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About This Item

经验公式(希尔记法):
C15H9F4N5OS
CAS Number:
分子量:
383.32
MDL编号:
UNSPSC代码:
12352200
NACRES:
NA.77
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方案

≥97% (HPLC)

质量水平

表单

solid

制造商/商品名称

Calbiochem®

储存条件

OK to freeze
protect from light

颜色

orange

溶解性

DMSO: 10 mg/mL

储存温度

2-8°C

SMILES字符串

FC(F)(F)c1c(ccc(c1)NC(=O)Nc2[s]c(nn2)c3ccncc3)F

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)

InChI key

WMCOYUSJXXCHFH-UHFFFAOYSA-N

一般描述

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).

生化/生理作用

Cell permeable: yes
Primary Target
BLM
Reversible: yes

包装

Packaged under inert gas

制备说明

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

其他说明

Rosenthal, A.S., et al. 2013. Bioorg. Med. Chem. Lett. 23, 5660.
Nguyen, G.H., et al. 2013. Chem. Biol.20, 55.

法律信息

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

免责声明

Toxicity: Standard Handling (A)

储存分类代码

11 - Combustible Solids

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable


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