| Bioactivity | TPPB is a cell-permeable benzolactam-derived protein kinase C (PKC) activator with a Ki of 11.9 nM. | ||||||||||||
| Invitro | By 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 (Compound 5e)[1]. TPPB has a role against Aβ25-35-induced neurotoxicity in PC12 cells. TPPB at concentration of 1 μM could antagonize Aβ25-35 induced cell damage. TPPB could increase the phosphorylation of Akt, PKC, MARCKS and MAPK, which are inhibited by Aβ25-35 treatment. TPPB inhibits the activation of caspase-3 induced by Aβ25-35[2]. | ||||||||||||
| In Vivo | TPPB is evaluated for induction of hyperplasia after topical application to the shaved backs of outbred Sencar mice and shows a modest response at 300 μg[1]. | ||||||||||||
| Name | TPPB | ||||||||||||
| CAS | 497259-23-1 | ||||||||||||
| Formula | C27H30F3N3O3 | ||||||||||||
| Molar Mass | 501.54 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. |