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Key Documents

SML0661

Sigma-Aldrich

ML216

≥98% (HPLC)

Sinônimo(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

Fórmula empírica (Notação de Hill):
C15H9F4N5OS
Peso molecular:
383.32
Código UNSPSC:
12352200
NACRES:
NA.77

Nível de qualidade

100

Ensaio

≥98% (HPLC)

forma

powder

cor

light orange to dark orange

solubilidade

DMSO: 2 mg/mL, clear (warmed)

temperatura de armazenamento

2-8°C

Aplicação

ML216 has been used in cell proliferation assays.

Ações bioquímicas/fisiológicas

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.

Pictogramas

Skull and crossbones
GHS06

Palavra indicadora

Danger

Frases de perigo

H301,H413

Classificações de perigo

Acute Tox. 3 Oral - Aquatic Chronic 4

Código de classe de armazenamento

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

Classe de risco de água (WGK)

WGK 3

Ponto de fulgor (°F)

Not applicable

Ponto de fulgor (°C)

Not applicable

Certificados de análise (COA)

Busque Certificados de análise (COA) digitando o Número do Lote do produto. Os números de lote e remessa podem ser encontrados no rótulo de um produto após a palavra “Lot” ou “Batch”.

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Sigma-Aldrich

C9911

(S)-(+)-Camptothecin

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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