A cell-permeable rhodanine compound that upregulates cellular p21Cip1/Waf1 and p27Kip1 protein levels (10uM for 16h in 501 Mel cultures) by preventing Skp2-Cks1-mediated substrate recruitment without affecting the F-box E3 ubiquitin ligase Skp2 interaction with Cks1 or the SCF (Skp1-cullin1-F-box) complex. Shown to inhibit the proliferation of human breast cancer MCF-7 and melanoma 501 Mel cells (IC50 = 8 and 30uM, respectively; 16h incubation). Unlike SMIP004, C1 does not affect cellular Cyclin E/CDK2 kinase activity or Skp2 level.
Synonyms:p21/Cip1/Waf1 Activator I; p27/Kip1 Activator I, S-phase Kinase-associated Protein 2 Inhibitor I; SCFSKP2 Inhibitor I, CRL1SKP2 Inhibitor I, (Z)-2-(4-Bromo-2-((4-oxo-3-(pyridin-3-ylmethyl)-2-thioxothiazolidin-5-ylidene)methyl)phenoxy)acetic acid
Molecular Formula:C₁₈H₁₃BrN₂O₄S₂
Solubility:DMSO
Primary Target:disrupts p27-Skp2 interaction
Molar Mass:465.3
Purity:≥99% (HPLC)
Form:Supplied as an orange brown powder.
Storage and Stability:May be stored at 4°C. For long-term storage, aliquot and store at 4°C. Do not freeze. For maximum recovery of product, centrifuge the original vial prior to removing the cap. Further dilutions can be made in assay buffer.
