An RXR agonist (Kd = 3 nM); selective for RXRs over RARs (Kd = >10

LG 100268 – 10 mg

Brand:
Cayman
CAS:
153559-76-3
Storage:
-20
UN-No:
Non-Hazardous - /

LG 100268 is an agonist of retinoid X receptors (RXRs; Kd = 3 nM).{20758} It is selective for RXRs over retinoic acid receptors (RARs; Kd = >10,000 nM).{36450} In vitro, LG 100268 (1 µM) induces apoptosis in HL-60 human leukemia cells when used in combination with TTNPB (Item No. 16144).{20758} LG 100268 (100, 300, and 1,000 nM) dose-dependently inhibits COX-2 expression and increases ATP-binding cassette transporter (ABCA1) levels in macrophage-like RAW 264.7 cells.{36451} In vivo, it inhibits vinyl carbamate-induced lung tumor growth in mice when administered at a dose of 40 mg/kg.  

 

Out of stock

Add to quotes
SKU: 21606 - Category:

Description

An RXR agonist (Kd = 3 nM); selective for RXRs over RARs (Kd = >10,000); induces apoptosis in HL-60 human leukemia cells when used at a concentration of 1 µM in combination with TTNPB; dose-dependently inhibits COX-2 expression (100, 300 and 1000 nM) and increases ABCA1 levels in macrophage-like RAW 264.7 cells; inhibits vinyl carbamate-induced lung tumor growth in mice (40 mg/kg)

Formal name: 6-[1-(5,6,7,8-tetrahydro-3,5,5,8,8-pentamethyl-2-naphthalenyl)cyclopropyl]-3-pyridinecarboxylic acid

Synonyms:  AGN 192620|CD3127

Molecular weight: 363.5

CAS: 153559-76-3

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Agonists||Research Area|Cancer|Cell Death|Apoptosis||Research Area|Endocrinology & Metabolism|Hormones & Receptors|RARs, RORs, & RXRs||Research Area|Immunology & Inflammation|Innate Immunity

Related products

  • A zwitterionic glycerophospholipid commonly used in the formation of lipid monolayers

    1,2-Dipalmitoyl-sn-glycero-3-PC – 50 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 - 50 mg

    Available on backorder

    Add to quotes
    View product page
  • A zwitterionic glycerophospholipid commonly used in the formation of lipid monolayers

    1,2-Dipalmitoyl-sn-glycero-3-PC – 25 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 - 25 mg

    Available on backorder

    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
    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
    View product page