RUBOXISTAURIN HYDROCHLORIDE Chemical Properties

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|

Safety Information

WGK Germany 

3

RUBOXISTAURIN HYDROCHLORIDE Usage And Synthesis

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

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

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