A nortriterpenoid; inhibits UGT1A6 and UGT2B7 (Kis = 0.6 and 17.3 μM

Demethylzeylasteral – 5 mg

Brand:
Cayman
CAS:
107316-88-1
Storage:
-20
UN-No:
Non-Hazardous - /

Demethylzeylasteral is a nortriterpenoid originally isolated from T. wilfordii that has diverse biological activities, including enzyme inhibitory, anti-angiogenic, antiproliferative, anti-inflammatory, and immunosuppressive properties.{45479,45480,45481,45482} Demethylzeylasteral inhibits the UDP-glucuronosyltransferase (UGT) isoforms UGT1A6 and UGT2B7 (Kis = 0.6 and 17.3 μM, respectively).{45480} It inhibits growth of bovine aortic endothelial cells (BAEs) and U251 human glioma cancer cells in vitro (IC50s = 0.21 and ~6.2 μM, respectively), as well as inhibits tumor growth and neovascularization in vivo in a B16/F10 melanoma mouse allograft model when administered at a dose of 30 mg/kg per day.{45479} Demethylzeylasteral (0.12 mg/kg per day) decreases renal proteinuria, lesions, immune cell infiltration, and protein levels of TNF-α, COX-2, and ICAM-1 in lupus-prone MRL/lpr mice.{45481} Demethylzeylasteral (10 mg/kg per day) also increases survival of recipient rats in a model of kidney transplant.{45482}  

 

Available on backorder

Add to quotes
SKU: 28595 - 5 mg Category:

Description

A nortriterpenoid; inhibits UGT1A6 and UGT2B7 (Kis = 0.6 and 17.3 μM, respectively); inhibits growth of BAEs and of human U251 glioma cancer cells in vitro (IC50s = 0.21 and ~6.2 μM, respectively); inhibits tumor growth and neovascularization in vivo in a B16/F10 melanoma allograft mouse model at 30 mg/kg per day; decreases renal proteinuria, lesions, immune cell infiltration, and protein levels of TNF-α, COX-2, and ICAM-1 in lupus-prone MRL/lpr mice at 0.12 mg/kg per day; increases kidney transplant survival in recipient rats at 10 mg/kg per day

Formal name: (9β,13α,14β,20α)-2,3-dihydroxy-9,13-dimethyl-6,23-dioxo-24,25,26-trinoroleana-1,3,5(10),7-tetraen-29-oic acid

Synonyms: 

Molecular weight: 480.6

CAS: 107316-88-1

Purity: ≥98%

Formulation: A crystalline solid

Related products

  • A potent inhibitor of Cdk2/cyclin E with an IC50 value of 0.1 µM; also inhibits Cdk7/cyclin H

    (R)-Roscovitine – 500 µg

    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 - 500 µg

    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 – 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 zwitterionic glycerophospholipid commonly used in the formation of lipid monolayers

    1,2-Dipalmitoyl-sn-glycero-3-PC – 100 mg

    1,2-Dipalmitoyl-sn-glycero-3-PC (DPPC) is a zwitterionic glycerophospholipid commonly used in the formation of lipid monolayers, bilayers, and liposomes for use in a variety of applications.{14480,24261,14478,14479} It has been used in the formation of proteoliposomes for implantation of γ-glutamyl transpeptidase into human erythrocyte membranes.{14478} Incorporation of glycosphingolipid antigens into DPPC-containing liposomes increases the immunogenicity of the antigens in mice.{14479}  

     

    Brand:
    Cayman
    SKU:10009473 - 100 mg

    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 – 10 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 - 10 mg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page