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HomeProduct name listEnzastaurin (LY317615)

Enzastaurin (LY317615)

Synonym(s):3-(1-Methyl-1H-indol-3-yl)-4-[1-[1-(2-pyridinylmethyl)-4-piperidinyl]-1H-indol-3-yl]-1H-pyrrole-2,5-dione;D04014;LY317615;LY-317615

Enzastaurin (LY317615) Structural

What is Enzastaurin (LY317615)?

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

The Uses of Enzastaurin (LY317615)

PKCβ-selective inhibitor, suppresses angiogenesis.

The Uses of Enzastaurin (LY317615)

Enzastaurin has been used in splicing analysis to study its effects on splicing of a mutated exon.

What are the applications of Application

Enzastaurin is a potent inhibitor of PKCβ, PKCα, PKCγ and PKCε

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

Properties of Enzastaurin (LY317615)

Melting point: 249-261℃
Boiling point: 767.2±60.0 °C(Predicted)
Density  1.34
RTECS  UX9626850
Flash point: 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.

Safety information for Enzastaurin (LY317615)

Signal word Warning
Pictogram(s)
ghs
Exclamation Mark
Irritant
GHS07
GHS Hazard Statements H302:Acute toxicity,oral
H413:Hazardous to the aquatic environment, long-term hazard
Precautionary Statement Codes P273:Avoid release to the environment.

Computed Descriptors for Enzastaurin (LY317615)

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