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Merck

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.

Synonym(s):

Rb/Raf-1 Disruptor 251, S-(2,4-Dichlorobenzyl)-isothiouronium chloride, RRD-251

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About This Item

Empirical Formula (Hill Notation):
C8H9Cl3N2S
CAS Number:
72214-67-6
Molecular Weight:
271.59
UNSPSC Code:
12352200
MDL number:
MFCD00035047
Assay:
≥97% (HPLC)
Form:
solid
Quality level:
100
Storage condition:
OK to freeze, desiccated (hygroscopic), protect from light

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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

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

Quality Level

100

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)

Storage Class

11 - Combustible Solids

wgk

WGK 3

Certificates of Analysis (COA)

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