An inhibitor of DUSP6 and DUSP1; a mixture of (E) and (Z) isomers; an (E/Z) isomeric mixture inhibits LPS-induced increases in the production of IL-1β

BCI (hydrochloride) – 1 mg

Brand:
Cayman
CAS:
95130-23-7
Storage:
-20
UN-No:
Non-Hazardous - /

BCI is an inhibitor of dual specificity phosphatase 6 (DUSP6) and DUSP1.{48592,48593} (E/Z)-BCI (0.5-2 µM) inhibits LPS-induced expression of Dusp6 in a concentration-dependent manner and increases nuclear protein levels of Nrf2 in RAW 264.7 macrophages. It also inhibits LPS-induced increases in the production of IL-1β, IL-6, and reactive oxygen species (ROS) in RAW 264.7 and isolated mouse peritoneal macrophages in an ERK-independent manner. (E/Z)-BCI inhibits proliferation, migration, and invasion of gastric cancer cells in an ERK-dependent manner and induces cell death in part via the DNA damage response pathway.{48593} It reduces tumor growth in a gastric cancer patient-derived xenograft (PDX) mouse model when administered at a dose of 35 mg/kg every seven days and has an additive effect when used in combination with CDDP (cisplatin; Item No. 13119). The (E) isomer of BCI inhibits DUSP6 and DUSP1 in HeLa cells (IC50s = 12.3 and 11.5 µM, respectively, for the human recombinant enzymes) and prevents pERK2 dephosphorylation induced by DUSP6 in vitro.{38246} It is selective for DUSP6 and DUSP1 over DUSP3/VHR, Cdc25B, and PTP1B, for which it has no activity. (E)-BCI induces expansion of the cardiac progenitor cell pool and increases heart size in zebrafish embryos. This product is a mixture of the (E) and (Z) isomers of BCI.{48593}  

 

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Description

An inhibitor of DUSP6 and DUSP1; a mixture of (E) and (Z) isomers; an (E/Z) isomeric mixture inhibits LPS-induced increases in the production of IL-1β, IL-6, and ROS in RAW 264.7 and isolated mouse peritoneal macrophages in an ERK-independent manner at 0.5-2 µM; an (E/Z) isomeric mixture inhibits proliferation, migration, and invasion of gastric cancer cells in an ERK-dependent manner and reduces tumor growth in a gastric cancer PDX mouse model at 35 mg/kg every seven days; the (E) isomer inhibits DUSP6 and DUSP1 in HeLa cells (IC50s = 12.3 and 11.5 µM, respectively); the (E) isomer induces expansion of the cardiac progenitor cell pool and increases heart size in zebrafish embryos

Formal name: 3-(cyclohexylamino)-2,3-dihydro-2-(phenylmethylene)-1H-inden-1-one, monohydrochloride

Synonyms: 

Molecular weight: 353.9

CAS: 95130-23-7

Purity: ≥95% (mixture of isomers)

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Phosphatases||Research Area|Cancer|Cell Migration & Metastasis||Research Area|Cancer|Cell Signaling||Research Area|Cancer|DNA Damage and Repair||Research Area|Cardiovascular System|Heart|Cardiogenesis||Research Area|Cell Biology|Cell Signaling||Research Area|Immunology & Inflammation|Innate Immunity||Research Area|Oxidative Stress & Reactive Species|Antioxidant Activity||Research Area|Oxidative Stress & Reactive Species|Reactive Oxygen

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