5.31085
MLS000544460
≥97% (HPLC), Eya2 Phosphatase Inhibitor, solid
동의어(들):
Eya2 Phosphatase Inhibitor, MLS000544460, 3-Fluoro-N-(( E)-(5-pyridin-2-ylsulfanylfuran-2-yl)methylideneamino)benzamide, ( E)-3-Fluoro-Nʹ-((5-(pyridin-2-ylthio)furan-2-yl)methylene)benzohydrazide, Eab1 Inhibitor, Eyes Absent Homolog 2 Inhibitor
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크기 선택
제품정보 (DICE 배송 시 비용 별도)
실험식(Hill 표기법):
C17H12FN3O2S
CAS 번호:
Molecular Weight:
341.36
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
제품 이름
Eya2 Phosphatase Inhibitor, MLS000544460,
assay
≥97% (HPLC)
form
solid
potency
2.0 μM Ki
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
protect from light
color
beige
solubility
DMSO: 100 mg/mL
storage temp.
2-8°C
Quality Level
Biochem/physiol Actions
Cell permeable: yes
Primary Target
Eya2 C-terminal Eya domain (ED) protein tyrosine phosphatase
Eya2 C-terminal Eya domain (ED) protein tyrosine phosphatase
Reversible: yes
Disclaimer
Toxicity: Standard Handling (A)
General description
A cell-permeable furylidenebenzohydrazide compound that acts as a reversible inhibitor against Eya2 C-terminal Eya domain (ED) protein tyrosine phosphatase (PTP) activity (IC50 = 4.1 µM; 100 nM ED & 5 µM Mg2+; Substrate = 25 µM OMFP) via affinity docking at an allosteric pocket located opposite to the active site (KD = 6.1 or 2.0 µM, respectively, with or without 5 mM exogenous Mg2+; KD = 0.8 µM with 10 mM EDTA and no exogenous Mg2+), while being ineffective against the PTP activity of Eya3 & PTP1B or the Ser/Thr phosphatase activity of PPM1A & Scp1. Shown to reduce Eya2 overexpression-induced migration enhancement in MCF10A cultures (17% vs. 54% enhancement with or without 10 µM inhibitor). The inhibition appears to be non-competitive with respect to substrate in the presence of 5 mM Mg2+, while mixed mode of inhibition is observed at a low Mg2+ concentration of 5 µM.
Other Notes
Krueger, A.B., et al. 2014. J. Biol. Chem.289, 16349.
Krueger, A.B., et al. 2013. J. Biomol. Screen.18, 85.
Krueger, A.B., et al. 2013. J. Biomol. Screen.18, 85.
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
저장 등급
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
시험 성적서(COA)
제품의 로트/배치 번호를 입력하여 시험 성적서(COA)을 검색하십시오. 로트 및 배치 번호는 제품 라벨에 있는 ‘로트’ 또는 ‘배치’라는 용어 뒤에서 찾을 수 있습니다.
Konstantinos Sousounis et al.
eLife, 9 (2020-03-07)
How salamanders accomplish progenitor cell proliferation while faithfully maintaining genomic integrity and regenerative potential remains elusive. Here we found an innate DNA damage response mechanism that is evident during blastema proliferation (early- to late-bud) and studied its role during tissue
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