MRK003 is a γ-secretase inhibitor exhibits promising in vitro pre-clinical activity in multiple myeloma and non-Hodgkin's lymphoma. MRK003 treatment induced caspase-dependent apoptosis and inhibited proliferation of MM and NHL cell lines and patient cells. Examination of signaling events after treatment showed time-dependent decrease in levels of the notch intracellular domain, Hes1 and c-Myc. MRK003 downregulated cyclin D1, Bcl-Xl and Xiap levels in NHL cells and p21, Bcl-2 and Bcl-Xl in MM cells. In addition, MRK003 caused an upregulation of pAkt, indicating crosstalk with the PI3K/Akt pathway. (3'R,6S,9R)-5,6,7,8,9,10-六氢-5'-(2,2,2-三氟乙基)-2-[(1E)-3-[4-(三氟甲基)-1-哌啶基]-1-丙烯-1-基]螺[6,9-亚甲基苯并环辛烯E-11,3'-[1,2,5]噻二唑烷]1',1'-二氧化物
CAS 623165-93-5 MFCD23165935
化学结构图
SMILES: O=S1(=O)N[C@]2(CN1CC(F)(F)F)[C@@H]1CC[C@@H]2Cc2cc(/C=C/CN3CCC(C(F)(F)F)CC3)ccc2C1
化学属性
| Mol. Formula | C25H31F6N3O2S |
|---|---|
| Mol. Weight | 551.59 |
| Appearance | Solid powder |
| Solubility | Soluble in DMSO, not in water |
别名和识别编码
| Chemical Name | MRK003 is a γ-secretase inhibitor exhibits promising in vitro pre-clinical activity in multiple myeloma and non-Hodgkin's lymphoma. MRK003 treatment induced caspase-dependent apoptosis and inhibited proliferation of MM and NHL cell lines and patient cells. Examination of signaling events after treatment showed time-dependent decrease in levels of the notch intracellular domain, Hes1 and c-Myc. MRK003 downregulated cyclin D1, Bcl-Xl and Xiap levels in NHL cells and p21, Bcl-2 and Bcl-Xl in MM cells. In addition, MRK003 caused an upregulation of pAkt, indicating crosstalk with the PI3K/Akt pathway. |
|---|---|
| Chemical Name Translation | (3'R,6S,9R)-5,6,7,8,9,10-六氢-5'-(2,2,2-三氟乙基)-2-[(1E)-3-[4-(三氟甲基)-1-哌啶基]-1-丙烯-1-基]螺[6,9-亚甲基苯并环辛烯E-11,3'-[1,2,5]噻二唑烷]1',1'-二氧化物 |
| Chemicalbook ID | CB62604251 |
| Formula | C25H31F6N3O2S |
| Synonym | MRK003; MRK 003; MRK-003. |
| IUPAC Name | (3'R,6R,9R)-5'-(2,2,2-trifluoroethyl)-2-((E)-3-(4-(trifluoromethyl)piperidin-1-yl)prop-1-en-1-yl)-5,6,7,8,9,10-hexahydrospiro[6,9-methanobenzo[8]annulene-11,3'-[1,2,5]thiadiazolidine] 1',1'-dioxide. |
| InChIKey | NKHUILHBYOOZDF-RWIQBJEJSA-N |
| InChI | InChI=1S/C25H31F6N3O2S/c26-24(27,28)16-34-15-23(32-37(34,35)36)21-5-6-22(23)14-19-12-17(3-4-18(19)13-21)2-1-9-33-10-7-20(8-11-33)25(29,30)31/h1-4,12,20-22,32H,5-11,13-16H2/b2-1+/t21-,22-,23-/m1/s1 |
| Canonical SMILES | FC(C1CCN(C/C=C/C2=CC=C3C(C[C@@]4([H])CC[C@]([C@@]4(CN5CC(F)(F)F)NS5(=O)=O)([H])C3)=C2)CC1)(F)F |
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- MRK003 is a γ-secretase inhibitor exhibits promising in vitro pre-clinical activity in multiple myeloma and non-Hodgkin's lymphoma. MRK003 treatment induced caspase-dependent apoptosis and inhibited proliferation of MM and NHL cell lines and patient cells. Examination of signaling events after treatment showed time-dependent decrease in levels of the notch intracellular domain, Hes1 and c-Myc. MRK003 downregulated cyclin D1, Bcl-Xl and Xiap levels in NHL cells and p21, Bcl-2 and Bcl-Xl in MM cells. In addition, MRK003 caused an upregulation of pAkt, indicating crosstalk with the PI3K/Akt pathway.
