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Merck
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Key Documents

SML1308

Sigma-Aldrich

KT195

≥98% (HPLC)

Sinónimos:

[4-(4′-Methoxy[1,1′-biphenyl]-4-yl)-1H-1,2,3-triazol-1-yl](2-phenyl-1-piperidinyl)-methanone

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About This Item

Fórmula empírica (notación de Hill):
C27H26N4O2
Número de CAS:
1402612-58-1
Peso molecular:
438.52
UNSPSC Code:
12352200
NACRES:
NA.77

Quality Level

100

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 5 mg/mL, clear (warmed)

storage temp.

2-8°C

Biochem/physiol Actions

KT195 is a potent (IC50 = 10 nM) and selective inhibitor of α/β-hydrolase domain-containing 6 (ABHD6), a serine hydrolase that acts as an alternative hydrolase of the endocannabinoid 2-arachidonoylglycerol (2-AG). KT195 has negligible activity against other serine hydrolases such as DAGLβ and has been used as a control probe for studies of DAGLβ as well as being a probe on its own to study ABHD6. KT195 treatment of Neuro2A cells caused significant accumulation of 2-AG. KT195 also lowered interleukin-1β (IL-1β) secretion from lipopolysaccharide-treated macrophages suggesting ABHD6 involvement in this activity as well.

pictograms

Skull and crossbones
GHS06

signalword

Danger

hcodes

H301,H413

Hazard Classifications

Acute Tox. 3 Oral - Aquatic Chronic 4

Storage Class

6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

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Contenido relacionado

Cravatt Group – Professor Product Portal

The aim of the Cravatt research group is to understand the roles that mammalian enzymes play in physiological and pathological processes and to use this knowledge to identify novel therapeutic targets for the treatment of human disease. To achieve these goals, they develop and apply new technologies that bridge the fields of chemistry and biology, ascribing to the philosophy that the most significant biomedical problems require creative multidisciplinary approaches for their solution. The group's technological innovations address fundamental challenges in systems biology that are beyond the scope of contemporary methods. For instance, enzymes are tightly regulated by post-translational events in vivo, meaning that their activity may not correlate with expression as measured by standard genomic and proteomic approaches. Considering that it is an enzyme's activity, rather than abundance that ultimately dictates its role in cell physiology and pathology, the Cravatt group has introduced a set of proteomic technologies that directly measures this parameter. These activity-based protein profiling (ABPP) methods exploit the power of chemistry to engender new tools and assays for the global analysis of enzyme activities. The enzyme activity profiles generated by ABPP constitute unique molecular portraits of cells and tissues that illuminate how metabolic and signaling networks are regulated in vivo. Additionally, by evaluating enzymes based on functional properties rather than mere abundance, ABPP acquires high-content proteomic information that is enriched in novel markers and targets for the diagnosis and treatment of human disease.

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