An inhibitor of PKC and Akt signaling
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Enzastaurin

Item No. 11601

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
3-(1-methyl-1H-indol-3-yl)-4-[1-[1-(2-pyridinylmethyl)-4-piperidinyl]-1H-indol-3-yl]-1H-pyrrole-2,5-dione
CAS Number
170364-57-5
Synonyms
  • LY317615
Molecular Formula
C32H29N5O2
Formula Weight
515.6
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 16.6 mg/mlDMF:PBS (pH 7.2)(1:3): 0.25 mg/mlDMSO: 10 mg/ml
λmax
285, 377, 467 nm
SMILES
O=C(N1)C(C2=CN(C3CCN(CC4=NC=CC=C4)CC3)C5=C2C=CC=C5)=C(C6=CN(C)C7=C6C=CC=C7)C1=O
InChi Code
InChI=1S/C32H29N5O2/c1-35-19-25(23-9-2-4-11-27(23)35)29-30(32(39)34-31(29)38)26-20-37(28-12-5-3-10-24(26)28)22-13-16-36(17-14-22)18-21-8-6-7-15-33-21/h2-12,15,19-20,22H,13-14,16-18H2,1H3,(H,34,38,39)
InChi Key
AXRCEOKUDYDWLF-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

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    Product Description

    Enzastaurin is a potent inhibitor of PKCβ (IC50 = 6 nM), with modest selectivity over PKCα, PKCγ, and PKCε (IC50 = 39, 83, and 110 nM, respectively).1 At 3 µM, enzastaurin also inhibits signaling through the Akt pathway.2 It suppresses angiogenesis, induces apoptosis, and reduces proliferation of cultured tumor cells.1,2 Because of these effects, enzastaurin has potential antineoplastic activity.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    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 Res. 65(16), 7462-7469 (2005).

    2. Querfeld, C., Rizvi, M.A., Kuzel, T.M., et al. The selective protein kinase C β inhibitor enzastaurin induces apoptosis in cutaneous T-cell lymphoma cell lines through the AKT pathway. J. Invest. Dermatol. 126(7), 1641-1647 (2006).

    3. Herbst, R.S., Oh, Y., Wagle, A., et al. Enzastaurin, a protein kinase Cβ-selective inhibitor, and its potential application as an anticancer agent in lung cancer. Clin. Cancer Res. 13(15.2), s4641-s4646 (2007).