A BCL6 inhibitor (IC50 = ~35 μM); selective for BCL6 over a panel of 50 kinases at 10 μM; reduces recruitment of the BCL6 corepressor proteins SMRT and BCOR to the BCL6 target loci CDKN1A

FX1 – 25 mg

Brand:
Cayman
CAS:
1426138-42-2
Storage:
-20
UN-No:
Non-Hazardous - /

FX1 is an inhibitor of the transcription factor B cell lymphoma 6 (BCL6; IC50 = ~35 μM).{43297} It is selective for BCL6 over a panel of 50 kinases at a concentration of 10 μM. FX1 (50 μM) reduces recruitment of the BCL6 corepressor proteins SMRT and BCOR to the BCL6 target loci CDKN1A, CD69, and CXCR4 in a ChIP assay. It represses growth of Farage, SUDLH-6, DOHH-2, OCI-Ly7, RCK8, SUDHL-4, OCI-Ly1, and SC-1 BCL6-dependent cell lines (GI50s = 16-54 μM) but not OCI-LY1-B50, Karpas 433, OCI-Ly19, or Toledo BCL6-independent cell lines (GI50s = >125 μM). In vivo, FX1 (50 mg/kg) reduces tumor volume in an HBL-1 large B cell lymphoma mouse xenograft model.  

 

Available on backorder

Add to quotes
SKU: 23908 - 25 mg Category:

Description

A BCL6 inhibitor (IC50 = ~35 μM); selective for BCL6 over a panel of 50 kinases at 10 μM; reduces recruitment of the BCL6 corepressor proteins SMRT and BCOR to the BCL6 target loci CDKN1A, CD69, and CXCR4 in a ChIP assay at 50 μM; represses growth of Farage, SUDLH-6, DOHH-2, OCI-Ly7, RCK8, SUDHL-4, OCI-Ly1, and SC-1 BCL6-dependent cell lines (GI50s = 16-54 μM); reduces tumor volume in an HBL-1 large B cell lymphoma mouse xenograft model at 50 mg/kg

Formal name: (5Z)-5-(5-chloro-1,2-dihydro-2-oxo-3H-indol-3-ylidene)-4-oxo-2-thioxo-3-thiazolidinepropanoic acid

Synonyms: 

Molecular weight: 368.8

CAS: 1426138-42-2

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors||Research Area|Cancer|Transcription Factors

Related products

  • 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
  • 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
    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
  • 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