BIX 02188
BIX 02188 is a selective inhibitor of MEK5 with IC50 value of 4.3 nM 1.
BIX 02188 belongs to the indolinone kinase inhibitor series. It selectively inhibited the catalytic activity of MEK5 but not other closely related kinases such as MEK1, MEK2, ERK2 and JNK2. BIX 02188 also inhibited ERK5 with IC50 value of 810 nM. In HeLa cells, treatment of BIX 02188 inhibited the phosphorylation of ERK5 but not ERK1/2. Besides that, BIX 02188 prevented the transcription of the downstream substrate MEF2C in HeLa and HEK293 cells. When tested with a panel of 79 kinases, BIX 02188 showed some degree of inhibition of the kinases CSF1R, KIT and LCK with IC50 values of 280 nM, 550 nM and 390 nM, respectively 1.
References:
1. Tatake R J, O’Neill M M, Kennedy C A, et al. Identification of pharmacological inhibitors of the MEK5/ERK5 pathway. Biochemical and biophysical research communications, 2008, 377(1): 120-125.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 412.48 |
| Cas No. | 1094614-84-2 |
| Formula | C25H24N4O2 |
| Solubility | insoluble in H2O; insoluble in EtOH; ≥10.3 mg/mL in DMSO |
| Chemical Name | (3E)-3-[[3-[(dimethylamino)methyl]anilino]-phenylmethylidene]-2-oxo-1H-indole-6-carboxamide |
| SDF | Download SDF |
| Canonical SMILES | CN(C)CC1=CC(=CC=C1)NC(=C2C3=C(C=C(C=C3)C(=O)N)NC2=O)C4=CC=CC=C4 |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Description | BIX02188 is a selective inhibitor of MEK5 with an IC50 value of 4.3 nM. | |||||
| Targets | MEK5 | ERK5 | TGFβR1 | |||
| IC50 | 4.3 nM | 810 nM | 1.8 μM | |||
Quality Control & MSDS
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Chemical structure
