General description
A cell-permeable benzylidene-thioxo-imidazolidinone compund that directly and reversibly binds to c-Rel to change its conformation and blocks its DNA binding and transcriptional activity (IC50 = 3 µM in EMSA). Shows good selectivity over Oct1 and AP1. Reduces IL-2 expression in activated T cells without affecting their viability. Induces growth arrest in diffuse large B-cell lymphoma (DLBCL) cell line Ly3 (IC50 = 18 uM). Shown to reduce alloactivation in T cells and diminish graft-versus-host disease (GVHD), but does not impair TCR-mediated killing. Improves the survival rate of lethally irradiated BABL/c mice transplanted with T cell depleted bone marrow cells from C57BL/6 mice (~24 mg/kg, i.p, daily).
A cell-permeable benzylidene-thioxo-imidazolidinone compund that directly and reversibly binds to c-Rel to change its conformation and blocks its DNA binding and transcriptional activity (IC50 = 3 µM in EMSA). Shows good selectivity over Oct1 and AP1. Reduces IL-2 expression in activated T cells without affecting their viability. Induces growth arrest in diffuse large B-cell lymphoma (DLBCL) cell line Ly3 (IC50 = 18 uM). Shown to reduce alloactivation in T cells and diminish graft-versus-host disease (GVHD), but does not impair TCR-mediated killing. Improves the survival rate of lethally irradiated BABL/c mice transplanted with T cell depleted bone marrow cells from C57BL/6 mice (~24 mg/kg, i.p, daily).
Please note that the molecular weight for this compound is batch-specific due to variable water content.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
c-Rel
Reversible: yes
Packaging
Packaged under inert gas
Warning
Toxicity: Standard Handling (A)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Use only fresh DMSO for reconstitution.
Other Notes
Shono, Y., et al. 2014. Cancer Discovery4, 578.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Molecular Weight: 329.17. Empirical Formula: C11H9BrN2O3S. Assay: ≥. 97% (HPLC). Quality Level: 100. form: powder. manufacturer/tradename: Calbiochem®. . storage condition: OK to freeze, protect from light. color: dark yellow. solubility: DMSO: 100 . mg/mL. storage temp.: 2-8°C. SMILES string: COC1: CC(: CC(: C1O)C: C2C(: O)NC(: S)N2)Br. Storage Class Code: 11 - Combustible Solids. WGK: WGK 3. Flash Point(F): Not applicable. Flash Point(C): Not applicable.- UPC:
- 51284706
- Condition:
- New
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- 5306540001