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
• 经验公式（希尔记法）: C₁₅H₉F₄N₅OS
• CAS号: 1430213-30-1
• 分子量: 383.32
• MDL號碼: MFCD24849400
• 分類程式碼代碼: 12352200
• NACRES: NA.77

属性

• 化驗: ≥97% (HPLC)
• 品質等級: 100
• 形狀: solid
• 製造商／商標名: Calbiochem^®
• 儲存條件: OK to freeze; protect from light
• 顏色: orange
• 溶解度: DMSO: 10 mg/mL
• 儲存溫度: 2-8°C
• SMILES 字串: 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 密鑰: WMCOYUSJXXCHFH-UHFFFAOYSA-N

说明

一般說明

A cell-permeable pyridinyl-thiadiazolylurea compound that selectively blocks Bloom′s syndrome protein (BLM) helicase activity of both full-length as well as truncated BLM^636-1298 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 (T_1/2 >1.2 h) and plasma stability (~100% at 5 h).

生化／生理作用

Cell permeable: yes

Primary Target
BLM

Reversible: yes

包裝

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

重構

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

其他說明

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

法律資訊

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

安全信息

• 儲存類別代碼: 11 - Combustible Solids
• 水污染物質分類（WGK）: WGK 3
• 閃點（°F）: Not applicable
• 閃點（°C）: Not applicable