GMQ is an activator of acid-sensing ion channel 3 (ASIC3).{54008} It evokes rapid inward currents with little desensitization in CHO cells expressing ASIC3 (EC50 = 67 µM at neutral pH). It is also an inhibitor of the GABAA receptor (IC50 = 0.39 µM in primary rat hippocampal neurons).{54009} GMQ has stimulatory effects on large-conductance calcium-activated potassium (BKCa) channels in GH3 rat pituitary cells and on non-selective cation currents in Rolf B1.T olfactory sensory neurons.{54010} It increases paw licking time in Asic3+/+ and, to a lesser extent, Asic3-/- mice when administered at a dose of 100 µM, an effect that can be blocked by the ASIC inhibitor amiloride (Item No. 14409).{54008}
Available on backorder
An ASIC3 activator (EC50 = 67 µM for evoking rapid inward currents in ASIC3-expressing CHO cells at neutral pH); an inhibitor of the GABAA receptor (IC50 = 0.39 µM in primary rat hippocampal neurons); increases paw licking time in Asic3+/+ and, to a lesser extent, Asic3-/- mice at 100 µM
Formal name: N-(4-methyl-2-quinazolinyl)-guanidine, monohydrochloride
Synonyms:
Molecular weight: 237.7
CAS: 5361-15-9
Purity: ≥95%
Formulation: A crystalline solid
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.
Available on backorder
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.
Available on backorder
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.
Available on backorder
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}
Available on backorder