Enzastaurin (LY317615) Chemical Properties

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

Hazard Codes 

Xn

Risk Statements 

22

WGK Germany 

3

HS Code 

29339900

Enzastaurin (LY317615) Usage And Synthesis

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.

Uses

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

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.

in vivo

IC 50

PKCβ: 6 nM (IC₅₀); PKCα: 39 nM (IC₅₀); PKCγ: 83 nM (IC₅₀); PKCε: 110 nM (IC₅₀)

References

[1] JEREMY R GRAFF. 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.[J]. Cancer research, 2005, 65 16: 7462-7469. DOI:10.1158/0008-5472.can-05-0071
[2] MUJAHID A RIZVI. Enzastaurin (LY317615), a protein kinase Cbeta inhibitor, inhibits the AKT pathway and induces apoptosis in multiple myeloma cell lines.[J]. Molecular Cancer Therapeutics, 2006, 5 7: 1783-1789. DOI:10.1158/1535-7163.mct-05-0465
[3] DJAMILA OUARET  Annette K L. Protein kinase C β inhibition by enzastaurin leads to mitotic missegregation and preferential cytotoxicity toward colorectal cancer cells with chromosomal instability (CIN).[J]. Cell Cycle, 2014, 13 17: 2697-2706. DOI:10.4161/15384101.2015.945383
[4] ALEXANDER G. ZESTOS. PKCβ Inhibitors Attenuate Amphetamine-Stimulated Dopamine Efflux[J]. ACS Chemical Neuroscience, 2016, 7 6: 757-766. DOI:10.1021/acschemneuro.6b00028
[5] ALEXIS M STRANAHAN. Blood-brain barrier breakdown promotes macrophage infiltration and cognitive impairment in leptin receptor-deficient mice.[J]. Journal of Applied Physics, 2016, 64 1: 2108-2121. DOI:10.1177/0271678x16642233

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