A neuroprotective agent; binds to histamine H1 and H2 receptors (IC50s = 3.8 and 287 nM

Dimebolin – 1 mg

Brand:
Cayman
CAS:
3613-73-8
Storage:
-20
UN-No:
Non-Hazardous - /

Dimebolin is a neuroprotective agent.{17760,15457,17770} It binds to histamine H1 and H2 receptors (IC50s = 3.8 and 287 nM, respectively), as well as α1A-, α1B-, α1D-, and α2A-adrenergic receptors (ARs), imidazoline I2 receptors, and the serotonin (5-HT) receptor subtypes 5-HT2A, 5-HT2C, 5-HT6, and 5-HT7 (Kis = 8-313 nM).{49510} It also inhibits NMDA-evoked currents and voltage-gated calcium channels in mouse primary striatal neurons (IC50s = 10 and 50 μM, respectively).{17760} Dimebolin (50 μM) inhibits glutamate-induced apoptosis in primary striatal neurons derived from the YAC128 transgenic mouse model of Huntington’s disease. It inhibits cell death induced by amyloid-β (25-35) (Item No. 24155) in cerebellar granule cells when used at a concentration of 25 μM.{15457} Dimebolin (1 mg/kg) inhibits decreases in two-way active avoidance reaction (TWAA) acquisition in a rat model of Alzheimer’s disease induced by 1-ethyl-1-(2-hydroxyethyl) aziridinium (AF64A).{17770}  

 

Available on backorder

Add to quotes
SKU: 9000556 - 1 mg Category:

Description

A neuroprotective agent; binds to histamine H1 and H2 receptors (IC50s = 3.8 and 287 nM, respectively), as well as α1A-, α1B-, α1D-, and α2A-ARs, imidazoline I2 receptors, and 5-HT2A, 5-HT2C, 5-HT6, and 5-HT7 receptors (Kis = 8-313 nM); inhibits NMDA-evoked currents and voltage-gated calcium channels in mouse primary striatal neurons (IC50s = 10 and 50 μM, respectively); inhibits glutamate-induced apoptosis in primary striatal neurons derived from the YAC128 transgenic mouse model of Huntington’s disease at 50 μM; inhibits cell death induced by amyloid-β (25-35) in cerebellar granule cells at 25 μM; inhibits decreases TWAA acquisition in a rat model of AF64A-induced Alzheimer’s disease at 1 mg/kg

Formal name: 2,3,4,5-tetrahydro-2,8-dimethyl-5-[2-(6-methyl-3-pyridinyl)ethyl]-1H-pyrido[4,3-b]indole

Synonyms:  Dimebon™|Latrepirdine

Molecular weight: 319.4

CAS: 3613-73-8

Purity: ≥98%

Formulation: A crystalline solid

Related products

  • 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 – 500 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 - 500 mg

    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
  • PtdIns-(3

    PtdIns-(3,4,5)-P3-biotin (sodium salt) – 10 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 - 10 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 – 10 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 - 10 mg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page