880813-36-5

880813-36-5 structure

Name: PhiKan 083
Chemical Name: 1-(9-Ethyl-9H-carbazol-3-yl)-N-methylmethanamine hydrochloride (1 :1)
CAS Number: 880813-36-5
Molecular Formula: C₁₆H₁₈N₂
Molecular Weight: 238.33
Catalog: Signaling Pathways Apoptosis MDM-2/p53
Create Date: 2017-03-25 17:52:05
Modify Date: 2024-01-20 19:43:56
PhiKan 083 is a carbazole derivative, which binds to the surface cavity and stabilizes Y220C (a p53 mutant), with a Kd of 167 μM measured by NMR[1], and a relative binding affinity (Kd) of 150 μM in Ln229 cells[3].

Name	1-(9-Ethyl-9H-carbazol-3-yl)-N-methylmethanamine hydrochloride (1 :1)
Synonyms	PhiKan 083

Description	PhiKan 083 is a carbazole derivative, which binds to the surface cavity and stabilizes Y220C (a p53 mutant), with a Kd of 167 μM measured by NMR[1], and a relative binding affinity (Kd) of 150 μM in Ln229 cells[3].
Related Catalog	Signaling Pathways >> Apoptosis >> MDM-2/p53 Research Areas >> Cancer
Target	Kd: 167 μM (p53-Y220C)[1], 150 μM (p53Y220C, in Ln229 cells)[3]
In Vitro	PhiKan 083 is a carbazole derivative, which binds to the surface cavity and stabilizes Y220C (a p53 mutant), with a Kd of 167 μM measured by NMR[1], shows a relative binding affinity (Kd) of 150 μM for p53Y220C in Ln229 cells[3]. PhiKan083 slows down its thermal denaturation rate[2]. PhiKan 083 (125 μM) reduces the cell viability of engineered variants of Ln229 cells. PhiKan 083 (100 μM) in conbination with doxorubicin (1 μM) enhances the pro-apoptotic activity in all variants of Ln229 cells (p535, p53Y220C, p53G245S, p53R282W)[3].
References	[1]. Boeckler FM, et al. Targeted rescue of a destabilized mutant of p53 by an in silico screened drug. Proc Natl Acad Sci U S A. 2008 Jul 29;105(30):10360-5. [2]. Rauf SM, et al. Effect of Y220C mutation on p53 and its rescue mechanism: a computer chemistry approach. Protein J. 2013 Jan;32(1):68-74. [3]. Paulmurugan R, et al. A protein folding molecular imaging biosensor monitors the effects of drugs that restore mutant p53 structure and its downstream function in glioblastoma cells. Oncotarget. 2018 Apr 20;9(30):21495-21511.