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Merck
CN

06566

(4-脒苯基)甲磺酰氟盐酸盐 盐酸盐

≥97.0% (AT)

别名:

p-APMSF, 对脒苯基甲磺酰氯盐酸盐 盐酸盐

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关于此项目

经验公式(希尔记法):
C8H9FN2O2S · HCl
化学文摘社编号:
分子量:
252.69
PubChem Substance ID:
UNSPSC Code:
12352202
Beilstein/REAXYS Number:
9083148
MDL number:
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biological source

synthetic

assay

≥97.0% (AT)

form

powder

mp

~205 °C (dec.)

storage temp.

−20°C

SMILES string

Cl[H].NC(=N)c1ccc(CS(F)(=O)=O)cc1

InChI

1S/C8H9FN2O2S.ClH/c9-14(12,13)5-6-1-3-7(4-2-6)8(10)11;/h1-4H,5H2,(H3,10,11);1H

InChI key

KHLLRHIUKOJXLL-UHFFFAOYSA-N

Application

APMSF was used to study the glucagon-receptor interaction; inhibition of cAMP formation led to the conclusion that there was a previously unexpected serine residue in the active site which may operate on the receptor by a mechanism similar to serine proteases.

Biochem/physiol Actions

具有赖氨酸或精氨酸底物特异性的丝氨酸蛋白酶的不可逆抑制剂。有效浓度是10-100 μM。
具有赖氨酸或精氨酸底物特异性的丝氨酸蛋白酶的不可逆抑制剂。有效浓度是10-100 μM。常用于表征新发现的蛋白酶。

Other Notes

An irreversible inhibitor of serine proteases

存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

ppe

Eyeshields, Gloves, type N95 (US)

法规信息

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历史批次信息供参考:

分析证书(COA)

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C G Unson et al.
Proceedings of the National Academy of Sciences of the United States of America, 91(2), 454-458 (1994-01-18)
Several glucagon analogs containing substitutions for serine have been synthesized to assess the role of the four serine residues in the hormone. The strategic importance of His1 has been confirmed, and we have previously identified an aspartic acid critical for
R Laura et al.
Biochemistry, 19(21), 4859-4864 (1980-10-14)
p-(Amidinophenyl)methanesulfonyl fluoride (p-APMSF) has been synthesized and shown to be a specific, irreversible inhibitor of the class of plasma serine proteases which demonstrate substrate specificity for the positively charged side chains of the amino acid lysine or arginine. In equimolar
Lacramioara Ivanciu et al.
Blood, 124(11), 1705-1714 (2014-05-30)
The membrane-dependent interaction of factor Xa (FXa) with factor Va (FVa) forms prothrombinase and drives thrombin formation essential for hemostasis. Activated platelets are considered to provide the primary biological surface to support prothrombinase function. However, the question of how other
Jie Li et al.
Oncotarget, 5(4), 882-893 (2014-03-25)
Glioblastoma remains one of the deadliest of human cancers, with most patients succumbing to the disease within two years of diagnosis. The available data suggest that simultaneous inactivation of critical nodes within the glioblastoma molecular circuitry will be required for
Kazunori Suzuki et al.
The Journal of pharmacology and experimental therapeutics, 352(3), 471-479 (2014-12-20)
Phosphodiesterase 10A (PDE10A) is a cAMP/cGMP phosphodiesterase highly expressed in medium spiny neurons (MSNs) in the striatum. We evaluated the in vivo pharmacological profile of a potent and selective PDE10A inhibitor, TAK-063 (1-[2-fluoro-4-(1H-pyrazol-1-yl)phenyl]-5-methoxy-3-(1-phenyl-1H-pyrazol-5-yl)-pyridazin-4(1H)-one). TAK-063 at 0.3 and 1 mg/kg p.o.

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货号GTIN
283061-5G04061826236659

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