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Merck

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

Product Name

Enzastaurin, ≥98% (HPLC)

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

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

Quality Level

100

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

signalword

Warning

hcodes

H302,H413

Hazard Classifications

Acute Tox. 4 Oral - Aquatic Chronic 4

Storage Class

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

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