| Identification | Back Directory | [Name]
Enzastaurin (LY317615) | [CAS]
170364-57-5 | [Synonyms]
D04014
DB-102
CS-1980
Ly317615
Enzastaurin
Enzastaurine
ENZASTAURIN HCL
Unii-uc96G28eqf
LY317615/Enzstataurin
LY317615 (Enzastaurin)
Enzastaurin ( LY317615 )
Enzastaurin (LY317615) USP/EP/BP
Enzastaurin, 98%, a potent PKCβ selective inhibitor
Enzastaurin,Enzstataurin,LY317615,170364-57-5,1H-Pyrrole-2,5-dione, 3-
3-(1-Methyl-1H-indol-3-yl)-4-(1-(1-(pyridin-2-ylmethyl)-piperidin-4-yl)-1H-indol-3-yl)-1H-pyrr
3-(1-Methyl-1H-indol-3-yl)-4-(1-(1-(pyridin-2-ylmethyl)-piperidin-4-yl)-1H-indol-3-yl)-1H-pyrrole
3-(1-methyl-1H-indol-3-yl)-4-(1-(1-(pyridin-2-ylmethyl)piperidin-4-yl)-1H-indol-3-yl)-1H-pyrrole-2
3-(1-Methyl-1H-indol-3-yl)-4-(1-(1-(2-pyridinylmethyl)-4-piperidinyl)-1H-indol-3-yl)-1H-pyrrole-2,5-dione
3-(1-Methyl-1H-indol-3-yl)-4-(1-(1-(pyridin-2-ylMethyl)piperidin-4-yl)-1H-indol-3-yl)-1H-pyrrole-2,5-dione
1H-Pyrrole-2,5-dione, 3-(1-methyl-1H-indol-3-yl)-4-(1-(1-(2-pyridinylmethyl)-4-piperidinyl)-1H-indol-3-yl)- | [Molecular Formula]
C32H29N5O2 | [MDL Number]
MFCD11040980 | [MOL File]
170364-57-5.mol | [Molecular Weight]
515.6 |
| Chemical Properties | Back Directory | [Melting point ]
249-261℃ | [Boiling point ]
767.2±60.0 °C(Predicted) | [density ]
1.34 | [RTECS ]
UX9626850 | [Fp ]
417.8℃ | [storage temp. ]
?20°C | [solubility ]
DMSO: soluble10mg/mL, clear (warmed) | [form ]
powder | [pka]
7.88±0.60(Predicted) | [color ]
, light orange to dark orange-red | [Stability:]
Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months. |
| Hazard Information | Back Directory | [Description]
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.4 Inhibits blood-brain barrier leakiness in a mouse model.5 | [Uses]
PKCβ-selective inhibitor, suppresses angiogenesis. | [Definition]
ChEBI: 3-(1-methyl-3-indolyl)-4-[1-[1-(2-pyridinylmethyl)-4-piperidinyl]-3-indolyl]pyrrole-2,5-dione is a member of indoles and a member of maleimides. | [Biochem/physiol Actions]
Enzastaurin is a potent and PKCβ preferring inhibitor. Also, Enzastaurin inhibits AKT and GSK3β. Enzastaurin acts as anti-angiogenic and antineoplastic agent. | [References]
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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