(E/Z)-BCI hydrochloride

Modify Date: 2024-01-13 17:48:01

(E/Z)-BCI hydrochloride Structure
(E/Z)-BCI hydrochloride structure
Common Name (E/Z)-BCI hydrochloride
CAS Number 95130-23-7 Molecular Weight 353.89
Density N/A Boiling Point 484.6ºC at 760mmHg
Molecular Formula C22H24ClNO Melting Point N/A
MSDS USA Flash Point 161.3ºC

 Use of (E/Z)-BCI hydrochloride


(E/Z)-BCI hydrochloride is a DUSP6 inhibitor with anti-inflammatory activities. (E/Z)-BCI hydrochloride attenuates LPS-induced inflammatory mediators and ROS production in macrophage cells via activating the Nrf2 signaling axis and inhibiting the NF-κB pathway [1].

 Names

Name 1H-Inden-1-one, 3-(cyclohexylamino)-2,3-dihydro-2-(phenylmethylen e)-, chloride (1:1)
Synonym More Synonyms

 (E/Z)-BCI hydrochloride Biological Activity

Description (E/Z)-BCI hydrochloride is a DUSP6 inhibitor with anti-inflammatory activities. (E/Z)-BCI hydrochloride attenuates LPS-induced inflammatory mediators and ROS production in macrophage cells via activating the Nrf2 signaling axis and inhibiting the NF-κB pathway [1].
Related Catalog
Target

DUSP6[1]

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 decreases ROS production and activates the Nrf2 pathway in LPS-activated macrophages[1]. Cell Proliferation 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.
In Vivo (E/Z)-BCI hydrochlorideenhance (35 mg/kg; i.p. injection; every 7 days for four weeks) enhances cisplatin efficacy in PDX models[2]. Animal Model: Patient-derived xenograft (PDX) models (Four- to five-week-old female BALB/c nude mice) [2] Dosage: 35 mg/kg Administration: i.p. injection; every 7 days by 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.
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.

 Chemical & Physical Properties

Boiling Point 484.6ºC at 760mmHg
Molecular Formula C22H24ClNO
Molecular Weight 353.89
Flash Point 161.3ºC
Exact Mass 352.14700
PSA 29.10000
LogP 2.32480

 Safety Information

RIDADR NONH for all modes of transport

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 Synonyms

MFCD16875416