SML1770
PhiKan083 hydrochloride
≥98% (HPLC)
别名:
9-Ethyl-N-methyl-9H-Carbazole-3-methanamine hydrochloride, PK-083 hydrochloride, PK083 hydrochloride, PhiKan-083 hydrochloride
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关于此项目
经验公式（希尔记法）:
C16H18N2 · HCl
化学文摘社编号:
分子量:
274.79
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
产品名称
PhiKan083 hydrochloride, ≥98% (HPLC)
InChI key
IXWVUPURFWFRNE-UHFFFAOYSA-N
SMILES string
CNCC1=CC2=C(C=C1)N(CC)C3=C2C=CC=C3.[H]Cl
assay
≥98% (HPLC)
form
powder
storage condition
desiccated
color
white to beige
solubility
H2O: 2 mg/mL, clear
storage temp.
2-8°C
Quality Level
Biochem/physiol Actions
Mutant p53 stabilizer
PhiKan083 is a small molecule that binds within a cavity on the surface of Y220C-mutated p53. This mutation, which is not involved in DNA interaction, causes a destabilization of the protein. PhiKan083 binding acts to stabilize the mutant p53 and slow the rate of denaturation.
wgk
WGK 3
signalword
Warning
hcodes
Hazard Classifications
Eye Irrit. 2 - Skin Irrit. 2
存储类别
11 - Combustible Solids
flash_point_f
Not applicable
flash_point_c
Not applicable
Matthias R Bauer et al.
ACS chemical biology, 11(8), 2265-2274 (2016-06-09)
Many oncogenic mutants of the tumor suppressor p53 are conformationally unstable, including the frequently occurring Y220C mutant. We have previously developed several small-molecule stabilizers of this mutant. One of these molecules, PhiKan083, 1-(9-ethyl-9H-carbazole-3-yl)-N-methylmethanamine, binds to a mutation-induced surface crevice with
Frank M Boeckler et al.
Proceedings of the National Academy of Sciences of the United States of America, 105(30), 10360-10365 (2008-07-25)
The tumor suppressor p53 is mutationally inactivated in approximately 50% of human cancers. Approximately one-third of the mutations lower the melting temperature of the protein, leading to its rapid denaturation. Small molecules that bind to those mutants and stabilize them
Keelan Z Guiley et al.
Cancer discovery, 13(1), 56-69 (2022-10-06)
The transcription factor and tumor suppressor protein p53 is the most frequently mutated and inactivated gene in cancer. Mutations in p53 result in deregulated cell proliferation and genomic instability, both hallmarks of cancer. There are currently no therapies available that
Joana Soares et al.
Oncotarget, 7(4), 4326-4343 (2016-01-07)
Restoration of the p53 pathway, namely by reactivation of mutant (mut) p53, represents a valuable anticancer strategy. Herein, we report the identification of the enantiopure tryptophanol-derived oxazoloisoindolinone SLMP53-1 as a novel reactivator of wild-type (wt) and mut p53, using a
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