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Merck
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주요 문서

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SML2713

Sigma-Aldrich

MU1210

≥98% (HPLC)

동의어(들):

1-Methyl-4-(9-(3-(pyridin-4-yl)-phenyl)-7-oxa-2-aza-bicyclo[4.3.0]nona-1,3,5,8-tetraen-3-yl)-1H-pyrazole, 5-(1-Methyl-1H-pyrazol-4-yl)-3-(3-(pyridin-4-yl)phenyl)furo[3,2-b]pyridine, VN339

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About This Item

실험식(Hill 표기법):
C22H16N4O
CAS Number:
2275601-87-9
Molecular Weight:
352.39
UNSPSC 코드:
12352200
NACRES:
NA.77

Quality Level

100

분석

≥98% (HPLC)

양식

powder

색상

white to beige

solubility

DMSO: 2 mg/mL, clear

저장 온도

−20°C

SMILES string

CN(N=C1)C=C1C2=CC=C3C(C(C4=CC=CC(C5=CC=NC=C5)=C4)=CO3)=N2

InChI

1S/C22H16N4O/c1-26-13-18(12-24-26)20-5-6-21-22(25-20)19(14-27-21)17-4-2-3-16(11-17)15-7-9-23-10-8-15/h2-14H,1H3

InChI key

HEAGNKNMQVIVMM-UHFFFAOYSA-N

생화학적/생리학적 작용

ATP site-targeting, potent and selective inhibitor against cdc-like kinase (cdc2-like kinase) CLK1, CLK2, CLK4, and homeodomain-interacting protein kinase 2 (HIPK2), but not CLK3.
MU1210 is a potent and selective inhibitor against cdc-like kinase (cdc2-like kinase) CLK1, CLK2, CLK4 (CLK1/2/4 IC50 = 8/20/12 nM; CLK1/2/4 Ki = 84/91/23 nM by NanoBRET) and HIPK2 (IC50 = 29 nM) with good selectivity over HIPK1/3 (IC50 = 187/159 nM), DYRK1a/1b/2 (IC50 = 213/956/1309 nM), CLK3 (IC50 >3 μM) and 194 other kinases. MU1210 enhances alternative spliced MDM4-S mRNA (10 μM, 24 h) and exhibits antiproliferation activity in MCF7 cultures (IC50 in 72 h = 1.1 μM). Unlike most ATP site-targeting kinase inhibitors, X-ray crystallography shows that MU1210 is anchored to the back pocket instead of the hinge region of CLK1. MU140 serves as a negative control.

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point (°F)

Not applicable

Flash Point (°C)

Not applicable

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시험 성적서(COA)

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문서 라이브러리 방문

Václav Němec et al.
Angewandte Chemie (International ed. in English), 58(4), 1062-1066 (2018-12-21)
Reported is the identification of the furo[3,2-b]pyridine core as a novel scaffold for potent and highly selective inhibitors of cdc-like kinases (CLKs) and efficient modulators of the Hedgehog signaling pathway. Initially, a diverse target compound set was prepared by synthetic

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