BIX 02189 - Moligand™, 10mM in DMSO , Inhibitor of mitogen-activated protein kinase 7;Inhibitor of mitogen-activated protein kinase kinase 5;Inhibitor of transforming growth factor beta receptor 1, CAS No.1094614-85-3, Inhibitor of mitogen-activated protein kinase 7;Inhibitor of mitogen-activated protein kinase kinase 5;Inhibitor of transforming growth factor beta receptor 1

CAS: 1094614-85-3 Cat. No.: B407824 Summenformel: C₂₇H₂₈N₄O₂ Molekulargewicht: 440.54

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

(Z)-3-((3-((dimethylamino)methyl)phenylamino)(phenyl)methylene)-N,N-dimethyl-2-oxoindoline-6-carboxamide

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Übersicht

Information

BIX02189 is a selective inhibitor ofMEK5withIC50of 1.5 nM, also inhibits ERK5 catalytic activity withIC50of 59 nM in cell-free assays, and does not inhibit closely related kinases MEK1, MEK2, ERK2, and JNK2.
In vitro

BIX02189 blocks MEK5 and ERK5 catalytic activity with IC50 values of 1.5 nM and 59 nM, respectively. They are more potent than the effect caused by BIX02188 with IC50 values of 4.3 nM and 810 nM, respectively. BIX02189 shows inhibitory activity against CSF1R (FMS) with IC50 of 46 nM but displays no activity against related kinases MEK1, MEK2, ERK1, p38α, JNK2, EGFR, and STK16 with IC50 values of >3.7 μM. Pretreatment with BIX02189 inhibits sorbitol-induced phosphorylation of ERK5 in HeLa cells in a dose dependent manner, and displays no inhibitory activity against the phosphorylation of ERK1/2, p38, and JNK1/2 MAPKs. Treatment with only BIX02189 for 24 hours in HeLa or HEK293 cells does not show any cytotoxic effect. BIX02189 inhibits MEK5/ERK5/MEF2C-driven luciferase expression in HeLa and HEK293 cells with IC50 values of 0.53 μM and 0.26 μM, respectively. This is a more significant than the effect caused by BIX02188. BIX02189 inhibits the activation of ERK5, and suppresses C-terminus of Hsc70-interacting protein (CHIP) mediated p53 ubiquitination, leading to the reverse of the protective effect caused by laminar flow (L-flow) in human umbilical vein endothelial cells (HUVECs) exposed to 15d-PGJ2. BIX02189 (10 uM) inhibits ERK5 phosphorylation, and reduces myocyte enhancer factor 2 (MEF2) transcriptional activity in neonatal rat cardiomyocytes (NRCMs) stimulated by isoproterenol. BIX02189 enhances the sorbitol induced apoptosis in NRCMs, confirming the protective role of ERK5 in cardiomyocytes.

In vivo

Cell Data

cell lines：B16F10, A549, and HT29 cells

Concentrations：Dissolved in DMSO, final concentration ~10 μM

Incubation Time：Pretreatment for 1.5 hours

Powder Purity:≥99%

Specifications

Synonyme

(Z)-3-((3-((dimethylamino)methyl)phenylamino)(phenyl)methylene)-N,N-dimethyl-2-oxoindoline-6-carboxamide

Spezifikationen & Reinheit

Moligand™, 10mM in DMSO

Biochemische und physiologische Mechanismen

BIX02189 is a selective inhibitor of MEK5 with IC50 of 1.5 nM, also inhibits ERK5 catalytic activity with IC50 of 59 nM in cell-free assays, and does not inhibit closely related kinases MEK1, MEK2, ERK2, and JNK2.

Storage

Store at -80°C

Verschickt in

Dry ice packs + Cold packs

Dieses Produkt erfordert Kühlkettenversand. Grundversand und andere Economy-Optionen sind nicht verfügbar.

Note

Moligand™

Aktionsart

INHIBITOR

Mechanismus der Wirkung

Inhibitor of mitogen-activated protein kinase 7;Inhibitor of mitogen-activated protein kinase kinase 5;Inhibitor of transforming growth factor beta receptor 1

Namen und Kennungen

• Isomere SMILES: CN(C)CC1=CC(=CC=C1)N=C(C2=CC=CC=C2)C3=C(NC4=C3C=CC(=C4)C(=O)N(C)C)O
• Alternative CAS-Nummer: 1265916-41-3
• MeSH-Eintrag: BIX 02189;BIX-02189;BIX02189
• Molekulargewicht: 440.54
• Reaxy-Rn: 60405313
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=60405313&ln=

Zugehörige Ziele (menschlich)

TGFBR1 Tchem TGF-beta receptor type-1 (1 Activities)

Discover Target: TGFBR1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

MAPK7 Tchem Mitogen-activated protein kinase 7 (1 Activities)

Discover Target: MAPK7

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

MAP2K5 Tchem Dual specificity mitogen-activated protein kinase kinase 5 (1 Activities)

Discover Target: MAP2K5

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Chemische und physikalische Eigenschaften

• Löslichkeit: Solubility (25°C) In vitro DMSO: 48 mg/mL warmed with 50ºC Water: bath (196.53 mM); Water: Insoluble; Ethanol: Insoluble