ChemicalBook Product Catalog Biochemical Engineering Inhibitors TGF-beta / Smad PKC inhibitor Enzastaurin (LY317615)

Enzastaurin (LY317615)

Product NameEnzastaurin (LY317615)
CAS170364-57-5
MFC32H29N5O2
MW515.6
EINECS
MOL File170364-57-5.mol

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.
InChIKey	AXRCEOKUDYDWLF-UHFFFAOYSA-N
SMILES	N1C(=O)C(=C(C1=O)c6c7c([n](c6)C)cccc7)c2c3c([n](c2)C4CCN(CC4)Cc5ncccc5)cccc3

Safety Information

Hazard Codes	Xn
Risk Statements	22
WGK Germany	3
HS Code	29339900
Storage Class	11 - Combustible Solids
Hazard Classifications	Acute Tox. 4 Oral Aquatic Chronic 4

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

Treatment of xenografts with Enzastaurin and radiation produces greater reductions in density of microvessels than either treatment alone. The decrease in microvessel density corresponds to delayed tumor growth^[3].

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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