2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Biological activity
Description
CAS NO.：15982-84-0
Product Name：
Synonyms：
EINEC:
Molecular Formula：C22H23NO
Molecular Weight：317.42
Target:
DUSP6[1]
In Vivo
(E/Z)-BCI hydrochloride (35 mg/kg; intraperitoneal injection; every 7 days; for four weeks; female BALB/c nude mice) treatment enhances cisplatin efficacy in PDX models[2]. Animal Model: Patient-derived xenograft (PDX) models (4-5-week-old female BALB/c nude mice)[2] Dosage: 35 mg/kg Administration: Intraperitoneal injection; every 7 days; for four weeks Result: Tumor weights in the PDX models treated plus CDDP were significantly suppressed compared with tumors from PDX model mice treated with either agent alone.
In Vitro
(E/Z)-BCI hydrochloride (2-10 μM; 72 hours) significantly decreases cell viability in a time and dose-dependent manner in gastric epithelial cell GES1, GC cell lines, and AGS cell lines[2]. (E/Z)-BCI hydrochloride (0.5-4 μM; 24 hours) significantly inhibits DUSP6 expression in LPS-activated macrophages[1]. (E/Z)-BCI hydrochloride (0.5-2 μM; 24 hours) treatment significantly inhibits the expression of IL-1β, TNF-α and IL-6 mRNA in LPS-activated macrophages[1]. (E/Z)-BCI hydrochloride decreases ROS production and activates the Nrf2 pathway in LPS-activated macrophages[1].(E/Z)-BCI hydrochloride inhibits cell proliferation, migration and invasion in a receptor-independent manner and enhances Cisplatin (CDDP) cytotoxicity (enhances CDDP-induced cell death and apoptosis) at pharmacological concentrations in the gastric cancer (GC) cells[2]. Cell Viability Assay[2] Cell Line: Gastric epithelial cell GES1, GC cell lines (HGC27, SGC7901, MKN45, BGC823, MGC803, SNU216, NUGC4), AGS cell lines Concentration: 2 μM, 4 μM, 6 μM, 8 μM, 10 μM Incubation Time: 72 hours Result: Cell viability was significantly decreased in a time and dose-dependent manner. Western Blot Analysis[1] Cell Line: RAW264.7 macrophage cells (by LPS-activated macrophages) Concentration: 0.5 μM, 1 μM, 2 μM, 4 μM Incubation Time: 24 hours Result: DUSP6 protein was significantly downregulated in LPS-activated macrophages. RT-PCR[1] Cell Line: RAW264.7 macrophage cells (by LPS-activated macrophages) Concentration: 0.5 μM, 1 μM, 2 μM Incubation Time: 24 hours Result: The expression of IL-1β, TNF-α and IL-6 mRNA was significantly inhibited inLPS-activated macrophages.
Kinase Assay
Cell Assay
Animal Administration
References
[1]. Zhang F, et al. DUSP6 Inhibitor (E/Z)-BCI Hydrochloride Attenuates Lipopolysaccharide-Induced Inflammatory Responses in Murine Macrophage Cells via Activating the Nrf2 Signaling Axis and Inhibiting the NF-κB Pathway. Inflammation. 2019 Apr;42(2):672-681.
[2]. Wu QN,et al. Pharmacological inhibition of DUSP6 suppresses gastric cancer growth and metastasis and overcomes cisplatin resistance. Cancer Lett. 2018 Jan 1;412:243-255.
Return Policy
If you are in any way unsatisfied with your purchase, you may return any item(s) within 365 days of its original purchase date.
Please provide your Order Number in the email. We strive to reply to all email inquiries within one business day.
