An inhibitor of PIKFYVE (IC50 = 5.2 nM); selectively inhibits IL-12 family inflammatory cytokine production (IC50s = 8

APY0201 – 1 mg

Brand:
Cayman
CAS:
1232221-74-7
Storage:
-20
UN-No:
Non-Hazardous - /

APY0201 is an inhibitor of FYVE finger-containing phosphoinositide kinase (PIKFYVE; IC50 = 5.2 nM) that selectively inhibits interleukin-12 (IL-12) family inflammatory cytokine production (IC50s = 8, 99, and >10,000 nM for IL-12p70, IL-12p40, and TNF-α in stimulated human peripheral blood mononuclear cells (PBMCs)).{40423} It is selective for PIKFYVE over a panel of 137 G protein-coupled receptors, enzymes, ion channels, transporters, and other kinases only exhibiting >50% inhibition at lymphocyte-oriented kinase (LOK) and inositol-tetrakisphosphate 1 kinase (ITPK1) at a concentration of 300 nM. APY0201 inhibits Il-12p70 production ex vivo in murine plasma and reduces colonic inflammation in a mouse Il-10-/- cell transfer model of inflammatory bowel disease in a dose-dependent manner.  

 

Available on backorder

Add to quotes
SKU: 9001589 - 1 mg Category:

Description

An inhibitor of PIKFYVE (IC50 = 5.2 nM); selectively inhibits IL-12 family inflammatory cytokine production (IC50s = 8, 99, and >10,000 nM for IL-12p70, IL-12p40, and TNF-α in stimulated human PBMCs); selective for PIKFYVE over a panel of 137 G protein-coupled receptors, enzymes, ion channels, and transporters, and other kinases only exhibiting >50% inhibition at LOK and ITPK1 at a concentration of 300 nM; inhibits Il-12p70 production ex vivo in murine plasma and reduces colonic inflammation in a mouse Il-10-/- cell transfer model of inflammatory bowel disease in a dose-dependent manner

Formal name: 2-[7-(4-morpholinyl)-2-(4-pyridinyl)pyrazolo[1,5-a]pyrimidin-5-yl]hydrazone, 3-methyl-benzaldehyde

Synonyms: 

Molecular weight: 413.5

CAS: 1232221-74-7

Purity: ≥98%

Formulation: A crystalline solid

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
  • 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 small molecule activator of stem cell renewal that allows the propagation of OG2 mES cells for at least 10 passages in an undifferentiated state; activity is mediated by the combined inhibition of RasGAP and ERK1 with Kd values of 98 and 212 nM

    SC-1 – 1 mg

    The maintenance of embryonic stem cells in culture typically requires feeder cells and various exogenous factors found in serum. Murine embryonic stem (mES) cells can be maintained in the absence of feeder cells and serum but require the leukemia inhibitor factor (LIF) and bone morphogenic protein (BMP) to prevent differentiation and promote self-renewal. SC-1 is a small molecule activator of stem cell renewal that allows the propagation of OG2 mES cells for at least 10 passages in an undifferentiated state.{14533} The activity of SC-1 is mediated by the combined inhibition of RasGAP and ERK1 with Kd values of 98 and 212 nM, respectively.{14533} Inhibition of RasGAP increases Ras signaling via the PI3-kinase pathway which promotes self-renewal, whereas inhibition of ERK blocks differentiation.  

     

    Brand:
    Cayman
    SKU:10009557 - 1 mg

    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