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1-(5-异喹啉磺酰基)-2-甲基哌嗪

1-(5-异喹啉磺酰基)-2-甲基哌嗪用途

蛋白激酶抑制剂H-7是蛋白激酶C(PKC)和环核苷酸依赖性蛋白激酶的有效抑制剂,PKC的Ki为6μM[1]。

1-(5-异喹啉磺酰基)-2-甲基哌嗪名称

[ CAS 号 ]:
84477-87-2

[ 中文名 ]:
1-(5-异喹啉磺酰基)-2-甲基哌嗪

[ 英文名 ]:
H-7

[英文别名 ]:

H-7
H-72HCl

1-(5-异喹啉磺酰基)-2-甲基哌嗪生物活性

[ 描述 ]:

蛋白激酶抑制剂H-7是蛋白激酶C(PKC)和环核苷酸依赖性蛋白激酶的有效抑制剂,PKC的Ki为6μM[1]。

[ 相关类别 ]:

信号通路 >> 表观遗传学 >> PKC

研究领域 >> 癌症

信号通路 >> TGF-beta/Smad 信号通路 >> PKC

[ 靶点 ]

PKC:6 μM (Ki)

[参考文献]

[1]. Hidaka H, et, al. Isoquinolinesulfonamides, novel and potent inhibitors of cyclic nucleotide dependent protein kinase and protein kinase C. Biochemistry. 1984 Oct 9;23(21):5036-41.

1-(5-异喹啉磺酰基)-2-甲基哌嗪物理化学性质

[ 密度 ]:
1.277 g/cm3

[ 沸点 ]:
495.3ºC at 760 mmHg

[ 熔点 ]:
114 °C

[ 分子式 ]:
C₁₄H₁₇N₃O₂S

[ 分子量 ]:
291.36900

[ 闪点 ]:
253.3ºC

[ 精确质量 ]:
291.10400

[ PSA ]:
70.68000

[ LogP ]:
2.56470

[ 外观性状 ]:
白色粉末

[ 折射率 ]:
1.652

[ 储存条件 ]:
2-8°C

1-(5-异喹啉磺酰基)-2-甲基哌嗪MSDS

1-(5-异喹啉磺酰基)-2-甲基哌嗪毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: TL9305000

CHEMICAL NAME :: Piperazine, 1-(5-isoquinolinylsulfonyl)-2-methyl-

CAS REGISTRY NUMBER :: 84477-87-2

LAST UPDATED :: 199612

DATA ITEMS CITED :: 1

MOLECULAR FORMULA :: C14-H17-N3-O2-S

MOLECULAR WEIGHT :: 291.40

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 94 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: EJCTEA European Journal of Cancer Part A. (Pergamon Press, c/o Elsevier Science, 660 White Plains Rd., Tarrytown, NY 10591) V.28A(4/5)- 1992- Volume(issue)/page/year: 30A,525,1994

1-(5-异喹啉磺酰基)-2-甲基哌嗪安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 危险品运输编码 ]:
NONH for all modes of transport

[ WGK德国 ]:
3

[ RTECS号 ]:
TL9305000

[ 海关编码 ]:
2935009090

1-(5-异喹啉磺酰基)-2-甲基哌嗪合成路线

1-(5-异喹啉磺酰基)-2-甲基哌嗪上下游产品

1-(5-异喹啉磺酰基)-2-甲基哌嗪上游产品

1-(5-异喹啉磺酰基)-2-甲基哌嗪下游产品

1-(5-异喹啉磺酰基)-2-甲基哌嗪海关

[ 海关编码 ]: 2935009090

[ 中文概述 ]:
2935009090 其他磺（酰）胺. 增值税率:17.0% 退税率:9.0% 监管条件:无最惠国关税:6.5% 普通关税:35.0%

[ 申报要素 ]: 品名, 成分含量, 用途

[ Summary ]:
2935009090 other sulphonamides VAT:17.0% Tax rebate rate:9.0% Supervision conditions:none MFN tariff:6.5% General tariff:35.0%

1-(5-异喹啉磺酰基)-2-甲基哌嗪文献

Protein kinase A stimulates Kv7.1 surface expression by regulating Nedd4-2-dependent endocytic trafficking.

Am. J. Physiol. Cell Physiol. 309 , C693-706, (2015)

The potassium channel Kv7.1 plays critical physiological roles in both heart and epithelial tissues. In heart, Kv7.1 and the accessory subunit KCNE1 forms the slowly activating delayed-rectifier potas...

Rho kinase inhibition by fasudil in the striatal 6-hydroxydopamine lesion mouse model of Parkinson disease.

J. Neuropathol. Exp. Neurol. 73(8) , 770-9, (2014)

Chronic degeneration of nigrostriatal projections, followed by nigral dopaminergic cell death, is a key feature of Parkinson disease (PD). This study examines the neuroprotective potential of the rho ...

Co-receptors are dispensable for tethering receptor-mediated phagocytosis of apoptotic cells.

Cell Death Dis. 6 , e1772, (2015)

During efferocytosis, phagocytic cells recognize dying cells by receptors binding to ligands specifically exposed on apoptotic cells. Multiple phagocytic receptors and some of their signaling pathways...

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