| Identification | Back Directory | [Name]
(3Z)-3-[[[3-[(Dimethylamino)methyl]phenyl]amino]phenylmethylene]-2,3-dihydro-2-oxo-1H-indole-6-carboxamide | [CAS]
334949-59-6 | [Synonyms]
(3Z)-3-[[[3-[(Dimethylamino)methyl]phenyl]amino]phenylmethylene]-2,3-dihydro-2-oxo-1H-indole-6-carboxamide
1H-Indole-6-carboxamide, 3-[[[3-[(dimethylamino)methyl]phenyl]amino]phenylmethylene]-2,3-dihydro-2-oxo-, (3Z)- | [Molecular Formula]
C25H24N4O2 | [MDL Number]
MFCD18157583 | [MOL File]
334949-59-6.mol | [Molecular Weight]
412.48 |
| Chemical Properties | Back Directory | [Boiling point ]
615.8±55.0 °C(Predicted) | [density ]
1.283 | [storage temp. ]
Sealed in dry,Store in freezer, under -20°C | [solubility ]
DMSO:32.5(Max Conc. mg/mL);78.79(Max Conc. mM)
DMSO:PBS (pH 7.2) (1:1):0.5(Max Conc. mg/mL);1.21(Max Conc. mM)
DMF:20.0(Max Conc. mg/mL);48.49(Max Conc. mM) | [form ]
A crystalline solid | [pka]
11.18±0.20(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Uses]
BIX02188 is a potent MEK5-selective inhibitor with an IC50 of 4.3 nM. BIX02188 inhibits ERK5 catalytic activity, with an IC50 of 810 nM. | [IC 50]
MEK5: 4.3 nM (IC50); ERK5: 810 nM (IC50); CSF1R (FMS): 280 nM (IC50); LCK: 390 nM (IC50); KIT: 550 nM (IC50); TGFβR1: 1.8 μM (IC50); ABL1: 2.1 μM (IC50); RPS6KA6 (RSK4): 3.2 μM (IC50); RPS6KA3 (RSK2): 4.1 μM (IC50); MAPK14 (p38 alpha): 3.9 μM (IC50); JAK3: 7.8 μM (IC50); SRC: 8.9 μM (IC50) | [References]
[1] Li L, et al. Fluid shear stress inhibits TNF-mediated JNK activation via MEK5-BMK1 in endothelial cells. Biochem Biophys Res Commun. 2008 May 23;370(1):159-63. DOI:10.1016/j.bbrc.2008.03.051
[2] Badshah II, et al. Erk5 is a mediator to TGFβ1-induced loss of phenotype and function in human podocytes. Front Pharmacol. 2014 Apr 21;5:71. DOI:10.3389/fphar.2014.00071
[3] Tatake RJ, et al. Identification of pharmacological inhibitors of the MEK5/ERK5 pathway. Biochem Biophys Res Commun. 2008 Dec 5;377(1):120-5. DOI:10.1016/j.bbrc.2008.09.087 |
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