An anthelmintic mitochondrial uncoupler; inhibits STAT3 (IC50 = 0.25 μM) and stimulates autophagy; induces mitochondrial uncoupling

Niclosamide – 100 g

Brand:
Cayman
CAS:
50-65-7
Storage:
-20
UN-No:
Limited Quantity - 3077 / 9

Niclosamide is an anthelmintic that disrupts mitochondrial metabolism in parasitic worms and animal models.{29804,17472,27785} It inhibits STAT3 (IC50 = 0.25 μM) and stimulates autophagy by reversibly inhibiting mammalian target of rapamycin complex 1 (mTORC1) signaling.{17472,18706} It completely inhibits phosphorylation of ribosomal S6 kinases (S6K) when used at a concentration of 3 µM.{17472} Niclosamide (1 µM) induces mitochondrial uncoupling, decreasing cellular ATP concentrations and increasing the ratio of ADP to ATP in HepG2 cells, and activates AMP-activated protein kinase (AMPK) in NIH3T3 cells.{27785} It also increases lipid oxidation by 5-fold in HepG2 cells. It prevents high-fat diet-induced hepatic steatosis and insulin resistance and improves glycemic control in db/db mice when administered at a dose of at 125 mg/kg per day.{27785} Niclosamide also inhibits proliferation and colony formation of DU145 prostate cancer cells, which have constitutively active STAT3 (IC50s = 0.7 and 0.1 µM, respectively).{18706}  

 

Available on backorder

Add to quotes
SKU: 10649 - 100 g Category:

Description

An anthelmintic mitochondrial uncoupler; inhibits STAT3 (IC50 = 0.25 μM) and stimulates autophagy; induces mitochondrial uncoupling, activates AMPK, and increases lipid peroxidation in vitro at 1 µM; prevents high-fat diet-induced hepatic steatosis and insulin resistance and improves glycemic control in db/db mice at 125 mg/kg per day; inhibits proliferation and colony formation of DU145 prostate cancer cells (IC50s = 0.7 and 0.1 µM, respectively)

Formal name: 5-chloro-N-(2-chloro-4-nitrophenyl)-2-hydroxy-benzamide

Synonyms:  NSC 178296

Molecular weight: 327.1

CAS: 50-65-7

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Antiparasitics|Anthelmintics||Product Type|Biochemicals|Small Molecule Activators|Kinases||Product Type|Biochemicals|Small Molecule Inhibitors|Oxidative Phosphorylation||Research Area|Cancer|Cell Signaling|JAK/STAT Signaling||Research Area|Cancer|Transcription Factors|STATs||Research Area|Cell Biology|Cell Signaling|PI3K/Akt/mTOR Signaling||Research Area|Cell Biology|Endomembrane System & Vesicular Trafficking|Autophagy||Research Area|Cell Biology|Mitochondrial Biology||Research Area|Endocrinology & Metabolism|Metabolic Diseases|Diabetes||Research Area|Endocrinology & Metabolism|Metabolic Diseases|NAFLD & NASH||Research Area|Endocrinology & Metabolism|Nutrient Sensing||Research Area|Epigenetics, Transcription, & Translation|Transcription Factors

Related products

  • 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
  • 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 – 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
  • 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