BIX02188

Modify Date: 2024-01-30 23:39:24

BIX02188 structure	Common Name	BIX02188
	CAS Number	334949-59-6	Molecular Weight	412.484
	Density	1.3±0.1 g/cm3	Boiling Point	615.8±55.0 °C at 760 mmHg
	Molecular Formula	C₂₅H₂₄N₄O₂	Melting Point	N/A
	MSDS	N/A	Flash Point	326.2±31.5 °C

Use of BIX02188

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.

Name	(3Z)-3-[({3-[(Dimethylamino)methyl]phenyl}amino)(phenyl)methylene]-2-oxo-6-indolinecarboxamide
Synonym	More Synonyms

Description	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.
Related Catalog	Signaling Pathways >> MAPK/ERK Pathway >> ERK Signaling Pathways >> Stem Cell/Wnt >> ERK Signaling Pathways >> MAPK/ERK Pathway >> MEK Research Areas >> Cancer
Target	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)
In Vitro	BIX02188 is a potent inhibitor of catalytic function of purified, active MEK5 enzyme. In activated HeLa cells, BIX02188 blocks phosphorylation of ERK5, without affecting phosphorylation of ERK1/2, JNK and p38 MAP kinases. To characterize the effects of BIX02188 in cultured endothelial cells (EC), H2O2 is used to activate BMK1. Bovine lung microvascular endothelial cells (BLMECs) are pretreated with 0.1-10 μM BIX02188 for 30 min, and then stimulated with 300 μM H2O2. BMK1 is dramatically activated by H2O2, with peak at 20 min. Phosphorylated BMK1 is inhibited by BIX02188 in a dose-dependent manner, with an IC50=0.8±1.0 μM, and maximal inhibition at concentrations >3 μM. To examine the specificity of BIX02188, The effect of 0.1-10 μM BIX02188 is measured on the activity of ERK1/2 and JNK. There is no significant inhibition of ERK1/2 and JNK at these concentrations. These observations confirm the selectivity of BIX02188 for MEK5-induced BMK1 phosphorylation[1]. BIX02188 inhibits MEK5 and ERK5 activity, with IC50s of 4.3 nM and 810 nM, respectively. BIX02188 does not inhibit closely related kinases MEK1, MEK2, ERK2, and JNK2. BIX02188 inhibits ERK5 phosphorylation in a dose dependent manner[2]. To assess the proliferation of podocytes in response to the pro-fibrotic stimulus of TGFβ1, podocytes are pre-incubated in the presence and absence of BIX02188 (10 μM) for 60 min after which cells are co-treated with TGFβ1 (2.5 ng/mL) for 48 h to provide adequate time for proliferation to occur and a colorimetric cell proliferation assay is employed where metabolic activity is directly proportional to cell number. Inhibition of Erk5 activation with BIX02188 incubation reduces podocyte cell number. TGFβ1 stimulation increases podocyte cell number which is prevented following BIX02188 co-treatment[3].
Cell Assay	Human podocyte cell lines are treated at 37°C with the growth factor TGFβ1 (2.5 ng/mL in serum-free media containing BSA (0.1% w/v)). Inhibitors are applied at 37°C in serum-free media. To diminish Erk5 activation the upstream activator Mek5 is chemically inhibited by BIX02188 (10 μM) with an additional 60 min pre-incubation. TGFβ1-mediated signaling is stopped with SB431542 (10 μM), targeting the type I TGFβ receptor Alk5, with a further 30 min pre-incubation. Transmembrane receptor-induced Ras function is prevented with an additional 30 min pre-incubation using farnesylthiosalicylic acid (FTS; 10 μM). Controls (vehicles) are treated with serum-free media containing DMSO (0.1% v/v) and BSA (0.1% w/v)[3].
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. [2]. Tatake RJ, et al. Identification of pharmacological inhibitors of the MEK5/ERK5 pathway. Biochem Biophys Res Commun. 2008 Dec 5;377(1):120-5. [3]. 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.

Density	1.3±0.1 g/cm3
Boiling Point	615.8±55.0 °C at 760 mmHg
Molecular Formula	C₂₅H₂₄N₄O₂
Molecular Weight	412.484
Flash Point	326.2±31.5 °C
Exact Mass	412.189911
LogP	2.36
Vapour Pressure	0.0±1.8 mmHg at 25°C
Index of Refraction	1.688
Storage condition	2-8℃

(3Z)-3-[({3-[(Diméthylamino)méthyl]phényl}amino)(phényl)méthylène]-2-oxo-6-indolinecarboxamide

(3Z)-3-[({3-[(Dimethylamino)methyl]phenyl}amino)(phenyl)methylen]-2-oxo-6-indolincarboxamid

(3Z)-3-[({3-[(Dimethylamino)methyl]phenyl}amino)(phenyl)methylene]-2-oxo-6-indolinecarboxamide

1H-Indole-6-carboxamide, 3-[[[3-[(dimethylamino)methyl]phenyl]amino]phenylmethylene]-2,3-dihydro-2-oxo-, (3Z)-

3-[[[3-[(Dimethylamino)methyl]phenyl]amino]phenylmethylene]-2,3-dihydro-2-oxo-1H-indole-6-carboxamide

BIX02188

DC Chemicals Limited
China
Product Name: BIX02188 (BIX 02188）
Price: $500.0/100mg $1000.0/250mg $2000.0/1g
Purity: 98.0%
Stocking Period: 3 Day
Contact: Tony Cao

Dayang Chem (Hangzhou) Co., Ltd.
China
Product Name: (3Z)-3-[[[3-[(Dimethylamino)methyl]phenyl]amino]phenylmethylene]-2,3-dihydro-2-oxo-1H-indole-6-carboxamide
Price: $Inquiry/100g $Inquiry/1kg $Inquiry/100kg $Inquiry/1000kg
Purity: 98.0%
Stocking Period: Inquiry
Contact: Ms Wang

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Price: $179/10mM*1mLinDMSO

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BIX02188

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