A selective cathepsin B inhibitor (Kis = 0.0087

CA-074 – 1 mg

Brand:
Cayman
CAS:
134448-10-5
Storage:
-20
UN-No:
Non-Hazardous - /

CA-074 is a selective epoxysuccinyl peptide inhibitor of the cysteine protease cathepsin B (Kis = 0.0087, 75, and 233 μM for rat cathepsin B, H, and L, respectively).{14250} It inhibits degradation of DQ-collagen IV and DQ-collagen I in 4T1.2 breast cancer cells in a concentration-dependent manner and reduces the number of lung and bone metastasis in a 4T1.2 mouse xenograft model, without affecting primary tumor growth, when administered at a dose of 50 mg/kg.{41935} CA-074 (0.1 and 0.2 mg/animal per day) reduces mercury-induced increases in expression of TNF-α, IL-1β, and the inflammasome component NRLP3 and decreases the severity of mercury-induced skin induration in mice.{41937} CA-074 also reduces ischemia-induced hippocampal neuron cell death in monkeys.{41936}  

 

Available on backorder

Add to quotes
SKU: 24679 - 1 mg Category:

Description

A selective cathepsin B inhibitor (Kis = 0.0087, 75, and 233 μM for rat cathepsin B, H, and L, respectively); inhibits degradation of DQ-collagen IV and DQ-collagen I in 4T1.2 breast cancer cells; reduces the number of lung and bone metastasis in a 4T1.2 mouse xenograft model at 50 mg/kg; reduces mercury-induced increases in expression of TNF-α, IL-1β, and the inflammasome component NRLP3 and decreases the severity of mercury-induced skin induration in mice at 0.1 and 0.2 mg/kg; reduces ischemia-induced hippocampal neuron cell death in monkeys

Formal name: N-[[3S-[(propylamino)carbonyl]-2S-oxiranyl]carbonyl]-L-isoleucyl-L-proline

Synonyms: 

Molecular weight: 383.4

CAS: 134448-10-5

Purity: ≥98%

Formulation: A solid

Product Type|Biochemicals|Small Molecule Inhibitors|Peptidases & Proteases||Research Area|Cancer|Cell Migration & Metastasis||Research Area|Immunology & Inflammation||Research Area|Neuroscience|Neuroprotection|Ischemia

Related products

  • A zwitterionic glycerophospholipid commonly used in the formation of lipid monolayers

    1,2-Dipalmitoyl-sn-glycero-3-PC – 25 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 - 25 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) – 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 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