Atovaquone-d4 is intended for use as an internal standard for the quantification of atovaquone (Item No. 23802) by GC- or LC-MS. Atovaquone is a broad-spectrum antiprotozoal agent that is active against Plasmodium, Toxoplasma, and Babesia, among other protozoa.{39560} It inhibits complex III activity on dihydroorotate in isolated P. falciparum and P. yoelii mitochondria more potently than in rat liver mitochondria (EC50s = 0.95, 0.94, and 510 nM, respectively) and depolarizes the mitochondrial membrane in P. yoelii-infected mouse erythrocytes (EC50 = 260 nM).{39561,39562} Atovaquone also inhibits transport mediated by human breast cancer resistance protein (BCRP) and P-glycoprotein in membrane vesicles (IC50s = 0.23 and 6.8 μM, respectively).{39563} It inhibits the growth of T. gondii in MRC-5 human lung fibroblasts in vitro (IC50 = ~64 nM) and increases mean survival of T. gondii-infected mice from 5.5 to 21.2 days when administered at a dose of 100 mg/kg per day.{39564} Formulations containing atovaquone have been used in the treatment of Pneumocystis pneumonia and toxoplasmosis as well as in combination with proguanil in the treatment of malaria and babesiosis.
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An internal standard for the quantification of atovaquone by GC- or LC-MS
Formal name: 2-[trans-4-(4-chlorophenyl)cyclohexyl]-3-hydroxy-1,4-naphthalenedione-5,6,7,8-d4
Synonyms:
Molecular weight: 370.9
CAS: 2070015-14-2
Purity: ≥99% deuterated forms (d1-d4)
Formulation: A solid
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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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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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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