An alkaloid with diverse biological activities; an inhibitor of Nav1.7 (IC50= 47.2 µM) and hERG (IC50 = 43.7 µM); increases the latent period of coughs

Peimine – 5 mg

Brand:
Cayman
CAS:
23496-41-5
Storage:
-20
UN-No:
Non-Hazardous - /

Peimine is an alkaloid that has been found in Fritillaria and has diverse biological activities, including ion channel inhibitory, anti-tussive, anticancer, and anti-inflammatory properties.{53420,56003,56004,56005,56006} It is an inhibitor of voltage-gated sodium channel 1.7 (Nav1.7; IC50= 47.2 µM) and human-ether-a-go-go (hERG), also known as Kv11.1 (IC50 = 43.7 µM).{56003,56004} It increases the latent period of coughs, decreases the number of coughs, and has expectorant activity in a mouse model of ammonia liquor-induced cough when administered at a dose of 3 mg/kg.{53420} Peimine (2.5, 5, and 10 µM) inhibits the growth of DU145, LNCaP, and PC3 prostate cancer, but not RWPE-1 non-cancerous, cells.{56005} It also induces phosphorylation of calcium/calmodulin-dependent protein kinase II (CaMKII) in, and apoptosis of, PC3 cells and inhibits PC3 cell invasion, migration, and epithelial-to-mesenchymal transition. Peimine (10, 20, or 50 mg/animal) reduces tumor growth in a PC3 mouse xenograft model. It decreases IL-1β-induced nitric oxide (NO) and prostaglandin E2 (PGE2; Item No. 14010) production and reduces inducible NO synthase (iNOS) and COX-2 protein levels in primary mouse articular chondrocytes in vitro.{56006} It also decreases the severity of osteoarthritis-associated histopathological alterations in a mouse model of osteoarthritis when administered at a dose of 20 mg/kg.  

 

Available on backorder

Add to quotes
SKU: 29963 - 5 mg Category:

Description

An alkaloid with diverse biological activities; an inhibitor of Nav1.7 (IC50= 47.2 µM) and hERG (IC50 = 43.7 µM); increases the latent period of coughs, decreases the number of coughs, and has expectorant activity in a mouse model of ammonia liquor-induced cough at 3 mg/kg; inhibits the growth of DU145, LNCaP, and PC3 prostate cancer, but not RWPE-1 non-cancerous, cells at 2.5, 5, and 10 µM; reduces tumor growth in a PC3 mouse xenograft model at 10, 20, or 50 mg/animal; decreases severity of osteoarthritis-associated histopathological alterations in a mouse model of osteoarthritis at 20 mg/kg

Formal name: (5α)-cevane-3β,6α,20-triol

Synonyms: 

Molecular weight: 431.7

CAS: 23496-41-5

Purity: ≥98%

Formulation: A crystalline solid

Related products

  • A powerful effector in both the TetR and revTetR transcriptional regulator systems

    Anhydrotetracycline (hydrochloride) – 50 mg

    The tetracycline repressor (TetR) is a transcriptional regulator which normally binds tightly to its palindromic tetO operator DNA, blocking gene expression.{17508} Tet causes the repressor to dissociate from the DNA, allowing transcription to occur. A novel reverse TetR (revTetR) requires tetracycline as a co-repressor to bind tetO and block transcription.{17509,17510} Anhydrotetracycline (hydrochloride) is a powerful effector in both the tetracycline repressor (TetR) and reverse TetR (revTetR) systems, binding the Tet repressor 35-fold more strongly than Tet.{17508,17511} Moreover, anhydrotetracycline poorly binds the 30S ribosomal subunit, compared to Tet,{17512} so it does not act as a general inhibitor of translation and is a poor antibiotic. Perhaps related to this, the concentration of anhydrotetracycline that inhibits eukaryotic cell growth is more than a 1,000-fold above the dose that alters transcription through TetR.{17508}  

     

    Brand:
    Cayman
    SKU:10009542 - 50 mg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page
  • PtdIns-(3

    PtdIns-(3,4,5)-P3-biotin (sodium salt) – 25 µg

    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.  

     

    Brand:
    Cayman
    SKU:10009531 - 25 µg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page
  • A potent inhibitor of Cdk2/cyclin E with an IC50 value of 0.1 µM; also inhibits Cdk7/cyclin H

    (R)-Roscovitine – 5 mg

    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}  

     

    Brand:
    Cayman
    SKU:10009569 - 5 mg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page
  • 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}

    CAY10512 – 50 mg

    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}  

     

    Brand:
    Cayman
    SKU:10009536 - 50 mg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page