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CID-2858522

Catalog No. TQ0305 CAS 758679-97-9

CID-2858522 is an effective and specific antigen receptor-mediated NF-κB activation inhibitor (IC50: 70 nM).

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CID-2858522, CAS 758679-97-9

Pack Size	Availability	Price/USD
1 mg	In stock	$ 59.00
5 mg	In stock	$ 145.00
10 mg	In stock	$ 233.00
25 mg	In stock	$ 393.00
50 mg	In stock	$ 582.00
1 mL * 10 mM (in DMSO)	In stock	$ 148.00

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Description	CID-2858522 is an effective and specific antigen receptor-mediated NF-κB activation inhibitor (IC50: 70 nM).
Targets&IC50	NF-κB:70 nM
In vitro	CID-2858522 (Compound 1) also inhibits testosterone hydroxylase in the presence of human liver microsomes and an NADPH generating system (IC50: 85 μM) [1]. In the HEK293 cell line, CID-2858522 suppresses NF-κB reporter gene activity in a concentration-dependent manner, with IC50 ~70 nM and with maximum inhibition achieved at 0.25-0.5 μM. In contrast, CID-2858522 does not inhibit TNF-induced NF-κB-reporter gene activity at concentrations as high as 4 μM. CID-2858522 also potently inhibits PMA/Ionomycin-induced NF-κB reporter gene activity in transient transfection assays [2].
In vivo	CID-2858522 exhibits nonlinear pharmacokinetics, showing higher serum levels at the 0.5 h measurement time for the 30 mg/kg dose compared to 50 mg/kg but displaying typical dose-dependent behavior when measured at t=3 h. The increasing accumulation seen at a dose of 50 mg/kg may be due to a depot effect created by CYP3A4 inhibition. The cohort exhibits clear signs of morbidity at t=3 h at the 50 mg/kg dose [2].
Cell Research	Cell viability is estimated based on cellular ATP levels. HEK293 cells at a density of 10^5/mL are seeded at 90 μL per well in 96-well white plates and cultured overnight. Compounds (e.g., CID-2858522; 1 μM, 2 μM, 3 μM, and 4 μM) are added (5 μL in medium) to wells and cells are cultured for 16 h, Finally, 50 μL ATPlite solution is added to each well and luminescence activity is read using a luminometer [2].
Animal Research	Three male mice are subjected to CID-2858522 (single i.p doses at 10, 30, and 50 mg/kg). Blood is drawn at 0.5 and 3 h, and subsequent LC/MS analysis of pooled samples is performed to determine the overall blood levels of CID-2858522 [2].

Molecular Weight	465.63
Formula	C28H39N3O3
CAS No.	758679-97-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 6.5 mg/mL (13.96 mM)

References and Literature

1. Okolotowicz KJ, et al. Selective benzimidazole inhibitors of the antigen receptor-mediated NF-kappaB activationpathway. Bioorg Med Chem. 2010 Mar 1;18(5):1918-24. 2. Peddibhotla S, et al. Inhibition of protein kinase C-driven nuclear factor-kappaB activation: synthesis, structure-activity relationship, and pharmacological profiling of pathway specific benzimidazole probe molecules. J Med Chem. 2010 Jun 24;53(12):4793-7.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Antidepressant Compound Library Transcription Factor-Targeted Compound Library NF-κB Signaling Compound Library Anti-Lung Cancer Compound Library Anti-Liver Cancer Compound Library Pyroptosis Compound Library Anti-Cancer Compound Library Anti-Prostate Cancer Compound Library Antioxidant Compound Library

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Keywords

CID-2858522 758679-97-9 NF-Κb NF-κB CID2858522 Nuclear factor-kappaB Nuclear factor-κB inhibit Inhibitor CID 2858522 inhibitor

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