XMD8-85 is an ERK5 inhibitor (IC50 = 87 nM in an enzyme assay).{42420} It is selective for ERK5 over tyrosine non-receptor kinase 2 (TNK2; IC50 = 959 nM), but does inhibit the leucine-rich repeat kinase 2 (LRRK2) mutant LRRK2G2019S (IC50 = 26 nM), which has been found in patients with Parkinson’s disease.{46785,42420} XMD8-85 inhibits EGF-induced ERK5 autophosphorylation in HeLa cells (EC50 = 0.19 μM).{42420}
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An ERK5 inhibitor (IC50 = 87 nM in an enzyme assay); selective for ERK5 over TNK2 (IC50 = 959 nM), but does inhibit LRRK2G2019S (IC50 = 26 nM); inhibits EGF-induced ERK5 autophosphorylation in HeLa cells (EC50 = 0.19 μM)
Formal name: 5,11-dihydro-2-[[2-methoxy-4-(4-methyl-1-piperazinyl)phenyl]amino]-5,11-dimethyl-6H-pyrimido[4,5-b][1,4]benzodiazepin-6-one
Synonyms: ERK5-IN-1
Molecular weight: 459.5
CAS: 1234479-76-5
Purity: ≥98%
Formulation: A solid
The PtdIn phosphates play an important role in the generation and transduction of intracellular signals.{8344,4096,14518} PtdIns-(3,4,5)-P3-biotin is an affinity probe which allows the PIP3 to be detected through an interaction with the biotin ligand. This design allows PtdIns-(3,4,5)-P3-biotin to serve as a general probe for any protein with a high affinity binding interaction with inositol-(3,4,5)-triphosphate phospholipids, such as phosphatidylinositol 3-kinase, PTEN, or PH-domain-containing proteins.
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The PtdIn phosphates play an important role in the generation and transduction of intracellular signals.{8344,4096,14518} PtdIns-(3,4,5)-P3-biotin is an affinity probe which allows the PIP3 to be detected through an interaction with the biotin ligand. This design allows PtdIns-(3,4,5)-P3-biotin to serve as a general probe for any protein with a high affinity binding interaction with inositol-(3,4,5)-triphosphate phospholipids, such as phosphatidylinositol 3-kinase, PTEN, or PH-domain-containing proteins.
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1,2-Dipalmitoyl-sn-glycero-3-PC (DPPC) is a zwitterionic glycerophospholipid commonly used in the formation of lipid monolayers, bilayers, and liposomes for use in a variety of applications.{14480,24261,14478,14479} It has been used in the formation of proteoliposomes for implantation of γ-glutamyl transpeptidase into human erythrocyte membranes.{14478} Incorporation of glycosphingolipid antigens into DPPC-containing liposomes increases the immunogenicity of the antigens in mice.{14479}
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1,2-Dipalmitoyl-sn-glycero-3-PC (DPPC) is a zwitterionic glycerophospholipid commonly used in the formation of lipid monolayers, bilayers, and liposomes for use in a variety of applications.{14480,24261,14478,14479} It has been used in the formation of proteoliposomes for implantation of γ-glutamyl transpeptidase into human erythrocyte membranes.{14478} Incorporation of glycosphingolipid antigens into DPPC-containing liposomes increases the immunogenicity of the antigens in mice.{14479}
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