1-(5-异喹啉磺酰基)哌嗪盐酸盐

• 常用名: 1-(5-异喹啉磺酰基)哌嗪盐酸盐
• 英文名: HA-100 hydrochloride
• CAS号: 141543-63-7
• 分子量: 313.80300
• 密度: N/A
• 沸点: 497.4ºC at 760 mmHg
• 分子式: C₁₃H₁₆ClN₃O₂S
• 熔点: 252-254ºC
• 闪点: 254.6ºC

1-(5-异喹啉磺酰基)哌嗪盐酸盐用途

HA-100盐酸盐是一种有效的蛋白激酶抑制剂,cGMP依赖性蛋白激酶(PKG)、cAMP依赖性蛋白激酶(PKA)、蛋白激酶C(PKC)和MLC激酶的IC50分别为4μM、8μM、12μM和240μM。HA-100盐酸盐也用作岩石抑制剂[1][2]。

1-(5-异喹啉磺酰基)哌嗪盐酸盐名称

• 中文名: 1-(5-异喹啉磺酰基)哌嗪盐酸盐
• 英文名: 1-(5-Isoquinolinesulfonyl)piperazine Hydrochloride

1-(5-异喹啉磺酰基)哌嗪盐酸盐生物活性

• 描述: HA-100盐酸盐是一种有效的蛋白激酶抑制剂,cGMP依赖性蛋白激酶(PKG)、cAMP依赖性蛋白激酶(PKA)、蛋白激酶C(PKC)和MLC激酶的IC50分别为4μM、8μM、12μM和240μM。HA-100盐酸盐也用作岩石抑制剂[1][2]。
• 相关类别:
  信号通路 >> 表观遗传学 >> PKC
  研究领域 >> 癌症
  信号通路 >> 细胞骨架 >> 肌球蛋白
  信号通路 >> 蛋白酪氨酸激酶 >> PKA
  信号通路 >> 干细胞及 Wnt 通路 >> PKA
  信号通路 >> 细胞周期/DNA损伤 >> 岩石
  信号通路 >> TGF-beta/Smad 信号通路 >> PKC
  信号通路 >> 干细胞及 Wnt 通路 >> 岩石
  信号通路 >> TGF-beta/Smad 信号通路 >> 岩石
• 靶点实验:

  PKG:4 μM (IC50)

  PKA:8 μM (IC50)

  PKC:12 μM (IC50)

  MLCK:240 μM (IC50)

  ROCK

• 体外研究: HA-100盐酸盐相对于ATP竞争性地抑制MLC激酶和PKC,Kis分别为61和6.5μM[1]。
• 参考文献:

  [1]. Hagiwara M, et, al. Selective modulation of calcium-dependent myosin phosphorylation by novel protein kinase inhibitors, isoquinolinesulfonamide derivatives. Mol Pharmacol. 1987 Jul;32(1):7-12.

  [2]. Yu J, et, al. Efficient feeder-free episomal reprogramming with small molecules. PLoS One. 2011 Mar 1;6(3):e17557.

1-(5-异喹啉磺酰基)哌嗪盐酸盐物理化学性质

• 沸点: 497.4ºC at 760 mmHg
• 熔点: 252-254ºC
• 分子式: C₁₃H₁₆ClN₃O₂S
• 分子量: 313.80300
• 闪点: 254.6ºC
• 精确质量: 313.06500
• PSA: 70.68000
• LogP: 2.97820
• InChIKey: MBZNIYPWRIDBOD-UHFFFAOYSA-N
• SMILES: Cl.O=S(=O)(c1cccc2cnccc12)N1CCNCC1
• 外观性状: 淡黄色固体
• 储存条件: 2-8°C，避光，干燥，密封

1-(5-异喹啉磺酰基)哌嗪盐酸盐安全信息

• 危害码 (欧洲): Xi

1-(5-异喹啉磺酰基)哌嗪盐酸盐靶点实验

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1-(5-异喹啉磺酰基)哌嗪盐酸盐英文别名

• 5-piperazin-1-ylsulfonylisoquinoline,hydrochloride