1050480-30-2

1050480-30-2 structure

Name: PhiKan 083
Chemical Name: PhiKan 083 hydrochloride
CAS Number: 1050480-30-2
Molecular Formula: C₁₆H₁₉ClN₂
Molecular Weight: 274.789
Catalog: Signaling Pathways Apoptosis MDM-2/p53
Create Date: 2018-02-10 17:04:15
Modify Date: 2024-01-02 12:46:38
PhiKan 083 hydrochloride is a carbazole derivative, which can stabilize Y220C (a p53 mutant), with a Kd of 167 μM measured by NMR, used for cancer research.

Name	PhiKan 083 hydrochloride
Synonyms	MFCD07168924 9H-Carbazole-3-methanamine, 9-ethyl-N-methyl-, hydrochloride (1:1) 1-(9-Ethyl-9H-carbazol-3-yl)-N-methylmethanamine hydrochloride (1:1)

Description	PhiKan 083 hydrochloride is a carbazole derivative, which can stabilize Y220C (a p53 mutant), with a Kd of 167 μM measured by NMR, used for cancer research.
Related Catalog	Signaling Pathways >> Apoptosis >> MDM-2/p53 Research Areas >> Cancer
Target	Kd: 167 μM (T-p53C-Y220C)[1]
In Vitro	PhiKan 083 hydrochloride is a stabilizer of Y220C (a p53 mutant), with a Kd of 167 μM measured by NMR. Analytical ultracentrifugation gives a Kd of 170 μM for PhiKan083, at 10°C. Isothermal titration of PhiKan083 with T-p53C-Y220C gives 1:1 stoichiometry and a Kd of 125 ± 10 μM[1]. PhiKan083 can binds with the cavity on the surface of Y220C-mutated p53[2].
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.