The KCNQ (Kv7) family of voltage-gated potassium (K+) channels consists of five members, KCNQ1-KCNQ5. KCNQ1-KCNQ5 are critical for setting up the excitation threshold of action potentials. KCNQ1 is expressed mainly in cardiac tissue, peripheral epithelial cells, and smooth muscle cells, while KCNQ2-KCNQ5 are predominantly expressed in the peripheral and central nervous system, including hippocampal cells, cortical cells, and dorsal root ganglion. ML-213 is a selective activator of KCNQ2 (Kv7.2) and KCNQ4 (Kv7.4) channels (EC50s = 230 and 510 nM for KCNQ2 and KCNQ4, respectively) that demonstrates > 80-fold selectivity against other related K+ channels.{24549}
A selective activator of KCNQ2 (Kv7.2) and KCNQ4 (Kv7.4) channels (EC50s = 230 and 510 nM for KCNQ2 and KCNQ4, respectively) that demonstrates > 80-fold selectivity against other related K+ potassium channels
Formal name: N-(2,4,6-trimethylphenyl)-bicyclo[2.2.1]heptane-2-carboxamide
Synonyms: CID-3111211
Molecular weight: 257.4
CAS: 489402-47-3
Purity: ≥98%
Formulation: A crystalline solid
Product Type|Biochemicals|Ion Channel Modulation|Activators||Research Area|Neuroscience
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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Cyclin-dependent kinases (CDKs) are key regulators of cell cycle progression and are therefore promising targets for cancer therapy. (R)-Roscovitine is a potent inhibitor of Cdk2/cyclin E with an IC50 value of 0.1 µM.{14988} It also inhibits Cdk7/cyclin H, Cdk5/p35, and cell division cycle (cdc)/cyclin B with IC50 values of 0.49, 0.16, and 0.65 µM, respectively.{14987,14988,14991} (R)-Roscovitine inhibits the growth of rapidly proliferating cells with an average IC50 value of 15.2 µM against a panel of 19 human tumor cell lines.{14988} In murine models of polycystic kidney disease, (R)-roscovitine effectively inhibited disease progression at doses of 50-100 mg/kg.{14564}
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