| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| L422481-1ml |
1ml |
现货  |
|
| 别名 | (R)-5'-苯基-7-脱氮杂腺苷 | 6-氨基-9-[(R)-5'-苯基(呋喃呋喃糖基)]-7-脱氮嘌呤 | (2R,3R,4S,5R)-2-(4-氨基-7H-吡咯并[2,3-d]嘧啶-7-基)-5-((R)-羟基(苯基)甲基)四氢呋喃-3 ,4-二醇 |
|---|---|
| 规格或纯度 | Moligand™, 10mM in DMSO |
| 英文名称 | LLY-283 |
| 生化机理 | LLY-283 是一种新型的精氨酸蛋白甲基转移酶 5（PRMT5）选择性抑制剂。LLY-283 可抑制体外和细胞中 PRMT5 酶的活性，其 IC50 分别为 22 nM 和 25 nM。LLY-283 具有抗肿瘤活性。 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 抑制剂 |
| 作用机制 | 蛋白精氨酸甲基转移酶 5 抑制剂 |
| 产品介绍 |
LLY-283 是一种新型的、选择性的 protein arginine methyltransferase 5 (PRMT5) 的抑制剂。LLY-283 可在体外和细胞中抑制PRMT5的酶活性，对应的IC50值分别为22 nM和25 nM。LLY-283 具有抗肿瘤活性。 Information LLY-283 LLY-283 is a novel and selective inhibitor of protein arginine methyltransferase 5 (PRMT5) . LLY-283 inhibits PRMT5 enzymatic activity in vitro and in cells with IC50 of 22 nM and 25 nM, respectively. LLY-283 shows antitumor activity. Targets PRMT5 (Cell-free assay); PRMT5 (Cell-based assay) 22 nM; 25 nM In vitro LLY-283 inhibits PRMT5 enzymatic activity in vitro and in cells with IC50 of 22 ± 3 and 25 ± 1 nM, respectively. LLY-283 directly binds to and occupies the SAM pocket. LLY-283 is a low nanomolar enzymatic inhibitor of the PRMT5:MEP50 complex in biochemical assays and is selective for PRMT5 over other methyltransferases including related family members. In vivo LLY-283 shows antitumor activity in mouse xenografts when dosed orally and can serves as an excellent probe molecule for understanding the biological function of PRMT5 in normal and cancer cells. LLY-283 can be used as an in vivo tool compound to evaluate the pharmacology of PRMT5 inhibition. Cell Research(from reference) Cell lines：Sf9 cells, A375 tumor cells, MCF7 cells Concentrations：1 µM, 10 µM Incubation Time：48 h |
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| 分子类型 | 小分子 |
|---|---|
| IUPAC Name | (2R,3R,4S,5R)-2-(4-aminopyrrolo[2,3-d]pyrimidin-7-yl)-5-[(R)-hydroxy(phenyl)methyl]oxolane-3,4-diol |
| INCHI | InChI=1S/C17H18N4O4/c18-15-10-6-7-21(16(10)20-8-19-15)17-13(24)12(23)14(25-17)11(22)9-4-2-1-3-5-9/h1-8,11-14,17,22-24H,(H2,18,19,20)/t11-,12+,13-,14-,17-/m1/s1 |
| InChi Key | WWOOWAHTEXIWBO-QFRSUPTLSA-N |
| Canonical SMILES | C1=CC=C(C=C1)C(C2C(C(C(O2)N3C=CC4=C(N=CN=C43)N)O)O)O |
| Isomeric SMILES | C1=CC=C(C=C1)[C@H]([C@@H]2[C@H]([C@H]([C@@H](O2)N3C=CC4=C(N=CN=C43)N)O)O)O |
| MeSH Entry Terms | (2R,3R,4S,5R)-2-(4-aminopyrrolo(2,3-d)pyrimidin-7-yl)-5-((R)-hydroxy(phenyl)methyl)oxolane-3,4-diol;lly-283 |
| 分子量 | 342.35 |
| Reaxy-Rn | 50692630 |
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=50692630&ln= |
| 分子量 | 342.350 g/mol |
|---|---|
| XLogP3 | 0.200 |
| 氢键供体数Hydrogen Bond Donor Count | 4 |
| 氢键受体数Hydrogen Bond Acceptor Count | 7 |
| 可旋转键计数Rotatable Bond Count | 3 |
| 精确质量Exact Mass | 342.133 Da |
| 单同位素质量Monoisotopic Mass | 342.133 Da |
| 拓扑极表面积Topological Polar Surface Area | 127.000 Ų |
| 重原子数Heavy Atom Count | 25 |
| 形式电荷Formal Charge | 0 |
| 复杂度Complexity | 464.000 |
| 同位素原子数Isotope Atom Count | 0 |
| 定义的原子立体中心计数Defined Atom Stereocenter Count | 5 |
| 未定义的原子立体中心计数Undefined Atom Stereocenter Count | 0 |
| 定义的键立体中心计数Defined Bond Stereocenter Count | 0 |
| 未定义的键立体中心计数Undefined Bond Stereocenter Count | 0 |
| 所有立体化学键的总数The total count of all stereochemical bonds | 0 |
| 共价键合单元计数Covalently-Bonded Unit Count | 1 |
| Reaxy-Rn | 50692630 |
|---|---|
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=50692630&ln= |
| RIDADR | NONHforallmodesoftransport |
| Concentration | 9-11（mmol/L） |
|---|---|
| Proton NMR spectrum | Conforms to Structure |
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