CID 2858522

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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 (1)
Reviews
Literature (3)
Pathways (1)

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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

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 the degree 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
0.2 mM 10.74 mL 53.69 mL 107.38 mL
1 mM 2.15 mL 10.74 mL 21.48 mL
2 mM 1.07 mL 5.37 mL 10.74 mL
10 mM 0.21 mL 1.07 mL 2.15 mL

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References

References are publications that support the biological activity of the product.

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


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View all NF-κB and IκB Inhibitors

Keywords: CID 2858522, CID 2858522 supplier, CID2858522, NF-kB, NF-kappaB, NF-κB, inhibitors, inhibits, PKC, protein, kinase, C-induced, activation, NF-kB/IkB, 4246, Tocris Bioscience

1 Citation for CID 2858522

Citations are publications that use Tocris products. Selected citations for CID 2858522 include:

Stec et al (2016) Cell line with endogenous EGFRvIII expression is a suitable model for research and drug development purposes. Oncotarget 7 31907 PMID: 27004406


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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.