An inhibitor of tubulin polymerization (IC50 = 10 μM); binds to tubulin at the colchicine binding site; induces microtubule depolymerization in A-10 cells (EC50 = 21 nM); inhibits growth in a cancer cell line panel (IC50s = 9-43 nM) via formation of multiple spindles and induction of mitotic arrest; reduces tumor size in an MDA-MB-231 breast cancer mouse xenograft model in a dose-dependent manner; inhibits HIF-1α in RCC4 cells in a concentration-dependent manner

ELR510444 – 25 mg

Brand:
Cayman
CAS:
1233948-35-0
Storage:
-20
UN-No:
Non-Hazardous - /

ELR510444 is an inhibitor of tubulin polymerization (IC50 = 10 μM) that binds to tubulin at the colchicine (Item No. 9000760) binding site.{38488} It induces microtubule depolymerization in A-10 cells (EC50 = 21 nM). ELR510444 inhibits growth in a cancer cell line panel (IC50s = 9-43 nM) via formation of multiple spindles and induction of mitotic arrest. Oral administration of ELR510444 (3-6 mg/kg) reduces tumor size in an MDA-MB-231 breast cancer mouse xenograft model in a dose-dependent manner. ELR510444 also inhibits hypoxia-inducible factor 1α (HIF-1α) in RCC4 cells in a concentration-dependent manner.{38487}  

 

Available on backorder

Add to quotes
SKU: - Category:

Description

An inhibitor of tubulin polymerization (IC50 = 10 μM); binds to tubulin at the colchicine binding site; induces microtubule depolymerization in A-10 cells (EC50 = 21 nM); inhibits growth in a cancer cell line panel (IC50s = 9-43 nM) via formation of multiple spindles and induction of mitotic arrest; reduces tumor size in an MDA-MB-231 breast cancer mouse xenograft model in a dose-dependent manner; inhibits HIF-1α in RCC4 cells in a concentration-dependent manner,

Formal name: N-[5-(5-cyano-2-thienyl)-2-methylphenyl]-4-methyl-benzenesulfonamide

Synonyms: 

Molecular weight: 368.5

CAS: 1233948-35-0

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Microtubule Dynamics||Product Type|Biochemicals|Small Molecule Inhibitors||Research Area|Cancer

Related products

  • 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 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
  • 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
    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