A kavalactone with diverse biological activities; a positive allosteric modulator of α4β2δ subunit-containing GABAA receptors (EC50s = 25 and 59 µM in the presence and absence of 300 µM kavain); reduces growth of WPMY-1 prostate cancer cells (IC50= 5.2 µg/ml); reduces LPS-induced TNF-α production in primary murine macrophages; reduces hind paw swelling and TNF-α production in a mouse model of collagen-induced arthritis; reduces acetic acid-induced abdominal constrictions in mice (ED50= 15.71 mg/kg)

Kavain – 100 mg

Brand:
Cayman
CAS:
500-64-1
Storage:
-20
UN-No:
Non-Hazardous - /

Kavain is a kavalactone and the major constituent of the pepper plant kava (P. methysticum) and has diverse biological activities.{46119,46120,46121,46122} It is a positive allosteric modulator of α4β2δ subunit-containing GABAA receptors with EC50 values of 25 and 59 µM in the presence and absence of 300 µM kavain, respectively, in Xenopus oocytes expressing human receptors.{46119} Kavain reduces growth of WPMY-1 prostate cancer cells (IC50 = 5.2 µg/ml).{46120} It reduces LPS-induced TNF-α production in primary murine macrophages in a concentration-dependent manner.{46121} In vivo, kavain (1 mg/animal) reduces hind paw swelling and TNF-α production in wild-type, but not Erk-/-, mice in a mouse model of collagen-induced arthritis. Kavain also reduces acetic acid-induced abdominal constrictions in mice (ED50= 15.71 mg/kg).{46122}  

 

Available on backorder

Add to quotes
SKU: 26524 - 100 mg Category:

Description

A kavalactone with diverse biological activities; a positive allosteric modulator of α4β2δ subunit-containing GABAA receptors (EC50s = 25 and 59 µM in the presence and absence of 300 µM kavain); reduces growth of WPMY-1 prostate cancer cells (IC50= 5.2 µg/ml); reduces LPS-induced TNF-α production in primary murine macrophages; reduces hind paw swelling and TNF-α production in a mouse model of collagen-induced arthritis; reduces acetic acid-induced abdominal constrictions in mice (ED50= 15.71 mg/kg)

Formal name: (6R)-5,6-dihydro-4-methoxy-6-[(1E)-2-phenylethenyl]-2H-pyran-2-one

Synonyms:  Kawain|NSC 112162

Molecular weight: 230.3

CAS: 500-64-1

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Ion Channel Modulation||Product Type|Biochemicals|Natural Products||Research Area|Cancer||Research Area|Immunology & Inflammation|Autoimmunity|Rheumatoid Arthritis||Research Area|Immunology & Inflammation|Innate Immunity||Research Area|Neuroscience|Pain Research

Related products

  • 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
  • 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) – 50 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 - 50 µg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page
  • 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 – 1 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 - 1 mg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page