A purine derivative; induces differentiation or dedifferentiation

Reversine – 25 mg

Brand:
Cayman
CAS:
656820-32-5
Storage:
-20
UN-No:
Non-Hazardous - /

Reversine is a 2,6-disubstituted purine derivative that was originally found to induce dedifferentiation of C2C12 culture myoblast cells into stem cell progenitors when used at a concentration of 5 µM for four days.{12913} Depending on cell type, reversine promotes either differentiation or dedifferentiation. For example, in NT2 neuronal and HL-60 human promyelocytic leukemia cells, it induces differentiation.{38283} It inhibits the Aurora A, B, and C kinases with IC50 values of 98-876 nM and acts as an antagonist at the adenosine A3 receptor with a Ki value of 0.66 µM.{38283,13281,38284} Reversine is also used for studies of chromosome segregation. It inhibits the mitotic spindle checkpoint enzyme MPS1 with IC50 values of 6 and 2.8 nM for its kinase domain and full-length version, respectively).{38284} Reversine induces autophagy in WRO human follicular thyroid cancer cells and decreases Akt/mTOR signaling.{34281}  

 

Available on backorder

Add to quotes
SKU: 10004412 - 25 mg Category:

Description

A purine derivative; induces differentiation or dedifferentiation, depending on cell type; inhibits the Aurora A, B, and C kinases with IC50 values of 98-876 nM; A3 receptor antagonist (Ki = 0.66 µM); inhibits MPS1 (IC50s = 6 and 2.8 nM for its kinase domain and full-length version, respectively); induces autophagy in WRO human follicular thyroid cancer cells; decreases Akt/mTOR signaling,

Formal name: N6-cyclohexyl-N2-[4-(4-morpholinyl)phenyl]-9H-purine-2,6-diamine

Synonyms: 

Molecular weight: 393.5

CAS: 656820-32-5

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|Aurora||Product Type|Biochemicals|Kinase Inhibitors|Other Non-Receptor Tyrosine Kinases||Product Type|Biochemicals|Kinase Inhibitors|Other Serine/Threonine Kinases||Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Autophagy||Research Area|Cancer|Cell Signaling|PI3K/Akt/mTOR Signaling||Research Area|Cell Biology|Cell Cycle||Research Area|Cell Biology|Cell Signaling|PI3K/Akt/mTOR Signaling||Research Area|Cell Biology|Cytoskeleton & Motor Proteins||Research Area|Cell Biology|Endomembrane System & Vesicular Trafficking|Autophagy||Research Area|Cell Biology|Stem Cell Research|Differentiation

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
  • CAY10512 is a substituted trans-stilbene analog of resveratrol that is 100-fold more potent as measured by antioxidant activity. The IC50 value for inhibition of TNFα-induced activation of NF-κB by CAY10512 is 0.15 µM compared to 20 µM by resveratrol.{14545}

    CAY10512 – 10 mg

    The nuclear factor-κB (NF-κB) regulates the expression of numerous genes involved in immunity and inflammation, cellular stress responses, growth, and apoptosis. Resveratrol, a polyphenolic trans-stilbene, is a known inhibitor of the activation of NF-κB and exhibits activity against a wide variety of cancer cells. CAY10512 is a substituted trans-stilbene analog of resveratrol that is 100-fold more potent as measured by antioxidant activity. The IC50 value for inhibition of TNFα-induced activation of NF-κB by CAY10512 is 0.15 µM compared to 20 µM by resveratrol.{14545}  

     

    Brand:
    Cayman
    SKU:10009536 - 10 mg

    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) – 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
    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