Description
BCI-215 is a potent and tumor cell-selective dual specificity MAPK phosphatase (DUSP-MKP) inhibitor. BCI-215 has cytotoxicity for tumor cells but not normal cells.
Product information
CAS Number: 1245792-67-9
Molecular Weight: 396.32
Formula: C22H22BrNO
Chemical Name: (2E)-5-bromo-3-(cyclohexylamino)-2-(phenylmethylidene)-2,3-dihydro-1H-inden-1-one
Smiles: O=C1C2C=CC(Br)=CC=2C(NC2CCCCC2)/C/1=C\C1C=CC=CC=1
InChiKey: JGWQWVVSCQBAFC-DEDYPNTBSA-N
InChi: InChI=1S/C22H22BrNO/c23-16-11-12-18-19(14-16)21(24-17-9-5-2-6-10-17)20(22(18)25)13-15-7-3-1-4-8-15/h1,3-4,7-8,11-14,17,21,24H,2,5-6,9-10H2/b20-13+
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 33.33 mg/mL (84.10 mM; Need ultrasonic).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
BCI-215 concentration-dependently increases pERK levels in DUSP-overexpressing cells with IC50 value in the micromolar range. BCI-215 (1-20 μM; 6 hours) retains fibroblast growth factor hyperactivating and cellular DUSP6/MKP-3 and DUSP1/MKP-1 inhibitory activity but is nontoxic to zebrafish embryos and an endothelial cell line. BCI-215 inhibits survival and motility of MDA-MB-231 human breast cancer cells but does not affect viability of cultured hepatocytes. BCI-215 is completely devoid of hepatocyte toxicity up to 100 µM. BCI-215 does not generate ROS in hepatocytes or in developing Zebrafish larvae.BCI-215 (22 µM) has antimigratory and proapoptotic activities in breast cancer cells that correlate with induction of ERK phosphorylation. BCI-215 (20 µM; 1 hour) induces mitogenic and stress signaling in cancer cells without generating ROS.
Products are for research use only. Not for human use.
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