BCI (hydrochloride)

BCI is an inhibitor of dual specificity phosphatase 6 (DUSP6) and DUSP1. (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-1beta, 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. 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, Cay-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. 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.Formal Name: 3-(cyclohexylamino)-2,3-dihydro-2-(phenylmethylene)-1H-inden-1-one, monohydrochloride. CAS Number: 95130-23-7. Molecular Formula: C22H23NO . HCl. Formula Weight: 353.9. Purity: >95% (mixture of isomers). Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 2 mg/ml, DMSO: 10 mg/ml, DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml. lambdamax: 312 nm. SMILES: O=C(C1=CC=CC=C1C/2NC3CCCCC3)C2=C\C4=CC=CC=C4.Cl. InChi Code: InChI=1S/C22H23NO.ClH/c24-22-19-14-8-7-13-18(19)21(23-17-11-5-2-6-12-17)20(22)15-16-9-3-1-4-10-16,/h1,3-4,7-10,13-15,17,21,23H,2,5-6,11-12H2,1H/b20-15+,. InChi Key: JPATUDRDKCLPTI-QMGGKDRNSA-N.