Isozyme selective inhibitor of protein kinase Cβ (PKCβ). Inhibits both the PKCβI (IC50=4.7nM) and PKCβII (IC50=5.9nM) isozymes. 76- and 61-fold more selective for inhibition of PKCβI and PKCβII over PKCα.Not offered in the US.
Product Details
| Alternative Name: | (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 . HCl, Ruboxistaurin . hydrochloride |
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| Formula: | C28H28N4O3 . HCl |
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| MW: | 468.6 . 36.5 |
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| CAS: | 169939-93-9 |
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| MI: | 14: 8290 |
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| Purity: | ≥98% (HPLC) |
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| Identity: | Determined by 1H-NMR. |
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| Appearance: | Red solid. |
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| Solubility: | Soluble in DMSO; slightly soluble in 100% ethanol or water. |
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| Shipping: | Ambient Temperature |
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| Long Term Storage: | -80°C |
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| Handling: | Protect from light |
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| Regulatory Status: | RUO - Research Use Only |
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Product Literature References
PKCβII-induced upregulation of PGP9.5 and VEGF in postoperative persistent pain in rats: X. Zhu, et al.; J. Pain Res.
11, 2095 (2018),
Abstract;
Full Text
Diabetes-induced increased oxidative stress in cardiomyocytes is sustained by a positive feedback loop involving Rho kinase and PKCβ2.: H. Soliman, et al.; Am. J. Physiol. Heart Circ. Physiol.
303, H989 (2012),
Abstract;
Full Text
Ruboxistaurin: LY 333531: Drugs R. D.
8, 193 (2007), (Review),
Abstract;
Protein kinase C beta inhibitor LY333531 attenuates intercellular adhesion molecule-1 and monocyte chemotactic protein-1 expression in the kidney in diabetic rats: Y. Wu, et al.; J. Pharmacol. Sci.
101, 335 (2006),
Abstract;
Full Text
Ruboxistaurin: C.A. Taulien & S.V. Joy; Drugs Today (Barc)
42, 577 (2006),
Abstract;
Role of p90 ribosomal S6 kinase (p90RSK) in reactive oxygen species and protein kinase C beta (PKC-beta)-mediated cardiac troponin I phosphorylation: S. Itoh, et al.; J. Biol. Chem.
280, 24135 (2005),
Abstract;
Full Text
Protein kinase Cbeta selective inhibitor LY333531 attenuates diabetic hyperalgesia through ameliorating cGMP level of dorsal root ganglion neurons: H. Kim, et al.; Diabetes
52, 2102 (2003),
Abstract;
Full Text
Effects of the protein kinase C beta inhibitor LY333531 on neural and vascular function in rats with streptozotocin-induced diabetes: M.A. Cotter, et al.; Clin Sci (Lond)
103, 311 (2002),
Abstract;
Role of PKC and TGF-beta receptor in glucose-induced proliferation of smooth muscle cells: Y. Yasuda, et al; BBRC
281, 71 (2001),
Abstract;
(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 : M.R. Jirousek, et al.; J. Med. Chem.
39, 2664 (1996),
Abstract;
General Literature References
Protein kinase C and the development of diabetic vascular complications: K.J. Way, et al.; Diabet. Med.
18, 945 (2001), Review,
Abstract;
