PIK-75 HydrochlorideCAS号: 372196-77-5分子式: C16H14BrN5O4S.HCl分子量: 488.74描述纯度储存/保存方法别名可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)参考文献
产品描述 | |
描述 |
PIK-75是一种p110α抑制剂,IC50为5.8 nM (比作用于p110β效果强200倍),亚型特异性的突变体在Ser773,也有效抑制DNA-PK,IC50为2 nM。与纯化的p110α结合, PIK-75是非竞争性抑制剂,Ki 为 36 nM。PIK-75也有效抑制DNA-PK,IC50为2 nM。 PIK-75 (1 μM) 通过显著降低无刺激的非哮喘气道平滑肌细胞(ASM),哮喘 ASM细胞 , 和肺成纤维细胞的线粒体活性,降低细胞寿命。 |
纯度 |
>98%
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储存/保存方法 |
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
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基本信息 | |
别名 |
PIK-75
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可溶性/溶解性 |
DMSO: ≥ 30 mg/mL
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生物活性 | |
靶点 |
DNA-PK ,p110α ,p110γ ,p110δ
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In vitro(体外研究) |
PIK-75 shows the impressive potency and isoform selectivity at p110α while the corresponding IC50 values are 1300 nM, 76 nM and 510 nM for other PI3K isoforms, p110β, -γ, and -δ, respectively. Furthermore, when binding to purified p110α, PIK-75 is a noncompetitive inhibitor with respect to ATP with Ki of 36 nM and competitive with respect to the substrate PI with Ki of 2.3 nM. PIK-75 also shows potent inhibition of DNA-PK. PIK-75 (1 μM) reduces cell survival by significantly decreasing mitochondrial activity in unstimulated nonasthmatic airway smooth muscle (ASM) cells, asthmatic ASM cells, and lung fibroblasts. While in TGFβ-stimulated ASM cells, PIK75 only decreases mitochondrial activity in asthmatic cells without effects in nonasthmatic cells. A recent study shows that PIK-75 (10 nM) inhibits TNF-α-induced CD38 mRNA expression and significantly attenuates of TNF-α-induced ADP-ribosyl cyclase activity in human airway smooth muscle cells.
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In vivo(体内研究) |
In the ErbB3WT tumor model, PIK-75 reduces in vitro chemotactic response to HRGβ1 and lowers pAkt levels by 40%. Besides, PIK-75 significantly reduces tumor cell motility and in vivo invasion in ErbB3WT primary tumors. In the CD1 male mice, PIK-75 leads to serious impairments in the insulin tolerance test (ITT) and glucose tolerance test (GTT), and an increase in glucose production during a pyruvate tolerance test (PTT).
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参考文献 | |
参考文献 |
分子结构图