An inhibitor of STK16 (IC50 = 295 nM); selective for STK16 over mTOR

STK16-IN-1 – 50 mg

Brand:
Cayman
CAS:
1223001-53-3
Storage:
-20
UN-No:
Non-Hazardous - /

STK16-IN-1 is an inhibitor of the serine/threonine kinase STK16 (IC50 = 295 nM).{46178} It is selective for STK16 over mTOR, PI3Kδ, and PI3Kγ in an enzyme assay (IC50s = 5,560, 856, and 867 nM, respectively) and over 440 additional kinases in a KinomeScan profiling assay. It decreases the growth of MCF-7 cells (GI50 = ~10 µM) and increases the number of binucleated cells. STK16-IN-1 (2.5-5 µM) potentiates the antiproliferative effects of colchicine (Item No. 9000760), paclitaxel (Item No. 10461), doxorubicin (Item No. 15007), and cisplatin (Item No. 13119) in MCF-7 cells.  

 

Available on backorder

Add to quotes
SKU: 27370 - 50 mg Category:

Description

An inhibitor of STK16 (IC50 = 295 nM); selective for STK16 over mTOR, PI3Kδ, and PI3Kγ (IC50s = 5,560, 856, and 867 nM, respectively, in an enzyme assay) and over 440 additional kinases in a KinomeScan profiling assay; decreases the growth of MCF-7 cells (GI50 = ~10 µM); potentiates the antiproliferative effects of colchicine, paclitaxel, doxorubicin, and cisplatin in MCF-7 cells at 2.5-5 µM

Formal name: 1-(4-fluoro-3-methylphenyl)-1,7-dihydro-2H-pyrrolo[2,3-h]-1,6-naphthyridin-2-one

Synonyms: 

Molecular weight: 293.3

CAS: 1223001-53-3

Purity: ≥98%

Formulation: A solid

Product Type|Biochemicals|Kinase Inhibitors|Other Serine/Threonine Kinases||Research Area|Cancer|Cell Signaling

Related products

  • PtdIns-(3

    PtdIns-(3,4,5)-P3-biotin (sodium salt) – 10 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 - 10 µg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page
  • 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
    Add to quotes
    View product page
  • A powerful effector in both the TetR and revTetR transcriptional regulator systems

    Anhydrotetracycline (hydrochloride) – 250 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 - 250 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 – 5 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 - 5 mg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page