5.06384
BLM Helicase Inhibitor, ML216
别名:
BLM Helicase Inhibitor, ML216, 1-(4-Fluoro-3-(trifluoromethyl)phenyl)-3-(5-(pyridin-4-yl)-1,3,4-thiadiazol-2-yl)urea, ML-216, ML-216, 1-(4-Fluoro-3-(trifluoromethyl)phenyl)-3-(5-(pyridin-4-yl)-1,3,4-thiadiazol-2-yl)urea
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关于此项目
经验公式（希尔记法）:
C15H9F4N5OS
化学文摘社编号:
分子量:
383.32
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
InChI key
WMCOYUSJXXCHFH-UHFFFAOYSA-N
InChI
1S/C15H9F4N5OS/c16-11-2-1-9(7-10(11)15(17,18)19)21-13(25)22-14-24-23-12(26-14)8-3-5-20-6-4-8/h1-7H,(H2,21,22,24,25)
SMILES string
FC(F)(F)c1c(ccc(c1)NC(=O)Nc2[s]c(nn2)c3ccncc3)F
assay
≥97% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
orange
solubility
DMSO: 10 mg/mL
Quality Level
General description
A cell-permeable pyridinyl-thiadiazolylurea compound that selectively blocks Bloom′s syndrome protein (BLM) helicase activity of both full-length as well as truncated BLM636-1298 forms (IC50 = 2.98 and 0.97 µM, respectively). Competes with and reversibly blocks DNA binding to BLM. However, the inhibition appears to be non-competitive with respect to ATP. Exhibits anti-proliferative activity in cells expressing BLM, but not in those lacking BLM. Induces sister chromatid exchanges (SCEs) and enhances the sensitivity of BLM containing PSNF5 cells to aphidicolin (>Cat. No. 178273) without affecting PSNG13 cells that are devoid of BLM. Displays favorable microsomal (T1/2 >1.2 h) and plasma stability (~100% at 5 h).
Biochem/physiol Actions
Cell permeable: yes
Primary Target
BLM
BLM
Reversible: yes
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Other Notes
Rosenthal, A.S., et al. 2013. Bioorg. Med. Chem. Lett. 23, 5660.
Nguyen, G.H., et al. 2013. Chem. Biol.20, 55.
Nguyen, G.H., et al. 2013. Chem. Biol.20, 55.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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