N-[2-oxo-2-(1,2,3,4-tetrahydronaphthalen-1-ylamino)ethyl]biphenyl-4-carboxamide

N-[2-oxo-2-(1,2,3,4-tetrahydronaphthalen-1-ylamino)ethyl]biphenyl-4-carboxamide 구조식 이미지
카스 번호:
850467-66-2
상품명:
N-[2-oxo-2-(1,2,3,4-tetrahydronaphthalen-1-ylamino)ethyl]biphenyl-4-carboxamide
동의어(영문):
CP 43;TAOK inhibitor 43;N-[2-oxo-2-(1,2,3,4-tetrahydronaphthalen-1-ylamino)ethyl]-4-phenylbenzamide;N-[2-Oxo-2-(1,2,3,4-tetrahydro-1-naphthalenylamino)ethyl]-4-biphenylcarboxamide;N-[2-oxo-2-(1,2,3,4-tetrahydronaphthalen-1-ylamino)ethyl]biphenyl-4-carboxamide;N-(2-Oxo-2-((1,2,3,4-tetrahydronaphthalen-1-yl)amino)ethyl)-[1,1'-biphenyl]-4-carboxamide;N-(2-Oxo-2-((1,2,3,4-tetrahydronaphthalen-1-yl)amino)ethyl)-[1,1'-biphenyl]-4-carboxamide;[1,1'-Biphenyl]-4-carboxamide, N-[2-oxo-2-[(1,2,3,4-tetrahydro-1-naphthalenyl)amino]ethyl]-;CP 43,TAO Kinase inhibitor-1,MAP kinase kinase kinase, MEKK, MAPKKK,CP43,CP-43,inhibit,TAO Kinase inhibitor 1,MAP3K,Inhibitor,TAO Kinase inhibitor1
CBNumber:
CB73375744
분자식:
C25H24N2O2
포뮬러 무게:
384.47
MOL 파일:
850467-66-2.mol

N-[2-oxo-2-(1,2,3,4-tetrahydronaphthalen-1-ylamino)ethyl]biphenyl-4-carboxamide 속성

끓는 점
673.2±54.0 °C(Predicted)
밀도
1.22±0.1 g/cm3(Predicted)
저장 조건
Store at -20°C
용해도
DMSO: 100 mM; Ethanol: 20 mM
물리적 상태
고체
산도 계수 (pKa)
13.08±0.46(Predicted)
색상
White to off-white

안전

N-[2-oxo-2-(1,2,3,4-tetrahydronaphthalen-1-ylamino)ethyl]biphenyl-4-carboxamide C화학적 특성, 용도, 생산

개요

Compound 43 TAO kinase inhibitor is an ATP-competitive inhibitor of the thousand-and-one amino acid kinases TAOK1 and TAOK2 (IC50s = 11 and 15 nM, respectively). It is selective for TAOK1 and TAOK2 over 62 kinases in a panel, but does inhibit TAOK3 by 87% and seven additional kinases by 21-52%. Compound 43 TAO kinase inhibitor inhibits proliferation of SK-BR-3, BT-549, and MCF-7 cells by 94, 82, and 46%, respectively, at a concentration of 10 μM. It reduces tau phosphorylation by TAOK2 at residues S262/S356 and S202/T205/S208 when used at concentrations ranging from 5 to 60 μM in a kinase assay and at residues S202/T205/S208 when used at concentrations of 5, 10, and 30 μM in HEK293 cells. Compound 43 TAO kinase inhibitor reduces tau phosphorylation of residues T123 and T427, which are phosphorylated by TAOK1 and TAOK2 in vitro and have been identified in tangles in Alzheimer’s disease brain tissue. It also reduces tau phosphorylation in cortical neurons in a transgenic mouse model of tauopathy and in induced pluripotent stem cell-derived neurons from patients with frontotemporal lobar degeneration.

용도

CP 43 is a potent TAO kinase (TAOK) inhibitor (IC50 values are 11 nM/L and 15 nM/L for TAOK1 and TAOK2, respectively). Inhibits TAOK phosphorylation and activation of JNK in vitro. Also prolongs duration of mitosis and increases mitotic cell death in the SKBR3 breast cancer cell line.

N-[2-oxo-2-(1,2,3,4-tetrahydronaphthalen-1-ylamino)ethyl]biphenyl-4-carboxamide 준비 용품 및 원자재

원자재

준비 용품


N-[2-oxo-2-(1,2,3,4-tetrahydronaphthalen-1-ylamino)ethyl]biphenyl-4-carboxamide 공급 업체

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