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Enzastaurin (LY317615)
PKC beta inhibitor,potent and selective

Catalog No.A1670
Size Price Stock Qty
10mM (in 1mL DMSO)
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Evaluation Sample
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Sample solution is provided at 25 µL, 10mM.

Product Citations

1. Piano I, Baba K, et al. "Heteromeric MT(1)/MT(2) melatonin receptors modulate the scotopic electroretinogram via PKCζ in mice." Exp Eye Res. 2018 Jul 27;177:50-54. PMID:30059666

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Chemical structure

Enzastaurin (LY317615)

Related Biological Data

Enzastaurin (LY317615)

Related Biological Data

Enzastaurin (LY317615)

Related Biological Data

Enzastaurin (LY317615)

Biological Activity

Description Enzastaurin (LY317615) is a potent and selective inhibitor of PKCβ with IC50 of 6 nM.
Targets PKCβ PKCα PKCγ PKCε    
IC50 6 nM 39 nM 83 nM 110 nM    


Kinase experiment [1]:

Kinase inhibition assays

The inhibition of PKCβII, PKCα, PKCε, or PKCγ activity by Enzastaurin was determined using a filter plate assay format measuring 33P incorporation into myelin basic protein substrate. Reactions were 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 were started by addition of the enzyme and incubated at room temperature for 60 mins. They were then quenched with 10% H3PO4, transferred to multiscreen anionic phosphocellulose 96-well filter plates, incubated for 30 to 90 mins, filtered and washed with 4 volumes of 0.5% H3PO4 on a vacuum manifold. Scintillation cocktail was added and plates were read on a Microbeta scintillation counter.

Cell experiment [1]:

Cell lines

HCT116 colon cancer and U87MG glioblastoma cells

Preparation method

The solubility of this compound in DMSO is > 10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months.

Reacting condition

4 μM, 48 hrs for both HCT116 colon cancer and U87MG glioblastoma cells; 03 ~ 4 μM for HCT116 colon cancer cells


In both HCT116 colon cancer and U87MG glioblastoma cells, Enzastaurin induced cell apoptosis. HCT116 colon cancer cells treated with Enzastaurin showed a dose-dependent increase in apoptosis.

Animal experiment [1]:

Animal models

Athymic nude mice bearing HCT116 colon cancer xenografts

Dosage form

75 mg/kg; p.o.; b.i.d., for 21 days


In mice bearing HCT116 colon cancer xenografts, Enzastaurin significantly suppressed the growth of HCT116 colon carcinoma. Enzastaurin time-dependently inhibited GSK3βSer9 phosphorylation in HCT116 colon cancer xenograft tissues.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.


[1]. Graff J R, McNulty A M, Hanna K R, et al. The protein kinase Cβ–selective inhibitor, enzastaurin (LY317615.HCl), suppresses signaling through the AKT pathway, induces apoptosis, and suppresses growth of human colon cancer and glioblastoma xenografts. Cancer Research, 2005, 65(16): 7462-7469.

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Chemical Properties

Cas No. 170364-57-5 SDF Download SDF
Synonyms N/A
Chemical Name 3-(1-methylindol-3-yl)-4-[1-[1-(pyridin-2-ylmethyl)piperidin-4-yl]indol-3-yl]pyrrole-2,5-dione
Canonical SMILES CN1C=C(C2=CC=CC=C21)C3=C(C(=O)NC3=O)C4=CN(C5=CC=CC=C54)C6CCN(CC6)CC7=CC=CC=N7
Formula C32H29N5O2 M.Wt 515.61
Solubility ≥8.6mg/mL in DMSO Storage Store at -20°C
Physical Appearance A crystalline solid Shipping Condition Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Research Update

1. A randomized, double-blind, placebo-controlled, Phase II study with and without enzastaurin in combination with docetaxel-based chemotherapy in patients with castration-resistant metastatic prostate cancer. Invest New Drugs. 2013 Aug;31(4):1044-50. doi: 10.1007/s10637-013-9940-0. Epub 2013 Feb 24.
The efficacy of docetaxel/prednisone with or without enzastaurin, an inhibitor of the beta isoform of protein kinase C with therapeutic activity against prostate cancer, in patients with castration-resistant metastatic prostate cancer has been explored.
2. The serine-threonine kinase p90RSK is a new target of enzastaurin in follicular lymphoma cells. Br J Pharmacol. 2013 Dec;170(7):1374-83. doi: 10.1111/bph.12351.
Follicular lymphoma cells are characterized not only by genetic alterations involving Bcl-2, Bcl-6 OR C-mYc but also by alterations in B-cell receptor signaling pathways.
4. Phase I study of enzastaurin and bevacizumab in patients with advanced cancer: safety, efficacy and pharmacokinetics. Invest New Drugs. 2013 Jun;31(3):653-60. doi: 10.1007/s10637-012-9850-6. Epub 2012 Jul 6.
The combination of enzastaurin and bevacizumab, which showed synergistic antitumor activity in preclinical studies, was evaluated for safety and efficacy.
5. A double-blind, randomized, placebo-controlled, phase 2 study of maintenance enzastaurin with 5-fluorouracil/leucovorin plus bevacizumab after first-line therapy for metastatic colorectal cancer. Cancer. 2012 Sep 1;118(17):4132-8. doi: 10.1002/cncr.26692. Epub 2011 Dec 27.
Enzastaurin with 5-fluorouracil/leucovorin plus bevacizumab was evaluated as maintance therapy for MCRC, since the combination of enzastaurin and bevacizumab was well-tolerated and demonstrated synergistic antitumor effects in phse 1 studies.


Enzastaurin is an ATP-competitive, selective oral inhibitor of protein kinase Cβ with IC50 value of 6 nM [1].

Protein kinase C (PKC) is a family of serine-threonine protein kinases that have been proved to play critical roles in the formation and progression of tumor cells. The PKCβ is especially found to contribute to the growth and proliferation of tumors such as diffuse large B-cell lymphoma, multiple myeloma and chronic lymphoid leukemia. The selective PKCβ inhibitor enzastaurin was found to have antiangiogenic activity in tumor model as well as suppress tumor proliferation and induce apoptosis. Besides that, enzastaurin showed the inhibitory effects on phosphorylation of ribosomal protein S6, GSK3β and AKT which are in pathways influenced by PKC. Due to these, enzastaurin was developed as a therapy for cancer [1 and 2].

Enzastaurin at low concentration suppressed cell proliferation of various tumor cells including colon carcinoma (HCT-116), glioblastoma (U87MG), non–small cell lung cancer (A549), melanoma (M14), ovarian cancer (OVCAR-3), breast cancer (MCF-7), leukemia (K562), prostate cancer (PC-3), renal cancer (CAKI-1) and central nervous system cancer (U251). Enzastaurin induced apoptosis of tumor cells at low concentration in a range of 1 to 4 μM and the apoptosis was proved to be caspase-independent. In addition, enzastaurin suppressed the phosphorylation ofGSK3βSer9, ribosomal protein S6Ser240/244 and AKTThr308 time-dependently in tumor cells and affected these pathways [1 and 3].

In mice models, oral administration of enzastaurin at a dose of 75 mg/kg resulted in significant proliferation inhibition of U87MG glioblastoma or HCT116 coloncarcinoma xenografts. In mice bearing human walden strommacro globulinemia xenografts, administration of enzastaurin at dose of 80 mg/kg significantly reduced tumor growth of WM and increased survival [1 and 2].

[1] Graff J R, McNulty A M, Hanna K R, et al.  The protein kinase Cβ–selective inhibitor, enzastaurin (LY317615.HCl), suppresses signaling through the AKT pathway, induces apoptosis, and suppresses growth of human colon cancer and glioblastoma xenografts. Cancer Research, 2005, 65(16): 7462-7469.
[2] Moreau A S, Jia X, Ngo H T, et al.  Protein kinase C inhibitor enzastaurin induces in vitro and in vivo antitumor activity in Waldenstr mmacroglobulinemia. Blood, 2007, 109(11): 4964-4972.
[3] Rizvi M A, Ghias K, Davies K M, et al.  Enzastaurin (LY317615), a protein kinase Cβ inhibitor, inhibits the AKT pathway and induces apoptosis in multiple myeloma cell lines. Molecular cancer therapeutics, 2006, 5(7): 1783-1789.