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Merck

SML0693

LY-333531 hydrochloride

≥98% (HPLC)

Synonym(s):

(9S)-9-[(Dimethylamino)methyl]-6,7,10,11-tetrahydro-9H,18H-5,21:12,17-Dimethenodibenzo[e,k]pyrrolo[3,4-h][1,4,13]oxadiazacyclohexadecine-18,20(19H)-dione hydrochloride, Ruboxistaurin

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About This Item

Empirical Formula (Hill Notation):
C28H28N4O3 · HCl
CAS Number:
Molecular Weight:
505.01
UNSPSC Code:
12352200
NACRES:
NA.77
Assay:
≥98% (HPLC)
Form:
powder
Quality level:
Storage condition:
desiccated, protect from light
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Quality Level

assay

≥98% (HPLC)

form

powder

storage condition

desiccated, protect from light

color

orange-red

solubility

DMSO: 10 mg/mL, clear

storage temp.

−20°C

SMILES string

Cl.[n]21c3c(c(c2)C4=C(c5c6c([n](c5)CC[C@H](OCC1)CN(C)C)cccc6)C(=O)NC4=O)cccc3

InChI

1S/C28H28N4O3.ClH/c1-30(2)15-18-11-12-31-16-21(19-7-3-5-9-23(19)31)25-26(28(34)29-27(25)33)22-17-32(13-14-35-18)24-10-6-4-8-20(22)24;/h3-10,16-18H,11-15H2,1-2H3,(H,29,33,34);1H/t18-;/m0./s1

InChI key

NYQIEYDJYFVLPO-FERBBOLQSA-N

General description

LY-333531 hydrochloride is also known as ruboxistaurin.

Application

LY-333531 hydrochloride/ruboxistaurin has been used as a PKCB blocker to compare phosphopeptides derived from stimulated wild-type cells to phosphopeptides derived from either PKCB knockout cells or wild-type cells.

Biochem/physiol Actions

LY333531 is a potent inhibitor of protein kinase Cβ (PKCβ; 4.7 and 5.9 nM IC50 values for PKCβ1 and PKCβ2, respectively). PKCβ isoforms are overexpressed in states of oxidative stress, especially in association with diabetes. In diabetic rats, LY333531 improves blood flow and leukocyte entrapment in the retina, and protects against myocardial hypertrophy and cardiac dysfunction.
LY333531 is a potent, specific inhibitor of PKCβ.

Features and Benefits

This compound is featured on the PKC page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.

Other Notes

Light sensitive


Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable



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Protein Kinase C β: a New Target Therapy to Prevent the Long-Term Atypical Antipsychotic-Induced Weight Gain.
Rimessi A, et al.
Neuropsychopharmacology, 42(7), 1491?1501-1491?1501 (2017)
Phosphorylation of residues inside the SNARE complex suppresses secretory vesicle fusion.
Malmersjo S, et al.
The Embo Journal, e201694071-e201694071 (2016)
Hongwei Yi et al.
Antioxidants & redox signaling, 30(17), 1949-1968 (2018-11-30)
Aims: Nonalcoholic fatty liver disease (NAFLD) is the most common cause of chronic liver diseases. However, there are no approved pharmacotherapies for the treatment of NAFLD other than managing life style and controlling diets. Extensive studies have demonstrated that multiple