- Enzastaurin
-
- $43.00
-
2026-08-20
- CAS:170364-57-5
- Purity: 99.88%
- Supply Ability: 10g
|
| | Enzastaurin (LY317615) Basic information |
| | Enzastaurin (LY317615) Chemical Properties |
| Melting point | 249-261℃ | | Boiling point | 767.2±60.0 °C(Predicted) | | density | 1.34 | | RTECS | UX9626850 | | Fp | 417.8℃ | | storage temp. | -20°C | | solubility | DMSO: soluble10mg/mL, clear (warmed) | | pka | 7.88±0.60(Predicted) | | form | powder | | 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 |
| 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 |
| | 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 | 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 |
|