Ledipasvir-d6 is intended for use as an internal standard for the quantification of ledipasvir (Item No. 18519) by GC- or LC-MS. Ledipasvir is an inhibitor of hepatitis C virus (HCV) non-structural protein 5A (NS5A).{53973,53974} It inhibits viral replication in genotype 1a and 1b HCV replicon cells (EC50s = 0.031 and 0.004 nM, respectively). It also inhibits viral replication in genotype 2a, 2b, 3a, 4a, 4d, 5a, 6a, and 6e HCV replicon cells (EC50s = 0.11-530 nM).{53974} Lepidasvir acts synergistically with IFN-α, ribavirin (Item No. 16757), or GS-9669 and additively with GS-9451, simeprevir (Item No. 22144), daclatasvir (Item No. 23730), or PSI-7977 (sofosbuvir; Item No. 15402) to inhibit viral replication in genotype 1a HCV replicon cells. Formulations containing ledipasvir have been used in combination therapy for the treatment of chronic HCV infection.
Available on backorder
An internal standard for the quantification of ledipasvir by GC- or LC-MS
Formal name: N-[(1S)-1-[[(6S)-6-[5-[9,9-difluoro-7-[2-[(1R,3S,4S)-2-[(2S)-2-[(methoxy-d3-carbonyl)amino]-3-methyl-1-oxobutyl]-2-azabicyclo[2.2.1]hept-3-yl]-1H-benzimidazol-6-yl]-9H-fluoren-2-yl]-1H-imidazol-2-yl]-5-azaspiro[2.4]hept-5-yl]carbonyl]-2-methylpropyl]-carbamic acid, methyl-d3 ester
Synonyms:
Molecular weight: 895.1
CAS: 2050041-12-6
Purity: ≥99% deuterated forms (d1-d6)
Formulation: A solid
The nuclear factor-κB (NF-κB) regulates the expression of numerous genes involved in immunity and inflammation, cellular stress responses, growth, and apoptosis. Resveratrol, a polyphenolic trans-stilbene, is a known inhibitor of the activation of NF-κB and exhibits activity against a wide variety of cancer cells. CAY10512 is a substituted trans-stilbene analog of resveratrol that is 100-fold more potent as measured by antioxidant activity. The IC50 value for inhibition of TNFα-induced activation of NF-κB by CAY10512 is 0.15 µM compared to 20 µM by resveratrol.{14545}
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 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
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