Home Ubiquitin E3 Ligase inhibitor - E3 ligase Ligand chemical BC-1215 For research use only.

BC-1215

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.

BC-1215 Chemical Structure

BC-1215 Chemical Structure

CAS: 1507370-20-8

Purity & Quality Control

Batch: S032201 DMSO] 79 mg/mL] false] Ethanol] 79 mg/mL] false] Water] Insoluble] false Purity: 99.99%
99.99

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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
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 TH1 panel cytokines in human PBMC.[1]
Cell Research 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.
In Vivo
In vivo

A small molecule Fbxo3 inhibitor, BC-1215, reduces inflammation by antagonizing actions of Fbxo3 on TRAF–cytokine signaling.[1]
Animal Research Animal Models model of a cecal ligation and puncture (CLP)-induced sepsis
Dosages 100 μg
Administration i.p.

Chemical Information & Solubility

Molecular Weight 394.51 Formula

C26H26N4
CAS No. 1507370-20-8 SDF --
Smiles C1=CC=NC(=C1)C2=CC=C(C=C2)CNCCNCC3=CC=C(C=C3)C4=CC=CC=N4
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 79 mg/mL ( (200.24 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 79 mg/mL

Water : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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