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Cat. Number
10-2132
Chemical Name
10-2132 Enzastaurin 170364-57-5
CAS Number
170364-57-5
Mol. Formula
C32H29N5O2
Mol. Weight
515.61
Qty 1
5mg
Qty 2
25mg
Appearance
Orange solid
Application Notes
98% by HPLC NMR (Conforms)
Synonym
LY-317615,3-(1-Methyl-1H-indol-3-yl)-4-[1-[1-(2-pyridinylmethyl)-4-piperidinyl]-1H-indol-3-yl]-1H-pyrrole-2,5-dione
Solubility
Soluble in DMSO (up to 7 mg/ml with warming)
Storage condition
-20°C (des.)
Stability
Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
References

Enzastaurin (170364-57-5) is a potent and selective PKCβ inhibitor.  IC50 = 6, 39, 83 and 110 nM, for PKCβ, PKCα, PKCγ and PKCε respectively.1 Induces apoptosis in multiple myeloma cell lines via inhibition of the AKT signaling pathway.2 Induces mitotic missegregation and preferential cytotoxicity in colorectal cancer cells with chromosomal instability.3 Attenuates amphetamine-stimulated dopamine efflux.4Inhibits blood-brain barrier leakiness in a mouse model.5

References/Citations

1) Graff et al. (2005), The protein kinase Cbeta-selective inhibitor, Enzastaurin (LY317615.HCl), suppresses signaling through the AKT pathway, induces apoptosis, and suppresses growth of human colon cancer and glioblastoma xenografts; Cancer Res. 65 7462
2) Rizvi et al. (2006) Enzastaurin (LY317615), a protein kinase Cβ inhibitor, inhibits the AKT pathway and induces apoptosis in multiple myeloma cell lines; Mol.Cancer Ther. 5 1783
3) Ouaret and Larsen (2014), Protein kinase Cβ inhibition by enzastaurin leads to mitotic missegregation and preferential cytotoxicity toward colorectal cancer cells with chromosomal instability (CIN); Cell Cycle 13 2697
4) Zestos et al. (2016), PKCβ Inhibitors Attenuate Amphetamine-Stimulated Dopamine Efflux; ACS Chem.Neurosci. 7 757
5) Stranahan et al. (2016), Blood-brain barrier breakdown promotes macrophage infiltration and cognitive impairment in leptin receptor-deficient mice; J.Cereb.Blood Flow Metab. 36 2108

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