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MedKoo product information:
BIX 02189
BIX 02189 is a selective MEK5/ERK5 inhibitor with an IC50 of 59 nM.
BIX02189 was reported to inhibit catalytic function of purified,
MEK5 enzyme.
Current developer:
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MedKoo Code#: 401150
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Name: BIX 02189
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CAS#: 1094614-85-3
Synonym:
BIX 02189
IUPAC/Chemical name:
(Z)-3-(((3-((dimethylamino)methyl)phenyl)amino)(phenyl)methylene)-N,N-dimethyl-2-oxoindoline-6-carboxamide
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Chemical structure
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Theoretical analysis
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MedKoo Code#: 401150
Name: BIX 02189
CAS#: 1094614-85-3
Chemical Formula: C27H28N4O2
Exact Mass: 440.22123
Molecular Weight: 440.53682
Elemental Analysis: C, 73.61; H, 6.41; N,
12.72; O, 7.26
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Availability and price:
BIX 02189
is in stock
20 mg / $280.00
50 mg / $550.00
100 mg / $950.00
Multiple grams
in stock at low prices.
To inquire quotation and lead time or to ask questions, please send email to
sales@medkoo.com to describe your needs. A representative
will respond your email shortly. We offer big discount for orders of bulk quantities.
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Information about this agent
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BIX02189 is a newly detected inhibitor of MEK5 and
ERK5 and plays a significant role in detecting the specific effects of
ERK5. Tyrosine hydroxylase enzyme is required for the synthesis of
catecholamines and its levels are controlled by ERK5. BIX02189 helped to
study the role of ERK5 in maintaining the levels of Tyrosine hydroxylase.
This inhibitor opens the gateway to analyze the physiological effects of
MEK5/ERK5 pathway.
ERK5 is a member of the MAPK family of proteins. Its
activation is required the regular maintenance and growth of neuronal
tissues. BIX 02189 inhibits the phosphorylation of ERK5. BIX 02189 has
been effectively used to study the physiological role of ERK5. The
molecular size of ERK5 is twice as big as ERK1/2 and the amino terminal
of this protein is homologous to ERK1/2. However the carboxy terminus of
this protein is unique as it has 2 proline rich regions and one NLS
(source: http://www.zimbio.com).
1: Gilley R, Lochhead PA, Balmanno K, Oxley D, Clark
J, Cook SJ. CDK1, not ERK1/2 or ERK5, is required for mitotic
phosphorylation of BIMEL. Cell Signal. 2012 Jan;24(1):170-80. Epub 2011
Sep 8. PubMed PMID: 21924351.
2: Yang Q, Lee JD. Targeting the BMK1 MAP kinase pathway in cancer
therapy. Clin Cancer Res. 2011 Jun 1;17(11):3527-32. Epub 2011 Mar 8.
PubMed PMID: 21385929; PubMed Central PMCID: PMC3107913.
3: Obara Y, Nemoto W, Kohno S, Murata T, Kaneda N, Nakahata N. Basic
fibroblast growth factor promotes glial cell-derived neurotrophic factor
gene expression mediated by activation of ERK5 in rat C6 glioma cells.
Cell Signal. 2011 Apr;23(4):666-72. Epub 2010 Dec 2. PubMed PMID:
21130871.
4: Kimura TE, Jin J, Zi M, Prehar S, Liu W, Oceandy D, Abe J, Neyses L,
Weston AH, Cartwright EJ, Wang X. Targeted deletion of the extracellular
signal-regulated protein kinase 5 attenuates hypertrophic response and
promotes pressure overload-induced apoptosis in the heart. Circ Res.
2010 Mar 19;106(5):961-70. Epub 2010 Jan 14. PubMed PMID: 20075332;
PubMed Central PMCID: PMC3003662.
5: Obara Y, Nakahata N. The signaling pathway leading to extracellular
signal-regulated kinase 5 (ERK5) activation via G-proteins and
ERK5-dependent neurotrophic effects. Mol Pharmacol. 2010 Jan;77(1):10-6.
Epub 2009 Oct 26. Review. PubMed PMID: 19858097.
6: Obara Y, Yamauchi A, Takehara S, Nemoto W, Takahashi M, Stork PJ,
Nakahata N. ERK5 activity is required for nerve growth factor-induced
neurite outgrowth and stabilization of tyrosine hydroxylase in PC12
cells. J Biol Chem. 2009 Aug 28;284(35):23564-73. Epub 2009 Jul 6.
PubMed PMID: 19581298; PubMed Central PMCID: PMC2749131.
7: Tatake RJ, O'Neill MM, Kennedy CA, Wayne AL, Jakes S, Wu D, Kugler SZ
Jr, Kashem MA, Kaplita P, Snow RJ. Identification of pharmacological
inhibitors of the MEK5/ERK5 pathway. Biochem Biophys Res Commun. 2008
Dec 5;377(1):120-5. Epub 2008 Oct 1. PubMed PMID: 18834865.
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Email:
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(Keyword; CAS#; MedKoo code#)
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