敏感性 | 对湿度敏感 |
溶解性 | Soluble in DMSO (30 mg/ml at 25 °C), water (< 1 mg/ml at 25 °C), ethanol (< 1 mg/ml at 25 °C), DMF (~16.6 mg/ml), and 1:3 solution of DMF:PBS(pH 7.2) (~0.25 mg/ml). |
存贮条件 | 储存温度-20°C |
应用 | A potent inhibitor of PKCβ, PKCα, PKCγ and PKCε. |
产品介绍 | Enzastaurin (LY317615)是一种有效的PKCβ选择性抑制剂,IC50为6 nM,比对PKCα, PKCγ和PKCε的作用强6到20倍。 |
备注 | Enzastaurin (LY317615) is a potent PKCβ selective inhibitor with IC50 of 6 nM, 6- to 20-fold selectivity against PKCα, PKCγ and PKCε. Phase 3. |
生化机理 | Enzastaurin (LY317615) is a potent PKC beta inhibitor for PKCβ, PKCα, PKCγ and PKCε with IC50 of 6 nM, 39 nM, 83 nM and 110 nM, respectively. Enzastaurin inhibits growth in all MM cell lines investigated, including MM.1S, MM.1R, RPMI 8226 (RPMI), RPMI-Dox40 (Dox40), NCI-H929, KMS-11, OPM-2, and U266, with IC50 values ranging from 0.6 to 1.6 μM. Enzastaurin induces apoptosis and suppresses proliferation in cultured tumor cells, including malignant lymphocytes of CTCL. Enzastaurin also suppresses the phosphorylation of GSK3βser9, ribosomal protein S6S240/244, and AKTThr308 |
别名 | 恩扎妥林;因扎妥雷;LY 317615; 3-(1-甲基-1H-吲哚-3-基)-4-(1-(1-(2-吡啶甲基)-4-哌啶基)-1H-吲哚-3-基)-1H-吡咯-2,5-二酮;LY317615; LY-317615; LY 317615;D04014;3-(1-Methyl-1H-indol-3-yl)-4-[1-[1-(2-pyridinylmethyl)-4-piperidinyl]-1H-indol-3-yl]-1H-pyrrole-2,5-dione |
Enzastaurin(LY317615),PKCβ抑制剂
Enzastaurin (LY317615) (订货以英文为准)
编号:E125760
CAS号:170364-57-5
分子式:C32H29N5O2
分子量:515.61
产品名称 | Enzastaurin (LY317615) |
中文名称 | Enzastaurin(LY317615),PKCβ抑制剂 |
CAS号 | 170364-57-5 |
MDL编码 | MFCD11040980 |
分子式(M.F.) | C32H29N5O2 |
分子量(M.W.) | 515.61 |
储存条件 | -20°C储存 |
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