- PD184352 (CI-1040)
- Cobimetinib (R-enantiomer)
- Cobimetinib
- BIX 02189
- XMD8-92
- Cobimetinib (racemate)
| BIX 02188MEK5 inhibitor,potent and selective |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
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- Purity = 97.37%
- COA (Certificate Of Analysis)
- HPLC
- NMR (Nuclear Magnetic Resonance)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure
| 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 | |||
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| Cas No. | 1094614-84-2 | SDF | Download SDF |
| Chemical Name | (3E)-3-[[3-[(dimethylamino)methyl]anilino]-phenylmethylidene]-2-oxo-1H-indole-6-carboxamide | ||
| Canonical SMILES | CN(C)CC1=CC(=CC=C1)NC(=C2C3=C(C=C(C=C3)C(=O)N)NC2=O)C4=CC=CC=C4 | ||
| Formula | C25H24N4O2 | M.Wt | 412.48 |
| Solubility | ≥10.3mg/mL in DMSO | Storage | Store at -20°C |
| Physical Appearance | A solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
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.
