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Ralimetinib dimesylate (LY2228820 dimesylate) is a novel and potent p38MAPK inhibitor. In vitro kinase enzyme activity showed that the IC50 for p38αMAPK and p38βMAPK of LY2228820 were 7 nM and 3 nM, respectively. Phosphorylation of MAPKAPK2 and/or HSP27, down stream targets of p38MAPK, was significantly inhibited by LY in both MM cell lines and LT-BMSCs.
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Source | Oncotarget (2016). Figure 3. LY2228820 |
| Method | colony assays | |
| Cell Lines | MDA-MB-231 cells | |
| Concentrations | 10 μM | |
| Incubation Time | 72 h | |
| Results | The triple combination significantly retarded shortterm proliferation of MDA-MB-231 cells compared to vehicle and single drug controls (p<0.001), as well as the two-agent combinations |
| Molecular Weight | 612.74 |
| Formula | C24H29FN6.2CH4O3S |
| CAS Number | 862507-23-1 |
| Solubility (25°C) | DMSO 30 mg/mL Water 33 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| 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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