| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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Purity: ≥98%
MK2-IN-1 HCl is a novel, potent, non-ATP competitive and selecitve MAPKAPK2(MK2) inhibitor(IC50=0.11 uM). By screening against a large panel of 150 protein kinases at a concentration of 10 μM, MK2-IN-1 was profiled for kinase selectivity, and only CK1γ3 was significantly inhibited at levels higher than 50%. The human THP1 acute monocytic leukemia cell line secreted pro-inflammatory cytokines less frequently as a result of MK2-IN-1, which led to a dose-dependent reduction in TNFα and IL6 production. The secretion of matrixmetalloprotease (MMP)13 from the SW1353 chondrosarcoma cell line and primary human chondrocyte cultures was also inhibited by MK2-IN-1 in a dose-dependent manner. Notably, given its high level of selectivity, our data imply that MK2-IN-1 may be an excellent pharmacologic tool for specifically exploring and validating MK2 biology.
| Targets |
MK2 (IC50 = 0.11 μM)
|
|---|---|
| ln Vitro |
Addition of the MK2 inhibitor MK2-IN-1 induced more alkaline phosphatase (AP)-positive colonies than the other factors in a short time , implying that MK2 may be responsible for the phosphorylation of Tfcp2l1.[2]
46C mESCs were treated with MK2-IN-1 for a period of time. The Tfcp2l1 protein level gradually increased without a change in the Tfcp2l1 transcript level within 2 h .[2] |
| References |
| Molecular Formula |
C27H26CL2N4O2
|
|---|---|
| Molecular Weight |
509.43
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| Exact Mass |
508.143
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| CAS # |
1314118-94-9
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| Related CAS # |
MK2-IN-1;1314118-92-7
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| PubChem CID |
70681199
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| Appearance |
Light yellow to pink solid
|
| LogP |
6.447
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| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
6
|
| Heavy Atom Count |
35
|
| Complexity |
645
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
ClC1C=CC(=CC=1)C1=CC=C(C(N(CC2C=CC=CN=2)C2C=CC(=CC=2)N2CCNCC2)=O)O1.Cl
|
| InChi Key |
AZDOSXSDARWKGX-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C27H25ClN4O2.ClH/c28-21-6-4-20(5-7-21)25-12-13-26(34-25)27(33)32(19-22-3-1-2-14-30-22)24-10-8-23(9-11-24)31-17-15-29-16-18-31;/h1-14,29H,15-19H2;1H
|
| Chemical Name |
5-(4-chlorophenyl)-N-(4-piperazin-1-ylphenyl)-N-(pyridin-2-ylmethyl)furan-2-carboxamide;hydrochloride
|
| Synonyms |
MK2-IN-1; MK2-IN 1; MK2 IN-1; MK25; MK-25; MK 25; MK2 Inhibitor IV; MK2 Inhibitor-IV
|
| 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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO: ~100 mg/mL (~196.3 mM)
Ethanol: ~2 mg/mL (~3.9 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.67 mg/mL (3.28 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 16.7 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1.67 mg/mL (3.28 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 16.7 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 1.67 mg/mL (3.28 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9630 mL | 9.8149 mL | 19.6298 mL | |
| 5 mM | 0.3926 mL | 1.9630 mL | 3.9260 mL | |
| 10 mM | 0.1963 mL | 0.9815 mL | 1.9630 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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