Enzastaurin (LY317615)
- Product Name
- Enzastaurin (LY317615)
- CAS No.
- 170364-57-5
- Chemical Name
- Enzastaurin (LY317615)
- Synonyms
- Enzastaurin;Ly317615;ENZASTAURIN HCL;3-(1-Methyl-1H-indol-3-yl)-4-(1-(1-(pyridin-2-ylMethyl)piperidin-4-yl)-1H-indol-3-yl)-1H-pyrrole-2,5-dione;D04014;DB-102;CS-1980;Enzastaurine;Unii-uc96G28eqf;LY317615/Enzstataurin
- CBNumber
- CB92128716
- Molecular Formula
- C32H29N5O2
- Formula Weight
- 515.6
- MOL File
- 170364-57-5.mol
Enzastaurin (LY317615) Property
- 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.
N-Bromosuccinimide Price
- Product number
- SML0762
- Product name
- Enzastaurin
- Purity
- ≥98% (HPLC)
- Packaging
- 5mg
- Price
- $124.45
- Updated
- 2025/07/31
- Product number
- SML0762
- Product name
- Enzastaurin
- Purity
- ≥98% (HPLC)
- Packaging
- 25mg
- Price
- $496
- Updated
- 2025/07/31
- Product number
- 11601
- Product name
- Enzastaurin
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $86
- Updated
- 2024/03/01
- Product number
- 11601
- Product name
- Enzastaurin
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $121
- Updated
- 2024/03/01
- Product number
- 11601
- Product name
- Enzastaurin
- Purity
- ≥98%
- Packaging
- 25mg
- Price
- $255
- Updated
- 2024/03/01
Enzastaurin (LY317615) Chemical Properties,Usage,Production
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
Enzastaurin (LY317615) Preparation Products And Raw materials
Raw materials
Preparation Products
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View Lastest Price from Enzastaurin (LY317615) manufacturers
- Product
- Enzastaurin (LY317615) 170364-57-5
- Price
- US $15.00-10.00/KG
- Min. Order
- 1KG
- Purity
- 99%+ HPLC
- Supply Ability
- Monthly supply of 1 ton
- Release date
- 2021-06-27
- Product
- Enzastaurin 170364-57-5
- Price
- US $1.00/KG
- Min. Order
- 1g
- Purity
- Min98% HPLC
- Supply Ability
- g/kg /ton
- Release date
- 2019-12-20