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

Dimebolin – 25 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 - 25 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

  • 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; activity is mediated by the combined inhibition of RasGAP and ERK1 with Kd values of 98 and 212 nM

    SC-1 – 5 mg

    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.  

     

    Brand:
    Cayman
    SKU:10009557 - 5 mg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page
  • A powerful effector in both the TetR and revTetR transcriptional regulator systems

    Anhydrotetracycline (hydrochloride) – 100 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 - 100 mg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page
  • A powerful effector in both the TetR and revTetR transcriptional regulator systems

    Anhydrotetracycline (hydrochloride) – 500 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 - 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 – 1 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 - 1 mg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page