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95130-23-7

95130-23-7 structure
95130-23-7 structure
  • Name: (E/Z)-BCI hydrochloride
  • Chemical Name: 1H-Inden-1-one, 3-(cyclohexylamino)-2,3-dihydro-2-(phenylmethylen e)-, chloride (1:1)
  • CAS Number: 95130-23-7
  • Molecular Formula: C22H24ClNO
  • Molecular Weight: 353.89
  • Catalog: Research Areas Inflammation/Immunology
  • Create Date: 2017-01-04 23:35:13
  • Modify Date: 2024-01-13 17:48:01
  • (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].

Name 1H-Inden-1-one, 3-(cyclohexylamino)-2,3-dihydro-2-(phenylmethylen e)-, chloride (1:1)
Synonyms MFCD16875416
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.

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
RIDADR NONH for all modes of transport