BMS-986115 is an orally bioavailable, gamma secretase (GS) and pan-Notch inhibitor, with potential antineoplastic activity. Upon administration, GS/pan-Notch inhibitor BMS 986115 binds to GS and blocks the proteolytic cleavage and release of the Notch intracellular domain (NICD), which would normally follow ligand binding to the extracellular domain of the Notch receptor. This prevents both the subsequent translocation of NICD to the nucleus to form a transcription factor complex and the expression of Notch-regulated genes. This results in the induction of apoptosis and the inhibition of growth of tumor cells that overexpress Notch. Overexpression of the Notch signaling pathway plays an important role in tumor cell proliferation and survival.
Chemical | |
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CAS Num | Unknown |
IUPAC Chemical Name | Unknown |
Synonym | BMS-986115; BMS 986115; BMS986115. |
Solubility | Soluble in DMSO, not in water |
SMILES Code | Unknown |
Biological | |
Targets and Effects | N/A |
Pathways | Apoptosis |
Physical | |
Appearance | Solid powder |
Purity | >98% (or refer to the Certificate of Analysis) |
Shipping Condition | Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs. |
Storage Condition | Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). |
Shelf Life | >2 years if stored properly |
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