BC-1215

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

BC-1215 (BC1215) 是一种有效、高度独特的选择性 E3 连接酶 F 盒组分 Fbxo3 抑制剂，IL1β IC50 为 0.9 ug/mL。

BC-1215 (BC1215) is a potent,?highly unique, selective E3 ligase F box component Fbxo3 inhibitor with IL1β IC50 of 0.9 ug/mL; inhibits the Fbxo3-TRAF activation pathway for cytokine release, increases immunoreactive Fbxl2 levels and reduces TRAF proteins, impairs Fbxo3 ubiquitination of Fbxl2 with IC50 of 0.1 uM in vitro ubiquitination assay; reversibly inhibits Fbxo3 to destabilize TRAF proteins, remarkably suppresses the majority of the Th1 panel cytokines including G-CSF, GM-CSF, GROα, I-309, IL1-α, IL1-β, IL1rα, IL-6, IL-12, IL-23, MIP-1α, MIP-1β and TNFα, in PBMCs; ameliorates the severity of viral pneumonia, septic shock, colitis, and cytokine-driven inflammation systemically in murine models.Solid Tumors Phase 1 Clinical.

Western Blot Analysis Cell Line:Murine lung epithellal (MLE) cells, PBMC cells and U937 cells Concentration:0, 0.4, 2, 10, 50 μg/mL Incubation Time:6 h, 18 h and 24 h Result:Decreased TRAF protein and inhibited a broad spectrum of Th1 panel cytokines.

Animal Model:Cecal ligation and puncture (CLP)-induced sepsis model Dosage:100 μg Administration:i.p.Result: Significantly attenuated CLP-induced secretion of all three circulating pro-inflammatory cytokines and decreased bacterial counts in the CLP model.

BC 1215 | BC1215

Proteasome/Ubiquitin

E3 Ubiquitin Ligase

E3 Ubiquitin Ligase

Cancer

Solid Tumors

1507370-20-8

394.522

C26H26N4

>98% (HPLC)

In Vitro:?DMSO : 1 mg/mL (2.53 mM)

C1=CC=NC(=C1)C2=CC=C(C=C2)CNCCNCC3=CC=C(C=C3)C4=CC=CC=N4

N1,N2-bis(4-(pyridin-2-yl)benzyl)ethane-1,2-diamine

(-20℃)

With Ice Pack

≥ 2 years