PhiKan 083

Modify Date: 2024-01-20 19:43:56

PhiKan 083 Structure
PhiKan 083 structure
Common Name PhiKan 083
CAS Number 880813-36-5 Molecular Weight 238.33
Density N/A Boiling Point N/A
Molecular Formula C16H18N2 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of PhiKan 083


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].

 Names

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

 PhiKan 083 Biological Activity

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
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.

 Chemical & Physical Properties

Molecular Formula C16H18N2
Molecular Weight 238.33
PSA 16.96000
LogP 4.72670
Storage condition 2-8℃

 Synonyms

PhiKan 083
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Price: ¥1375/10 mM * 1 mL in DMSO

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