IKK-16 (hydrochloride) (Synonyms: IKK Inhibitor VII) |
| カタログ番号GC12370 |
IKK-16 (塩酸塩) は、IKK2、IKK 複合体、および IKK1 に対する選択的 IκB キナーゼ (IKK) 阻害剤であり、IC50 はそれぞれ 40 nM、70 nM、および 200 nM です。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1186195-62-9
Sample solution is provided at 25 µL, 10mM.
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IC50: 200, 40, and 70 nM for IKKα, IKKβ, and IKK complex, respectively.
IKK-16 is an IκB kinases (IKKs) inhibitor.
The IκB kinase (IKK), part of a high molecular weight protein complex consisting of three subunits, IKK1, IKK2, and IKKc, emerged as a prime target for the development of novel anti-rheumatic and anti-inflammatory drugs.
In vitro: In screening study, it was found that compounds with an additional basic amino group were more active than the neutral inhibitors. The tertiary amines, such as IKK-16, was active in the low-nanomolar range. IKK-16 could inhibit TNFa-induced adhesion molecule expression in a potency range similar to the IjBa degradation. Although IKK-16 showed activity in the IFNc-induced expression of b2 microglobulin, its potency was weaker. These data demonstrated that IKK-16 had an effect on downstream gene expression, however, on the cellular level the selectivity was modest [1].
In vivo: Animal study found that the treatment with IKK 16 to mice could attenuate the impairment in systolic contractility, renal dysfunction, hepatocellular injury and lung inflammation in LPS/PepG-induced MOD and in polymicrobial sepsis. IKK-16 treatment could also significantly attenuated the increase in inducible nitric oxide synthase (iNOS) expression and increase the phosphorylation of Akt and endothelial nitric oxide synthase [2].
Clinical trial: So far, no clinical study has been conducted.
References:
[1] Waelchli, R. ,Bollbuck, B.,Bruns, C., et al. Design and preparation of 2-benzamido-pyrimidines as inhibitors of IKK. Bioorganic & Medicinal Chemistry Letters 16(1), 108-112 (2006).
[2] Coldewey, S. M.,Rogazzo, M.,Collino, M., et al. Inhibition of I k B kinase reduces the multiple organ dysfunction caused by sepsis in the mouse. Dis.Model Mech. 6, 1031-1042 (2013).
| Cas No. | 1186195-62-9 | SDF | |
| 同義語 | IKK Inhibitor VII | ||
| Chemical Name | [4-[(4-benzo[b]thien-2-yl-2-pyrimidinyl)amino]phenyl][4-(1-pyrrolidinyl)-1-piperidinyl]-methanone, monohydrochloride | ||
| Canonical SMILES | O=C(N1CCC(N2CCCC2)CC1)C3=CC=C(C=C3)NC4=NC=CC(C5=CC(C=CC=C6)=C6S5)=N4.Cl | ||
| Formula | C28H29N5OS • HCl | M.Wt | 520.1 |
| 溶解度 | ≤10mg/ml in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.9227 mL | 9.6135 mL | 19.2271 mL |
| 5 mM | 0.3845 mL | 1.9227 mL | 3.8454 mL |
| 10 mM | 0.1923 mL | 0.9614 mL | 1.9227 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 39 reference(s) in Google Scholar.)
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