Molecular Weight(MW): 515.61
Enzastaurin (LY317615) is a potent PKCβ selective inhibitor with IC50 of 6 nM in cell-free assays, 6- to 20-fold selectivity against PKCα, PKCγ and PKCε. Phase 3.
Cited by 13 Publications
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The protein kinase C (PKC)–specific inhibitor enzastaurininduces apoptosis of lupus B cells and prevents lupus developmentin Sle mice. C, Levels of serum IgG anti–double-stranded DNA(anti-dsDNA) and antihistone/anti-dsDNA autoantibodies fromvehicle-treated control mice and enzastaurin-treated mice, as analyzedby enzyme-linked immunosorbent assay. Bars in A–C show the meanSD of 3 independent experiments. D, Representative immunofluorescentimages of IgG deposition (top) and glomeruli (bottom) in kidneysections from Sle1.Sle3 mice treated with vehicle or enzastaurin. Originalmagnification 20 (top); 40 (bottom). PAS periodic acid–Schiff.
Arthritis Rheum 2013 65, 1022-31. Enzastaurin (LY317615) purchased from Selleck.The protein kinase C (PKC)–specific inhibitor enzastaurininduces apoptosis of lupus B cells and prevents lupus developmentin Sle mice. A, Effect of enzastaurin on apoptosis of lupus B cells.Purified splenic B cells were treated with anti-IgM antibody in thepresence or absence (control) of enzastaurin for 48 hours and analyzedwith an annexin V detection kit. The fractions of annexin V–positive(apoptotic) cells in the samples treated with only anti-IgM (control)are set at 1. B, Sensitivity of human 9G4-positive and 9G4-negativeB cells to PKC inhibition. Purified splenic B cells were treated withenzastaurin for 24 hours. The apoptotic fractions from untreatedsamples are set at 1. Results are representative of 2 independentexperiments.
Arthritis Rheum 2013 65, 1022-31. Enzastaurin (LY317615) purchased from Selleck.
PKC II contributes to the depolarization-induced enhancement of KCNQ currents. C, PKC inhibitor enzastaurin (2 μM) significantly reduced the depolarization (ND96-K)-induced increase in membrane PKC II levels. D, enzastaurin blocked the depolarization (0 mV)-induced increase of KCNQ2/Q3 current. **, p < 0.01 compared with the control.
J Biol Chem 2011 286, 39760-7. Enzastaurin (LY317615) purchased from Selleck.
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|Description||Enzastaurin (LY317615) is a potent PKCβ selective inhibitor with IC50 of 6 nM in cell-free assays, 6- to 20-fold selectivity against PKCα, PKCγ and PKCε. Phase 3.|
Enzastaurin application results in a marked dose-dependent inhibition of growth in all MM cell lines investigated, including MM.1S, MM.1R, RPMI 8226 (RPMI), RPMI-Dox40 (Dox40), NCI-H929, KMS-11, OPM-2, and U266, with IC50 from 0.6-1.6 μM. Enzastaurin direct impacts human tumor cells, inducing apoptosis and suppressing proliferation in cultured tumor cells. Enzastaurin also suppresses the phosphorylation of GSK3βser9, ribosomal protein S6S240/244, and AKTThr308 while having no direct effect on VEGFR phosphorylation.  Enzastaurin increases apoptosis in malignant lymphocytes of CTCL. When combined with GSK3 inhibitors, enzastaurin demonstrated an enhancement of cytotoxicity levels. Treatment with a combination of enzastaurin and the GSK3 inhibitor AR-A014418 led to increased levels of β-catenin total protein and β-catenin-mediated transcription. Blocking of β-catenin-mediated transcription or small hairpin RNA (shRNA) knockdown of β-catenin induced the same cytotoxic effects as that of enzastaurin plus AR-A014418. Additionally, treatment with enzastaurin and AR-A014418 decreased the mRNA levels and surface expression of CD44. 
|In vivo||Treatment of xenografts with Enzastaurin and radiation produced greater reductions in density of microvessels than either treatment alone. The decrease in microvessel density corresponded to delayed tumor growth. |
Kinase inhibition assays:The inhibition of PKCβII, PKCα, PKCε, or PKCγ activity by enzastaurin is determined using a filter plate assay format measuring 33P incorporation into myelin basic protein substrate. Reactions are done in 100 μL reaction volumes in 96-well polystyrene plates with final conditions as follows: 90 mM HEPES (pH 7.5), 0.001% Triton X-100, 4% DMSO, 5 mM MgCl2, 100 μM CaCl2, 0.1 mg/mL phosphatidylserine, 5 μg/mL diacetyl glyerol, 30 μM ATP, 0.005 μCi/μL 33ATP, 0.25 mg/mL myelin basic protein, serial dilutions of enzastaurin (1-2,000 nM), and recombinant human PKCβII, PKCα, PKCε, or PKCγ enzymes (390, 169, 719, or 128 pM, respectively). Reactions are started by addition of the enzyme and incubated at room temperature for 60 minutes. They are then quenched with 10% H3PO4, transferred to multiscreen anionic phosphocellulose 96-well filter plates, incubated for 30 to 90 minutes, filtered and washed with 4 volumes of 0.5% H3PO4 on a vacuum manifold. Scintillation cocktail is added and plates are read on a Microbeta scintillation counter. IC50 values are determined by fitting a three-variable logistic equation to the 10-point dose-response data using ActivityBase 4.0.
|In vitro||DMSO||30 mg/mL (58.18 mM)|
|In vivo||15% Captisol||30 mg/mL|
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT01432951||Active, not recruiting||Solid Tumor|Lymphoma, Malignant||Eli Lilly and Company||November 2011||Phase 1|
|NCT01388335||Completed||Solid Tumor|Lymphoma, Malignant||Eli Lilly and Company||August 2011||Phase 1|
|NCT00685633||Withdrawn||Prostate Cancer||Eastern Cooperative Oncology Group|National Cancer Institute (NCI)||December 2008||Phase 2|
|NCT00744991||Completed||Cutaneous T-Cell Lymphoma||Eli Lilly and Company||September 2008||Phase 2|
|NCT00718419||Completed||Waldenstroms Macroglobulinemia|Multiple Myeloma||Eli Lilly and Company||July 2008||Phase 2|
|NCT00709995||Active, not recruiting||Metastatic Renal Cell Carcinoma||Eli Lilly and Company||June 2008||Phase 2|
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