A KDM2/7 inhibitor (IC50s = 6.8

TC-E 5002 – 50 mg

Brand:
Cayman
CAS:
1453071-47-0
Storage:
-20
UN-No:
Non-Hazardous - /

TC-E 5002 is an inhibitor of the histone lysine demethylase (KDM) subfamily KDM2/7 (IC50s = 6.8, 0.2, and 1.2 µM for KDM2A, KDM7A, and KDM7B, respectively).{39306} It is selective for the KDM2/7 subfamily over KDM4A, KDM4C, KDM5A, and KDM6A/UTX (IC50s = >120, 83, 55, and 100 µM, respectively). It inhibits the growth of N2a, KYSE150, and HeLa cells with GI50 values of 86, 16, and 40 µM, respectively, which are in the range where it increases H3K27me2 levels in KYSE150 and HeLa cells. TC-E 5002 decreases gene expression of E2F1, a transcription factor activated by KDM7B that leads to progression of the cell cycle. In addition, TC-E 5002 treatment leads to cell cycle arrest at the G0/G1 phase in KYSE150 and HeLa cells.  

 

Available on backorder

Add to quotes
SKU: - Category:

Description

A KDM2/7 inhibitor (IC50s = 6.8, 0.2, and 1.2 µM for KDM2A, KDM7A, and KDM7B, respectively); selective for the KDM2/7 subfamily over KDM4A, KDM4C, KDM5A, and KDM6A/UTX (IC50s = >120, 83, 55, and 100 µM, respectively); inhibits growth of N2a, KYSE150, and HeLa cells (GI50s = 86, 16, and 40 µM, respectively); increases H3K27me2 levels, decreases gene expression of E2F1, and leads to cell cycle arrest in the G0/G1 phase in vitro,,

Formal name: N-(9-cyclopropyl-1-oxononyl)-N-hydroxy-β-alanine

Synonyms: 

Molecular weight: 285.4

CAS: 1453071-47-0

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Demethylases||Research Area|Cancer|Cell Cycle|G1||Research Area|Cancer|Transcription Factors

Related products

  • 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 – 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
  • 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 powerful effector in both the TetR and revTetR transcriptional regulator systems

    Anhydrotetracycline (hydrochloride) – 100 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 - 100 mg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page