[CAS NO. 724711-21-1] MK2-IN-3
PRODUCTS SPECIFICATIONS [724711-21-1]
DESCRIPTION [724711-21-1]
Overview
| MDL | MFCD16293712 |
|---|---|
| Molecular Weight | 340.38 |
| Molecular Formula | C21H16N4O |
| SMILES | O=C1C2=C(NC(C3=CC(C4=CC5=CC=CC=C5N=C4)=NC=C3)=C2)CCN1 |
Summary
MK2-IN-3 is a potent and selective inhibitor of MAPKAP-K2 (MK-2) , with an IC 50 of 8.5 nM. MK2-IN-3 shows selectivity for MK-2 over MK-3, MK-5, ERK2 , MNK1 , p38a (IC 50 s=0.21, 0.081, 3.44, 5.7, and >100 μM, respectively) and MSK1, MSK2, CDK2 , JNK2 , IKK2 (IC 50 s>200 μM). MK2-IN-3 can reduce TNFα production in both U937 cells and in vivo [1] .
IC50 & Target
IC50: 8.5 nM (MK-2); 81 nM (MK-5); 210 nM (MK-3); 3.44 μM (ERK2); 5.7 μM (MNK1) [1]
In Vitro
MK2-IN-3 (compound 16) inhibits MK-2 and TNFα production in U937 cells, with IC 50 s of 8.5 nM and 4.4 μM, respectively [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MK2-IN-3 (compound 16) (20 mg/kg; a single p.o. before LPS challenge) inhibits 20% TNFα production in rat LPS (rLPS) model [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvent & Solubility
DMSO : 62.5 mg/mL ( 183.62 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.9379 mL | 14.6895 mL | 29.3789 mL |
| 5 mM | 0.5876 mL | 2.9379 mL | 5.8758 mL |
| 10 mM | 0.2938 mL | 1.4689 mL | 2.9379 mL |