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Merck
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Documenti fondamentali

SML0661

Sigma-Aldrich

ML216

≥98% (HPLC)

Sinonimo/i:

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

Formula empirica (notazione di Hill):
C15H9F4N5OS
Peso molecolare:
383.32
Codice UNSPSC:
12352200
NACRES:
NA.77

Saggio

≥98% (HPLC)

Stato

powder

Colore

light orange to dark orange

Solubilità

DMSO: 2 mg/mL, clear (warmed)

Temperatura di conservazione

2-8°C

Applicazioni

ML216 has been used in cell proliferation assays.

Azioni biochim/fisiol

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.

Pittogrammi

Skull and crossbones
GHS06

Avvertenze

Danger

Indicazioni di pericolo

H301,H413

Classi di pericolo

Acute Tox. 3 Oral - Aquatic Chronic 4

Codice della classe di stoccaggio

6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects

Classe di pericolosità dell'acqua (WGK)

WGK 3

Punto d’infiammabilità (°F)

Not applicable

Punto d’infiammabilità (°C)

Not applicable

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Certificati d'analisi (COA)

Lot/Batch Number
085M4731V
033M4731V

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Sigma-Aldrich

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Suramin sodium salt ≥98% (TLC)

Sigma-Aldrich

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Suramin sodium salt

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;
Characterization of the EBV-Induced Persistent DNA Damage Response.
Hafez AY and Luftig MA
Viruses, 9(12), 366-366 (2017)
Probe Reports from the NIH Molecular Libraries Program (2010)

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