A broad-spectrum inhibitor of TACE

TAPI-2 – 1 mg

Brand:
Cayman
CAS:
187034-31-7
Storage:
-20
UN-No:
Non-Hazardous - /

The extracellular domains of many different types of transmembrane proteins, including growth factors, growth factor receptors and cell adhesion molecules, are proteolytically released (shed) in response to environmental cues. TNF protease inhibitor 2 (TAPI-2) is a broad-spectrum inhibitor of TNF-α converting enzyme (TACE), other ADAMs (a disintegrin and metalloproteinases), and other matrix metalloproteinases. It inhibits phorbol-12-myristate-13-acetate-induced (PMA) shedding of various cell surface proteins, such as TGF-α, β amyloid precursor protein, L-selectin, and IL-6 receptor α subunit, with an IC50 value of 10 µM.{23493} TAPI-2 inhibits ADAM8, 10, 12, and TACE with Ki values of 10, 3, 100, and 0.12 µM, respectively.{23492} In T4-2 breast cancer cells, 20 µM TAPI-2 prevented mobilization of the growth factors TGF-α and amphiregulin leading to reversion of the malignant cellular phenotype.{23494}  

 

Add to quotes
SKU: - Category:

Description

A broad-spectrum inhibitor of TACE, other ADAMs, and other MMPs; inhibits PMA-induced shedding of various cell surface proteins, such as TGF-α, βAPP, L-selectin, IL-6 receptor α subunit (IC50 = 10 µM); prevents mobilization of the growth factors TGF-α and amphiregulin in culture leading to reversion of malignant breast cancer cell phenotype

Formal name: N-[2-[2-(hydroxyamino)-2-oxoethyl]-4-methyl-1-oxopentyl]-3-methyl-L-valyl-N-(2-aminoethyl)-L-alaninamide

Synonyms:  TNF Protease Inhibitor 2

Molecular weight: 415.5

CAS: 187034-31-7

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|MMPs||Research Area|Cancer||Research Area|Cell Biology|Proteolysis|Cytosolic & Secreted Proteases

Related products

  • 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 – 10 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 - 10 mg

    Available on backorder

    Add to quotes
    View product page
  • PtdIns-(3

    PtdIns-(3,4,5)-P3-biotin (sodium salt) – 25 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 - 25 µg

    Available on backorder

    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
    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
    View product page