The first identified small molecule inhibitor of BLM helicase (IC50 = 1.8 μM) that is 28-fold selective against the related helicases RECQ1

ML-216 – 5 mg

Brand:
Cayman
CAS:
1430213-30-1
Storage:
-20
UN-No:
Non-Hazardous - /

Bloom (BLM) helicase is a DNA unwinding enzyme important for DNA repair in the homologous recombination pathway. Mutations of the BLM gene result in reduced BLM helicase activity that is associated with the rare genetic disorder, Bloom’s Syndrome, and a predisposition to developing cancer. ML-216 is the first identified small molecule inhibitor of BLM helicase (IC50 = 1.8 μM) that is 28-fold selective against the related helicases RECQ1, RECQ5, and E. coli UvrD (IC50s ≥ 50 μM).{24550} At 25-50 μM, ML-216 has been shown to dose-dependently inhibit the proliferation of BLM-expressing PSNF5 fibroblast cells but not BLM-deficient PSNG13 fibroblast cells.{24550}  

 

Add to quotes
SKU: - Category:

Description

The first identified small molecule inhibitor of BLM helicase (IC50 = 1.8 μM) that is 28-fold selective against the related helicases RECQ1, RECQ5, and E. coli UvrD (IC50s ≥ 50 μM); 25-50 μM dose-dependently inhibits the proliferation of BLM-expressing PSNF5 fibroblast cells

Formal name: N-[4-fluoro-3-(trifluoromethyl)phenyl]-N’-[5-(4-pyridinyl)-1,3,4-thiadiazol-2-yl]-urea

Synonyms:  CID-49852229

Molecular weight: 383.3

CAS: 1430213-30-1

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Nucleic Acid Turnover/Signaling||Research Area|Cancer|DNA Damage and Repair

Related products

  • 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
    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
    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
    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