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Merck
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文件

PZ0242

Sigma-Aldrich

PF-06658607

≥98% (HPLC)

别名:

Probe 4, 依鲁替尼, （R）-1-（3-（4-氨基-3-（4-（3-乙炔基苯氧基）苯基）-1H-吡唑并[3,4-d]嘧啶-1-基）哌啶-1-基）丙-2-烯-1-酮

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About This Item

经验公式（希尔记法）:
C27H24N6O2
CAS号:
1621002-24-1
分子量:
464.52
分類程式碼代碼:
12352200
NACRES:
NA.77

品質等級

100

化驗

≥98% (HPLC)

形狀

powder

顏色

white to beige

溶解度

DMSO: 20 mg/mL, clear

儲存溫度

room temp

應用

PF-06658607 已用于评价共价激酶抑制剂的全蛋白选择性。

生化／生理作用

PF-06658607 是一种烷基化不可逆的 Brutons 酪氨酸激酶（BTK）抑制剂，可与 ATP 结合袋中的活性位点半胱氨酸残基共价反应。PF-06658607 已被用作蛋白质组分析的探针，以鉴定脱靶结合底物。炔烃部分允许通过铜催化的点击化学方法添加基于叠氮化物的检测探针。

象形圖

Exclamation mark
GHS07

訊號詞

Warning

危險聲明

H315,H319,H335

危險分類

Eye Irrit. 2 - Skin Irrit. 2 - STOT SE 3

標靶器官

Respiratory system

儲存類別代碼

11 - Combustible Solids

水污染物質分類（WGK）

WGK 3

閃點（°F）

Not applicable

閃點（°C）

Not applicable

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Bryan R Lanning et al.
Nature chemical biology, 10(9), 760-767 (2014-07-21)
Kinases are principal components of signal transduction pathways and the focus of intense basic and drug discovery research. Irreversible inhibitors that covalently modify non-catalytic cysteines in kinase active sites have emerged as valuable probes and approved drugs. Many protein classes

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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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