CID 2858522

Pricing Availability Delivery Time Qty
Cat.No. 4246 - CID 2858522 | C28H39N3O3 | CAS No. 758679-97-9
Description: Selectively inhibits PKC-induced NF-κB activation
Chemical Name: 1-[3,5-Bis(1,1-dimethylethyl)-4-hydroxyphenyl]-2-[2-[(3-hydroxypropyl)amino]-5,6-dimethyl-1H-benzimidazol-1-yl]ethanone
Purity: ≥98% (HPLC)
Datasheet
Citations
Literature
Pathways

Biological Activity

Selectively inhibits protein kinase C (PKC)-induced activation of the NF-κB pathway (IC50 < 0.1 μM for PMA-stimulated IL-8 production). Inhibits antigen receptor-stimulated NF-κB activation in chronic lymphocytic leukemia (CLL) B cells. Does not inhibit other NF-κB pathways, including that activated by tumor necrosis factor (TNF).

Technical Data

M. Wt 465.63
Formula C28H39N3O3
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 758679-97-9
PubChem ID 2858523
InChI Key CYCGGKILBWERDJ-UHFFFAOYSA-N
Smiles OCCCNC2=NC1=CC(C)=C(C)C=C1N2CC(C3=CC(C(C)(C)C)=C(O)C(C(C)(C)C)=C3)=O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 9.31 20
ethanol 9.31 20

Preparing Stock Solutions

The following data is based on the product molecular weight 465.63. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.15 mL 10.74 mL 21.48 mL
5 mM 0.43 mL 2.15 mL 4.3 mL
10 mM 0.21 mL 1.07 mL 2.15 mL
50 mM 0.04 mL 0.21 mL 0.43 mL

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Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

Peddibhotla et al (2010) Inhibition of protein kinase C-driven NF-κB activation: synthesis, SAR, and pharmacological profiling of pathway specific benzimidazole probe molecules. J.Med.Chem. 53 4793 PMID: 20481485

Shi et al (2010) Chemical biology strategy reveals pathway-selective inhibitor of NF-κB activation induced by protein kinase C and antigen receptors. ACS Chem.Bio. 5 287 PMID:


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Keywords: CID2858522 NF-kB NF-kappaB NF-κB inhibitors inhibits PKC protein kinase C-induced activation NF-kB/IkB

Citations for CID 2858522

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Literature in this Area

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Pathways for CID 2858522

NF-κB

NF-κB Signaling Pathway

NF-κB signaling plays an important role in inflammation, the innate and adaptive immune response and stress. Dysregulated signaling can occur in inflammatory and autoimmune diseases.

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