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RRD-251

Chemical Structure : RRD-251

CAS No.: 131916-62-6

RRD-251 (RRD251)

Catalog No.: PC-35100Not For Human Use, Lab Use Only.

RRD-251 is a small molecule disruptor of Rb/Raf-1 interaction, potently and selectively disrupts the Rb/Raf-1 (IC50=77 nM) but not Rb/E2F, Rb/prohibitin, Rb/cyclin E, and Rb/HDAC binding.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

RRD-251 is a small molecule disruptor of Rb/Raf-1 interaction, potently and selectively disrupts the Rb/Raf-1 (IC50=77 nM) but not Rb/E2F, Rb/prohibitin, Rb/cyclin E, and Rb/HDAC binding.
RRD-251 inhibits Rb to recruit Raf-1 to proliferative promoters and inhibited E2F1-dependent transcriptional activity.
RRD-251 inhibits anchorage-dependent and anchorage-independent growth of human cancer cells.
RRD-251 significantly inhibits tumor growth in tumors with functional Rb in vivo.

Physicochemical Properties

M.Wt 235.126
Formula C8H8Cl2N2S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

2,4-dichlorobenzyl carbamimidothioate

References

1. Kinkade R, et al. Cancer Res. 2008 May 15;68(10):3810-8.

2. Singh S, et al. Mol Cancer Ther. 2010 Dec;9(12):3330-41.

3. Treviño JG, et al. Mol Cancer Ther. 2013 Dec;12(12):2722-34.

4. Wallace AS, et al. Oncotarget. 2016 Jul 19;7(29):46401-46418.

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