assay
≥98% (HPLC)
form
powder
color
light orange to dark orange
solubility
DMSO: 2 mg/mL, clear (warmed)
storage temp.
2-8°C
Quality Level
Application
ML216已用于细胞增殖检测。
Biochem/physiol Actions
ML216是Bloom（BLM）解旋酶的一种膜可渗透选择性抑制剂，其是RecQ DNA解旋酶家族的成员。由BLM突变引起的Bloom综合症与癌症易感性、生长迟缓、免疫缺陷、日光敏感性和生育能力缺陷有关。相对于RecQ家族的其他成员，ML216对于BLM具有选择性，尤其是在体内，并可能是在BLM核酸底物结合位点起作用，抑制DNA结合并阻断BLM的解旋酶活性。基于维持端粒酶的ALT（端粒的替代性延长）机制（而非端粒酶，该酶容易受到BLM的抑制），ML216可能在肿瘤细胞研究中其作用。
ML216是Bloom（BLM）解旋酶的一种膜渗透选择性抑制剂。
ML216是一种4-F-苯基类似物。它可阻断BLM丰富的成纤维细胞(PSNF5)的细胞增殖，并且对BLM缺乏的成纤维细胞(PSNG13)的影响较小。
signalword
Danger
hcodes
Hazard Classifications
Acute Tox. 3 Oral - Aquatic Chronic 4
存储类别
6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Probe Reports from the NIH Molecular Libraries Program (2010)
Characterization of the EBV-Induced Persistent DNA Damage Response.
Hafez AY and Luftig MA
Viruses, 9(12), 366-366 (2017)
Synthesis and SAR studies of 5-(pyridin-4-yl)-1,3,4-thiadiazol-2-amine derivatives as potent inhibitors of Bloom Helicase.
Rosenthal AS, et al.
Bioorganic & Medicinal Chemistry Letters, 23(20), 5660-5666 (2013)
Xiangrong Chen et al.
eLife, 10 (2021-03-02)
BLM (Bloom syndrome protein) is a RECQ-family helicase involved in the dissolution of complex DNA structures and repair intermediates. Synthetic lethality analysis implicates BLM as a promising target in a range of cancers with defects in the DNA damage response;
Elsa Callen et al.
Molecular cell, 77(1), 26-38 (2019-10-28)
53BP1 activity drives genome instability and lethality in BRCA1-deficient mice by inhibiting homologous recombination (HR). The anti-recombinogenic functions of 53BP1 require phosphorylation-dependent interactions with PTIP and RIF1/shieldin effector complexes. While RIF1/shieldin blocks 5'-3' nucleolytic processing of DNA ends, it remains
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