559270
Rb/Raf-1 Disruptor 251
A cell-permeable and orally active isothiouronium compound that potently and selectively disrupts the Rb/Raf-1 interaction, while exhibiting no effect against Rb/B-Raf, Rb/E2F1, Rb/HDAC1, Raf-1/MEK1.
别名:
Rb/Raf-1 Disruptor 251, S-(2,4-Dichlorobenzyl)-isothiouronium chloride, RRD-251
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关于此项目
Assay:
≥97% (HPLC)
Form:
solid
Storage condition:
OK to freeze, desiccated (hygroscopic), protect from light
Quality Segment
assay
≥97% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, desiccated (hygroscopic), protect from light
color
white
solubility
ethanol: 20 mg/mL, DMSO: 50 mg/mL
shipped in
ambient
storage temp.
2-8°C
InChI
1S/C8H8Cl2N2S.ClH/c9-6-2-1-5(7(10)3-6)4-13-8(11)12;/h1-3H,4H2,(H3,11,12);1H
InChI key
COMNQRICZGJVLE-UHFFFAOYSA-N
General description
A cell-permeable and orally active isothiouronium compound that potently and selectively disrupts the Rb/Raf-1 interaction (IC50 = 77 nM in cell-free binding assays), while exhibiting no effect against Rb/B-Raf, Rb/E2F1, Rb/prohibitin, Rb/cyclin E, Rb/HDAC1, Raf-1/MEK1, or Raf-1/MEK2 interaction. Suppresses cellular E2F transcription activity and reduces serum-induced Rb phosphorylation. Shown to display Rb-dependent antitumor activity both in cultures in vitro and in mice in vivo.
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 1 month at -20°C. However, it is strongly recommended that stock solutions be prepared fresh just prior to each use.
Other Notes
Kinkade, R., et al. 2008. Cancer Res.68, 3810.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Irritant (B)
存储类别
11 - Combustible Solids
wgk
WGK 3