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TAK-715 is a p38 MAPK inhibitor for p38α with IC50 of 7.1 nM, 28-fold more selective for p38α over p38β, no inhibition to p38γ/δ, JNK1, ERK1, IKKβ, MEKK1 or TAK1.
| Cell Experiment | |
|---|---|
| Cell lines | HMC-1 |
| Preparation method | In the first part of the study, qPCR was employed to evaluate the expression of inflammatory mediators in HMC-1 cells treated with EXs-CSU-R or EXs-CSU-S. In the second part of the study, qPCR was used to evaluate the effects of MAPK, TLR2, and TLR4 inhibitors on the production of inflammatory mediators in HMC-1 cells induced by EXs-CSU-S and EXs-CSU-R. The concentrations of tryptase-1, histamine, IL-6, TNF-α, VEGF, CXCL-1, CXCL-5, and CCl-2 in the supernatants of HMC-1 cells incubated with EXs-CSU-S and EXs-CSU-R as well as the concentrations of mediators in 40 μg EXs were measured using ELISA kits according to the manufacturer’s instructions. Mediator concentrations were expressed as relative values normalized to those of the control group. |
| Concentrations | 5 μM |
| Incubation time | 8 h |
| Animal Experiment | |
|---|---|
| Animal models | Adjuvant-induced arthritis (AA) rat model |
| Formulation | Saline |
| Dosages | 30 mg/kg |
| Administration | Orally |
| Molecular Weight | 399.51 |
| Formula | C24H21N3OS |
| CAS Number | 303162-79-0 |
| Solubility (25°C) | DMSO 70 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[2] D Falck, et al. Tandem mass spectrometry study of p38α kinase inhibitors and related substances
| Related p38 MAPK Products |
|---|
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BIRB 796 (Doramapimod) is a protein kinase inhibitor of p38 MAPK with Kd of 100pM. |
| Selonsertib
GS-4997 is a highly selective and potent once-daily oral ASK1 inhibitor with potential anti-inflammatory, antineoplastic and anti-fibrotic activities. |
| Adezmapimod
Adezmapimod (SB203580) is a P38 MAPK inhibitor with an IC50 of 0.3-0.5 μM, which is 10 times less selective than SAPK3(106T) and SAPK4(106T), and inhibits PKB phosphorylation with an IC50 of 3-5 μM. |
| SB 202190
SB 202190 is a highly selective, potent and cell permeable inhibitor of p38 MAP kinase with IC50 values of 50 and 100 nM inhibiting p38α and p38β, respectively. |
| PH-797804
PH-797804 is a highly selective and potent inhibitor of p38 MAP kinase with IC50 of 26 nM. |
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