MK2 Inhibitor IV (Synonyms: MK 25) |
Katalog-Nr.GC16723
One-Click Copy Product Info
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MK2 Inhibitor IV ist ein potenter und selektiver MAPKAPK2(MK2)-Inhibitor (IC50=0,11 uM) mit einem nicht-ATP-kompetitiven Bindungsmodus.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1314118-94-9
Sample solution is provided at 25 µL, 10mM.
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MK2 Inhibitor IV is a highly selective and non-ATP competitive MK2 inhibitor with IC50 value of 0.11 μM [1].
MAP kinase-activated protein kinase 2 (MAPKAPK2 or MK2) is a member of the Ser/Thr protein kinase family and regulated through direct phosphorylation by p38 MAP kinase. Activation of the p38/MK2 pathway involved in promoting pro-inflammatory cytokine production and related inflammatory diseases [1].
MK2 Inhibitor IV is a highly selective and non-ATP competitive MK2 inhibitor. In a broad panel of 150 protein kinases, MK2 Inhibitor IV only significantly inhibited CK1γ3 at greater than 50%. MK2 Inhibitor IV also demonstrated no inhibition against a panel of cytochrome P450 (CYP) enzymes up to 30 μM. In the human THP1 acute monocytic leukemia cell line, MK2 Inhibitor IV inhibited pro-inflammatory cytokine secretion. MK2 Inhibitor IV also dose-dependently inhibited LPS-stimulated TNFα and IL6 secretion with IC50 values of 4.4 μM and 5.2 μM, respectively. In the SW1353 chondrosarcoma cell line and human primary chondrocyte cultures, MK2 Inhibitor IV dose dependently inhibited IL1β-stimulated matrixmetalloprotease (MMP)13 secretion with IC50 values of 5.7 μM and 2.2 μM, respectively.
Reference:
[1]. Huang X, Shipps GW Jr, Cheng CC, et al. Discovery and Hit-to-Lead Optimization of Non-ATP Competitive MK2 (MAPKAPK2) Inhibitors. ACS Med Chem Lett. 2011 Jun 24;2(8):632-7.
| Cas No. | 1314118-94-9 | SDF | |
| Überlieferungen | MK 25 | ||
| Chemical Name | 5-(4-chlorophenyl)-N-[4-(1-piperazinyl)phenyl]-N-(2-pyridinylmethyl)-2-furancarboxamide, monohydrochloride | ||
| Canonical SMILES | O=C(N(C1=CC=C(N2CCNCC2)C=C1)CC3=NC=CC=C3)C4=CC=C(C5=CC=C(Cl)C=C5)O4.Cl | ||
| Formula | C27H25ClN4O2 • HCl | M.Wt | 509.4 |
| Löslichkeit | <5.09mg/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 | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.9631 mL | 9.8155 mL | 19.6309 mL |
| 5 mM | 392.6 μL | 1.9631 mL | 3.9262 mL |
| 10 mM | 196.3 μL | 981.5 μL | 1.9631 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
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.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 18 reference(s) in Google Scholar.)