BC-1215

Catalog No.S0322 Batch:S032201

Technical Data

Formula	C₂₆H₂₆N₄
Molecular Weight	394.51	CAS No.	1507370-20-8
Solubility (25°C)*	In vitro	DMSO	79 mg/mL (200.24 mM)
		Ethanol	79 mg/mL (200.24 mM)
		Water	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description

BC-1215 is an inhibitor of F-box protein 3 (Fbxo3, a ubiquitin E3 ligase component) with IC50 of 0.9 μg/mL and LC50 of 87 μg/ml for IL-1β release. BC-1215 inhibits the Fbxo3-TRAF activation pathway by destabilizing TRAF1-6.

Targets

IL-1β release ^[1] (Cell-free assay)	IL-1β release ^[1] (Cell-free assay)
0.9 μg/mL	87 μg/mL(LC50)

In vitro

BC-1215, a Fbxo3 inhibitor, inhibits the Fbxo3-TRAF activation pathway by destabilizing TRAF1-6 proteins. Also, BC-1215 inhibits LPS-induced secretion of a broad spectrum of T_H1 panel cytokines in human PBMC.^[1]

In vivo

A small molecule Fbxo3 inhibitor, BC-1215, reduces inflammation by antagonizing actions of Fbxo3 on TRAF–cytokine signaling.^[1]

Protocol (from reference)

Cell Assay:^{^[1]}	Cell lines Murine lung epithelial (MLE) cells, PBMC, U937 cells Concentrations -- Incubation Time -- Method Murine lung epithelial (MLE) cells were treated with benzathine or BC-1215 at different concentrations for 16 h. Cells were collected and assayed for TRAF1-6, Fbxl2, Fbxo3, and actin immunoblotting. PBMC were treated with either vehicle or 2 μg/ml LPS for 18 h, some cells were also co-treated with BC-1215 in a dose dependent manner up to 10 μg/ml. 18 h later, cells were collected and processed for TRAF immunoblots. U937 cells were transfected with either empty or Fbxo3 plasmid for 24 h. Cells were also treated with BC-1215 in a dose dependent manner up to 10 μg/ml. 18 h later, cells were collected and processed for TRAF immunoblots. PBMC (0.6 ml at 1.5 x 10⁶/ml) were treated with 2 ug/ml LPS for 16 h with BC-1215 at 10 μg/ml. Cytokine release was monitored by the human cytokine array.
Animal Study:^{^[1]}	Animal Models model of a cecal ligation and puncture (CLP)-induced sepsis Dosages 100 μg Administration i.p.

Cell Assay:^{^[1]}

Cell lines
Murine lung epithelial (MLE) cells, PBMC, U937 cells
Concentrations
--
Incubation Time
--
Method
Murine lung epithelial (MLE) cells were treated with benzathine or BC-1215 at different concentrations for 16 h. Cells were collected and assayed for TRAF1-6, Fbxl2, Fbxo3, and actin immunoblotting. PBMC were treated with either vehicle or 2 μg/ml LPS for 18 h, some cells were also co-treated with BC-1215 in a dose dependent manner up to 10 μg/ml. 18 h later, cells were collected and processed for TRAF immunoblots. U937 cells were transfected with either empty or Fbxo3 plasmid for 24 h. Cells were also treated with BC-1215 in a dose dependent manner up to 10 μg/ml. 18 h later, cells were collected and processed for TRAF immunoblots. PBMC (0.6 ml at 1.5 x 10⁶/ml) were treated with 2 ug/ml LPS for 16 h with BC-1215 at 10 μg/ml. Cytokine release was monitored by the human cytokine array.

Animal Study:^{^[1]}

Animal Models
model of a cecal ligation and puncture (CLP)-induced sepsis
Dosages
100 μg
Administration
i.p.

References

[1] Bill B Chen, et al. Nat Immunol. 2013 May;14(5):470-9.

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