An inhibitor of ABHD6 (IC50 = 0.21 nM in Neuro2A cells); inhibits ABHD6 in a 2-AG hydrolysis assay (IC50 = 13.6 nM for the mouse recombinant enzyme expressed in HEK293T cells); selective for ABHD6 over DAGLβ at 1 µM but inhibits LYPLA1 and LYPLA2 at 10 µM; inhibits ABHD6 activity in mouse liver and brain in vivo at 5-10 and ~40 mg/kg

KT185 – 25 mg

Brand:
Cayman
CAS:
1472640-86-0
Storage:
-20
UN-No:
Non-Hazardous - /

KT185 is an orally bioavailable inhibitor of α/β-hydrolase domain-containing protein 6 (ABHD6) with an IC50 value of 0.21 nM in a competitive activity-based protein profiling assay using Neuro2A membranes.{24855} It inhibits ABHD6 in a 2-arachidonoyl glycerol (2-AG; Item No. 62160) hydrolysis assay (IC50 = 13.6 nM for the mouse recombinant enzyme expressed in HEK293T cells). KT185 is selective for ABHD6 over diacylglycerol lipase β (DAGLβ) at 1 µM but inhibits lysophospholipase 1 (LYPLA1) and LYPLA2 at 10 µM. It inhibits ABHD6 activity in mouse liver and brain in vivo when administered at doses of 5-10 and approximately 40 mg/kg, respectively, without inhibiting fatty acid amide hydrolase (FAAH) in the brain. KT185 inhibits increases in the frequency of spontaneous inhibitory post-synaptic currents (sIPSCs) induced by nicotine (Item No. 29138) in the rat ventral tegmental area (VTA) but does not reduce nicotine self-administration in rats when administered intracerebroventricularly at a dose of 200 µg.{51209} It has been used as a negative control for the off-target effect of the DAGL inhibitor KT172 (Item No. 19112) on ABHD6.  

 

Available on backorder

Add to quotes
SKU: - Category:

Description

An inhibitor of ABHD6 (IC50 = 0.21 nM in Neuro2A cells); inhibits ABHD6 in a 2-AG hydrolysis assay (IC50 = 13.6 nM for the mouse recombinant enzyme expressed in HEK293T cells); selective for ABHD6 over DAGLβ at 1 µM but inhibits LYPLA1 and LYPLA2 at 10 µM; inhibits ABHD6 activity in mouse liver and brain in vivo at 5-10 and ~40 mg/kg, respectively; inhibits nicotine-induced increases in sIPSC frequency in the rat VTA but does not reduce nicotine self-administration in rats at 200 µg; has been used as a negative control for the off-target effect of KT172 on ABHD6

Formal name: [4′-[1-[(2-phenyl-1-piperidinyl)carbonyl]-1H-1,2,3-triazol-4-yl][1,1′-biphenyl]-3-yl]-1-piperidinyl-methanone

Synonyms: 

Molecular weight: 519.6

CAS: 1472640-86-0

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Glycerolipid Lipases||Research Area|Lipid Biochemistry|Glycerolipids|Lipases||Research Area|Neuroscience|Behavioral Neuroscience|Addiction Research||Research Area|Neuroscience|Cannabinoid Research|Endocannabinoids

Related products

  • 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 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 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 zwitterionic glycerophospholipid commonly used in the formation of lipid monolayers

    1,2-Dipalmitoyl-sn-glycero-3-PC – 250 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 - 250 mg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page