Types: RKO and HCT116 cells Tested Concentrations: 0.75, 1.5, and 3 μM Incubation Duration: 48 h Experimental Results: Significantly inhibited DNA synthesis in both RKO and HCT116 cells. Western Blot Analysis[1] Cell Types: RKO and HCT116 cells Tested Concentrations: 0.75, 1.5, and 3 μM Incubation Duration: 48 h Experimental Results: Dose-dependently increased expression levels of key autophagy-related markers, Beclin1 and LC3A/B both markers in RKO and HCT116 cells. Enhanced expression of Beclin1 and LC3A/ B in these cells in RKO and HCT116 cells with TNF-α. Reduced p65 expression and inhibited its nuclear translocation in a dose-dependent manner. RT-PCR[1] Cell Types: RKO and HCT116 cells Tested Concentrations: 0.75, 1.5, and 3 μM Incubation Duration: 48 h Experimental Results: Significantly down regulated the expression of TNF-α, IL-6, and IL-1β in a dose dependent manner. Western Blot Analysis[1] Cell Types: IKKβ knockdown CRC cells or IKKβ overexpression CRC cells Tested Concentrations: 3 μM Incubation Duration: 48 h Experimental Results: Reduced the phosphorylation levels of both IκBα and p65, while concurrently increasing the expression of key autophagy markers, Beclin1 and LC3A/B and exhibited superior efficacy in inhibiting IKKβ phosphorylation and suppressing NF-κB signaling upon TNF-α stimulation in IKKβ knockdown cells. Increased p-IκBα and p-p65 levels and reduced Beclin1 and LC3A/B expression upon TNF-α stimulation in overexpression of IKKβ cells. Decreased NF-κB phosphorylation and restoration of autophagy-related protein levels, even under TNF-α stimulation and IKKβ-overexpressing conditions. Cell Viability Assay[1] Cell Types: HCT116, RKO, and NCM460 cells Tested Concentrations: 0, 0.4 0.8, 1.2, 1.6 and 2.0 μM Incubation Duration: 48 h Experimental Results: Exhibited potent inhibitory activity, with IC50 values of 3.94 μM for RKO and 2.59 μM for HCT116. Showed significantly lower toxicity in NCM460 cells, with an IC50 of 21.25 μM. |
| References |
| Molecular Formula |
C23H24FN7
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|---|---|
| Molecular Weight |
417.48
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| Appearance |
Typically exists as solids at room temperature
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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 |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3953 mL | 11.9766 mL | 23.9532 mL | |
| 5 mM | 0.4791 mL | 2.3953 mL | 4.7906 mL | |
| 10 mM | 0.2395 mL | 1.1977 mL | 2.3953 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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