An ADAM10 inhibitor (IC50 = 5.3 nM); selective for ADAM10 over ADAM17

GI 254023X – 1 mg

Brand:
Cayman
CAS:
260264-93-5
Storage:
-20
UN-No:
Non-Hazardous - /

GI 254023X is an inhibitor of the metalloproteinase-disintegrin ADAM10 (IC50 = 5.3 nM).{50359} It is selective for ADAM10 over ADAM17, matrix metalloproteinase-1 (MMP-1), and MMP-3 (IC50s = 541, 108, and 187 nM, respectively), but also inhibits MMP-9 and MMP-13 (IC50s = 2.5 and 1.1 nM, respectively). GI 254023X inhibits constitutive shedding of CX3CL1, but not shedding induced by phorbol 12-myristate 13-acetate (PMA; Item No. 10008014), in COS-7 cells transfected with human chemokines (IC50s = 0.4 and >10 μM, respectively). It also inhibits constitutive, but not PMA-induced, secretion of the IL-6 receptor (IL-6R) from THP-1 macrophages (IC50s = 1.8 and >10 μM, respectively). GX 254023X (1 μM) decreases shedding of low density lipoprotein receptor-related protein 1 (LRP1) induced by amyloid-β (1-42) (Aβ42; Item No. 20574) in human brain microvessel endothelial cells (HBMECs) and increases Aβ42 transit across an in vitro blood brain barrier model in a concentration-dependent manner.{50360} In vivo, GI 254023X (200 mg/kg) reduces brain LRP1 shedding and increases plasma levels of Aβ40 in a mouse model of Alzheimer’s disease.  

 

Available on backorder

Add to quotes
SKU: 28284 - 1 mg Category:

Description

An ADAM10 inhibitor (IC50 = 5.3 nM); selective for ADAM10 over ADAM17, MMP-1 and MMP-3 (IC50s = 541, 108, and 187 nM, respectively); inhibits MMP-9 and MMP-13 (IC50s = 2.5 and 1.1 nM, respectively); inhibits constitutive, but not PMA-induced shedding of CX3CL1 in COS-7 cells transfected with human chemokines (IC50s = 0.4 and >10 μM, respectively); inhibits constitutive, but not PMA-induced, secretion of IL-6R from THP-1 macrophages (IC50s = 1.8 and >10 μM, respectively); decreases Aβ42-induced shedding of LRP1 in HBMECs; increases Aβ42 transit across an in vitro blood brain barrier model; reduces brain LRP1 shedding and increases plasma levels of Aβ40 in a mouse model of Alzheimer’s disease at 200 mg/kg

Formal name: (αR)-N-[(1S)-2,2-dimethyl-1-[(methylamino)carbonyl]propyl]-α-[(1S)-1-(formylhydroxyamino)ethyl]-benzenepentanamide

Synonyms:  GI 4023|SRI 028594

Molecular weight: 391.5

CAS: 260264-93-5

Purity: ≥98%

Formulation: A crystalline solid

Related products

  • 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
  • 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
  • CAY10512 is a substituted trans-stilbene analog of resveratrol that is 100-fold more potent as measured by antioxidant activity. The IC50 value for inhibition of TNFα-induced activation of NF-κB by CAY10512 is 0.15 µM compared to 20 µM by resveratrol.{14545}

    CAY10512 – 100 mg

    The nuclear factor-κB (NF-κB) regulates the expression of numerous genes involved in immunity and inflammation, cellular stress responses, growth, and apoptosis. Resveratrol, a polyphenolic trans-stilbene, is a known inhibitor of the activation of NF-κB and exhibits activity against a wide variety of cancer cells. CAY10512 is a substituted trans-stilbene analog of resveratrol that is 100-fold more potent as measured by antioxidant activity. The IC50 value for inhibition of TNFα-induced activation of NF-κB by CAY10512 is 0.15 µM compared to 20 µM by resveratrol.{14545}  

     

    Brand:
    Cayman
    SKU:10009536 - 100 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 – 50 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 - 50 mg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page