Ruboxistaurin hydrochloride
Cat. No.：YN310052
CAS No. ：169939-93-9
| 产品名称: | Ruboxistaurin hydrochloride |
| CAS No.: | 169939-93-9 |
| Chemical Name: | (9S)-[(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 |
| Synonyms: | LY 333531 hydrochloride |
| 分子量: | 505.01 |
| 分子式: | C₂₈H₂₉ClN₄O₃ |
| SMILES: | O=C1NC(C(C2=CN(C3=CC=CC=C32)CCO[C@H](CN(C)C)CC4)=C1C5=CN4C6=CC=CC=C56)=O.[H]Cl |
| 存储: | Please store the product under the recommended conditions in theCertificate of Analysis. |
| 运输: | Room temperature in continental US; may vary elsewhere. |
| 产品描述: | Ruboxistaurin hydrochloride (LY 333531 hydrochloride) 是一种选择性的，ATP-竞争性的PKCβ抑制剂，对PKCβI和PKCβII的IC50值分别为 4.7 nM 和 5.9 nM，对 PKCη (IC50，52 nM)，PKCα (IC50，360 nM)，PKCγ (IC50，300 nM) 和 PKCδ (IC50，250 nM) 的抑制作用相对较弱，而对 PKCζ (IC50，>100 μM) 无作用。 |
| IC50和靶点: | [{name:"PKCβI:4.7 nM (IC50)"},{name: "PKCβII:5.9 nM (IC50)"},{name: "PKCη:52 nM (IC50)"},{name: "PKCδ:250 nM (IC50)"},{name: "PKCγ:300 nM (IC50)"},{name: "PKCα:360 nM (IC50)"},{name: "PKCε:600 nM (IC50)"}] |
| In Vitro: | |
| In Vivo: | |
| Clinical Trial: | |
| Solvent & Solubility: |
Jirousek, M.R., Gillig, J.R., Gonzalez, C.M., et al.(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 CβJ. Med. Chem.39(14),2664-2671(1996)
Vignaux, P.A., Minerali, E., Foil, D.H., et al.Machine learning for discovery of GSK3b inhibitorsACS Omega5(41),26551-26561(2020)
Gray, R.D., Lucas, C.D., MacKellar, A., et al.Activation of conventional protein kinase C (PKC) is critical in the generation of human neutrophil extracellular trapsJ. Inflamm. (Lond)10(1),12(2013)
Kim, H., Sasaki, T., Maeda, K., et al.Protein kinase Cβ selective inhibitor LY333531 attenuates diabetic hyperalgesia through ameliorating cGMP level of dorsal root ganglion neuronsDiabetes52(8),2102-2109(2019)
