TPPB

TPPB 是可渗透细胞的苯并内酰胺衍生蛋白的激酶 C 激活剂,Ki 值为11.9 nM。

CAS号

497259-23-1

分子式

C27H30F3N3O3

主要靶点

PKC

仅限科研使用

Cat No : CM11435

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Synonyms



产品信息

TPPB is a kinase C activator of cell-permeable benzolactam-derived protein (Ki: 11.9 nM).

CAS号 497259-23-1
分子式 C27H30F3N3O3
主要靶点 PKC
主要通路 表观遗传|细胞骨架
分子量 501.54
纯度 98.00%, 此纯度可做参考,具体纯度与批次有关系,可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名

靶点活性

PKC:11.9 nM (ki)

体内活性

TPPB is evaluated for the induction of hyperplasia displays a modest response at 300 μg after topical application to the shaved backs of outbred Sencar mice and [1].

体外活性

TPPB inhibits the activation of caspase-3 induced by Aβ25-35. TPPB could increase the phosphorylation of Akt, PKC, MARCKS, and MAPK, which are inhibited by Aβ25-35 treatment. TPPB at a concentration of 1 μM could antagonize Aβ25-35 induced cell damage. By the use of a cell line derived from an Alzheimer’s disease patient, significant enhancement of sAPPα secretion is achieved at 1 μM concentration for TPPB. TPPB has a role against Aβ25-35-induced neurotoxicity in PC12 cells [1][2].

溶解度

DMSO:125 mg/mL (249.23 mM),Sonification is recommended.

参考文献

1.Kozikowski AP, et al. New amide-bearing benzolactam-based protein kinase C modulators induce enhanced secretion of the amyloid precursor protein metabolite sAPPalpha. J Med Chem. 2003 Jan 30;46(3):364-73.
2.Yang HQ, et al. Neuroprotective effects of new protein kinase C activator TPPB against Aβ25-35 induced neurotoxicity in PC12 cells. Neurochem Res. 2012 Oct;37(10):2213-21.

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