SML0661
ML216
≥98% (HPLC)
Synonym(s):
1-(4-Fluoro-3-(trifluoromethyl)phenyl)-3-(5-(pyridin-4-yl)-1,3,4-thiadiazol-2-yl)urea
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About This Item
Empirical Formula (Hill Notation):
C15H9F4N5OS
Molecular Weight:
383.32
NACRES:
NA.77
UNSPSC Code:
12352200
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
Related Categories
Application
ML216 has been used in cell proliferation assays.
Biochem/physiol Actions
ML216 is a 4-F-phenyl analog. It blocks cell proliferation of BLM-proficient fibroblast cells (PSNF5) and shows very less effects on BLM-deficient fibroblast cells (PSNG13).
ML216 is a membrane permeable selective inhibitor of Bloom (BLM) helicase, a member of the RecQ DNA helicase family. Bloom′s syndrome, caused by a mutation in BLM, is associated with susceptibility to cancer, growth retardation, immunodeficiency, sunlight sensitivity, and fertility defects. ML216 is selective for BLM over other members of the RecQ family, especially in vivo, and appears to act at the BLM-nucleic acid substrate binding site, inhibiting DNA binding and blocking BLM′s helicase activity. ML216 could be useful in studies of tumor cells depending on the ALT (alternative lengthening of telomeres) mechanism for telomere maintenance rather than on telomerase, which are proposed to be susceptible to BLM inhibition.
ML216 is a membrane permeable selective inhibitor of Bloom (BLM) helicase.
signalword
Danger
hcodes
Hazard Classifications
Acute Tox. 3 Oral - Aquatic Chronic 4
Storage Class
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
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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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