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Merck
CN

SML0762

Enzastaurin

≥98% (HPLC)

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, LY-317615, LY317615

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About This Item

Empirical Formula (Hill Notation):
C32H29N5O2
CAS Number:
170364-57-5
Molecular Weight:
515.60
UNSPSC Code:
12352200
NACRES:
NA.77

Key Documents

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Quality Level

100

Assay

≥98% (HPLC)

form

powder

storage condition

desiccated

color

, light orange to dark orange-red

solubility

DMSO: 10 mg/mL, clear (warmed)

storage temp.

−20°C

SMILES string

N1C(=O)C(=C(C1=O)c6c7c([n](c6)C)cccc7)c2c3c([n](c2)C4CCN(CC4)Cc5ncccc5)cccc3

InChI

1S/C32H29N5O2/c1-35-19-25(23-9-2-4-11-27(23)35)29-30(32(39)34-31(29)38)26-20-37(28-12-5-3-10-24(26)28)22-13-16-36(17-14-22)18-21-8-6-7-15-33-21/h2-12,15,19-20,22H,13-14,16-18H2,1H3,(H,34,38,39)

InChI key

AXRCEOKUDYDWLF-UHFFFAOYSA-N

Related Categories

Application

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

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.
Enzastaurin is a potent and PKCβ proffering inhibitor.
It is an orally administered drug. It can induce apoptosis, inhibit angiogenesis and proliferation of cells. Enzastaurin can be used for the treatment of haematological cancers.

Features and Benefits

This compound is featured on the GSK-3, PKB/Akt and PKC pages of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.

Pictograms

Exclamation mark
GHS07

Signal Word

Warning

Hazard Statements

H302,H413

Precautionary Statements

P273 - P301 + P312 + P330

Hazard Classifications

Acute Tox. 4 Oral - Aquatic Chronic 4

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

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Certificates of Analysis (COA)

Lot/Batch Number
0000169327
0000176584
0000173874
0000173874
0000169327

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Enzastaurin: A lesson in drug development.
Bourhill T
Critical Reviews in Oncology/Hematology (2017)
Staurosporine allows dystrophin expression by skipping of nonsense-encoding exon
Atsushi N
Brain & Development (2016)
Novel kinome profiling technology reveals drug treatment is patient and 2D/3D model dependent in glioblastoma.
Fabro, et al.
Frontiers in Oncology, 12, 1012236-1012236 (2022)
Mehdi Bouhaddou et al.
Cell, 182(3), 685-712 (2020-07-10)
The causative agent of the coronavirus disease 2019 (COVID-19) pandemic, severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), has infected millions and killed hundreds of thousands of people worldwide, highlighting an urgent need to develop antiviral therapies. Here we present a
Shannon M White et al.
Developmental cell, 49(3), 425-443 (2019-05-08)
Merlin/NF2 is a bona fide tumor suppressor whose mutations underlie inherited tumor syndrome neurofibromatosis type 2 (NF2), as well as various sporadic cancers including kidney cancer. Multiple Merlin/NF2 effector pathways including the Hippo-YAP/TAZ pathway have been identified. However, the molecular

Articles

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Glycogen Synthase Kinase 3 (GSK-3) Overview

Glycogen synthase kinase 3 (GSK-3) is a highly conserved family of serine/threonine kinases for over 100 proteins in many pathways. See a list of accepted GSK-3 modulators and related products.

肝醣合成酶激酶3 (GSK-3)概述

肝醣合成酶激酶3 (GSK-3)是一种高度保守的丝氨酸/苏氨酸激酶家族，适于在多种途径中处理100多种蛋白质。查看允许的GSK-3调节剂和相关产品列表。

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