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
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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The maintenance of embryonic stem cells in culture typically requires feeder cells and various exogenous factors found in serum. Murine embryonic stem (mES) cells can be maintained in the absence of feeder cells and serum but require the leukemia inhibitor factor (LIF) and bone morphogenic protein (BMP) to prevent differentiation and promote self-renewal. SC-1 is a small molecule activator of stem cell renewal that allows the propagation of OG2 mES cells for at least 10 passages in an undifferentiated state.{14533} The activity of SC-1 is mediated by the combined inhibition of RasGAP and ERK1 with Kd values of 98 and 212 nM, respectively.{14533} Inhibition of RasGAP increases Ras signaling via the PI3-kinase pathway which promotes self-renewal, whereas inhibition of ERK blocks differentiation.
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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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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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