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RUBOXISTAURIN HYDROCHLORIDE

Product Name
RUBOXISTAURIN HYDROCHLORIDE
CAS No.
169939-93-9
Chemical Name
RUBOXISTAURIN HYDROCHLORIDE
Synonyms
LY333531 HCl;CAS:169939-93-9;Ruboxistaurin HCl;Ruboxistaurin(LY333531HCl);Ruboxistaurin Hydrochloride;Ruboxistaurin HCl(LY333531 );ruboxistaurin/LY 333531 hydrochloride;Ruboxistaurin hydrochloride (LY333531);LY 333531 hydrochloride - Ruboxistaurin;LY333531 Hydrochloride(Ruboxistaurin HCl)
CBNumber
CB9206452
Molecular Formula
C28H29ClN4O3
Formula Weight
505.02
MOL File
169939-93-9.mol
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RUBOXISTAURIN HYDROCHLORIDE Property

alpha 
D25 -28.7° (c = 1.0 in ethanol)
storage temp. 
Inert atmosphere,Store in freezer, under -20°C
solubility 
DMSO: soluble10mg/mL, clear
form 
powder
color 
orange-red
InChIKey
NYQIEYDJYFVLPO-QAYAHANANA-N
SMILES
O=C1NC(=O)C2C3=CN(CCO[C@]([H])(CN(C)C)CCN4C5=CC=CC=C5C(=C4)C1=2)C1=CC=CC=C31.Cl |&1:12,r|
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Safety

WGK Germany 
3
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
SML0693
Product name
LY-333531 hydrochloride
Purity
≥98% (HPLC)
Packaging
1mg
Price
$148.2
Updated
2025/07/31
Cayman Chemical
Product number
13964
Product name
LY333531 (hydrochloride)
Purity
≥98%
Packaging
1mg
Price
$106
Updated
2024/03/01
Cayman Chemical
Product number
13964
Product name
LY333531 (hydrochloride)
Purity
≥98%
Packaging
5mg
Price
$311
Updated
2024/03/01
TRC
Product number
R701525
Product name
RuboxistaurinHydrochloride
Packaging
0.5mg
Price
$185
Updated
2021/12/16
Axon Medchem
Product number
Axon2362
Product name
LY333531hydrochloride-Ruboxistaurin
Purity
99%
Packaging
5mg
Price
$214.5
Updated
2021/12/16
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RUBOXISTAURIN HYDROCHLORIDE Chemical Properties,Usage,Production

Description

LY333531 is an inhibitor of PKCβ (IC50s = 4.7 and 5.9 nM for PKCβ1 and PKCβ2, respectively). It is selective for PKCβ1 and PKCβ2 over PKCα, -γ, -δ, -ε, -ζ, and -η (IC50s = 360, 300, 250, >100,000, and 52 nM, respectively). LY333531 also inhibits glycogen synthase kinase 3β (GSK3β; IC50 = 39.4 nM). It inhibits neutrophil extracellular trap (NET) formation induced by phorbol 12-myristate 13-acetate (PMA; ) in primary human neutrophils when used at a concentration of 1 μM. LY333531 increases the mechanical nociceptive threshold in a rat model of diabetic hyperalgesia induced by streptozotocin (STZ; ).

Uses

A protein kinase C (PKC) β inhibitor, exhibits significant anti-angiogenic activity that reduces the response of vascular endothelial cells to stimulation by vascular endothelial growth factor (VEGF). It is used in treatment of diabetic microvascular comp

Uses

Ruboxistaurin is a protein kinase C (PKC) β inhibitor, exhibits significant anti-angiogenic activity that reduces the response of vascular endothelial cells to stimulation by vascular endothelial growth factor (VEGF). Ruboxistaurin is used in treatment of diabetic microvascular complications.

in vivo

Ruboxistaurin (1 mg/kg; 8 weeks) markedly reduces GEC apoptosis as well as swiprosin-1 upregulation, and ameliorates renal glomerular injury in the diabetic mice. Ruboxistaurin also potently attenuates the expression of PARP, cleaved-caspase9, cleaved-caspase3, and the Bax/Bcl-2 ratio, in diabetic mice[3]. Ruboxistaurin (0.1, 1.0, or 10.0 mg/kg; p.o.) dramatically reduces the number of leukocytes trapped in the retinal microcirculation of diabetic rats[4].

IC 50

PKCβI: 4.7 nM (IC50); PKCβII: 5.9 nM (IC50); PKCη: 52 nM (IC50); PKCδ: 250 nM (IC50); PKCγ: 300 nM (IC50); PKCα: 360 nM (IC50); PKCε: 600 nM (IC50)

References

[1] MICHAEL R. JIROUSEK. (S)-13-[(Dimethylamino)methyl]-10,11,14,15-tetrahydro-4,9:16,21-dimetheno- 1H,13H-dibenzo[e,k]pyrrolo[3,4-h][1,4,13]oxadiazacyclohexadecene-1,3(2H)-dione (LY333531) and Related Analogues: Isozyme Selective Inhibitors of Protein Kinase Cβ[J]. Journal of Medicinal Chemistry, 1996, 39 14: 2664-2671. DOI: 10.1021/jm950588y
[2] PATRICIA A. VIGNAUX. Machine Learning for Discovery of GSK3β Inhibitors[J]. ACS Omega, 2020, 5 41: 26551-26561. DOI: 10.1021/acsomega.0c03302
[3] ROBERT D GRAY. Activation of conventional protein kinase C (PKC) is critical in the generation of human neutrophil extracellular traps.[J]. Journal of Inflammation-London, 2013, 10 1: 12. DOI: 10.1186/1476-9255-10-12
[4] HYOH KIM. Protein kinase Cbeta selective inhibitor LY333531 attenuates diabetic hyperalgesia through ameliorating cGMP level of dorsal root ganglion neurons.[J]. Diabetes, 2003, 52 8: 2102-2109. DOI: 10.2337/diabetes.52.8.2102

RUBOXISTAURIN HYDROCHLORIDE Preparation Products And Raw materials

Raw materials

Preparation Products

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RUBOXISTAURIN HYDROCHLORIDE Suppliers

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169939-93-9, RUBOXISTAURIN HYDROCHLORIDERelated Search:

Trimethylamine hydrochloride Betaine hydrochloride L-Lysine hydrochloride Dimethylamine hydrochloride RUBOXISTAURIN HYDROCHLORIDE RUBOXISTAURIN 3-Isopropenyl-1-methyl-1H-pyrrole 3,4-Di-1H-indol-3-yl-1H-pyrrole-2,5-dione

  • Ruboxistaurin Hydrochloride
  • (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
  • (S)-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 monohydrochloride
  • Ruboxistaurin HCl
  • Ruboxistaurin(LY333531HCl)
  • LY 333531 hydrochloride - Ruboxistaurin
  • Ruboxistaurin hydrochloride (LY333531)
  • Ruboxistaurin HCl(LY333531 )
  • LY333531 HCl
  • (7S)-7-((Dimethylamino)methyl)-22,25-dihydro-11H,21H,31H-6-oxa-1,3(3,1)-diindola-2(3,4)-pyrrolacyclononaphane-22,25-dione hydrochloride
  • LY333531 Hydrochloride(Ruboxistaurin HCl)
  • Ruboxistaurin|||LY333531 HCl|||LY 333531 hydrochloride
  • LY-333531 hydrochloride, protein kinase Cbeta inhibitor
  • ruboxistaurin/LY 333531 hydrochloride
  • Ruboxistaurin hydrochloride, 10 mM in DMSO
  • CAS:169939-93-9
  • 9H,18H-5,21:12,17-Dimethenodibenzo[e,k]pyrrolo[3,4-h][1,4,13]oxadiazacyclohexadecine-18,20(19H)-dione, 9-[(dimethylamino)methyl]-6,7,10,11-tetrahydro-, monohydrochloride, (9S)- (9CI)
  • 169939-93-9
  • C28H28N4O3HCl
  • C28H29N4O3Cl
  • Amines
  • Heterocycles
  • Inhibitors
  • Intermediates & Fine Chemicals
  • Pharmaceuticals