PF-543
|
|
|
- CAS号:
- 1706522-79-3
- 英文名:
- PF-543
- 英文别名:
- PF 543 HCl;WNKWAZFYPZMDGJ-VQIWEWKSSA-N;PF-543 Hydrochloride
DISCONTINUED;(2R)-1-[[(4-[[3-Methyl-5-[(phenylsulfonyl)methyl]phenoxy]methyl]phenyl]methyl]-2-pyrrolidinemethanol hydrochloride;Nrf-2,PF543 hydrochloride,anti-cancer,sphingosine-competitive,S1P,Sphingosine Kinase 1 Inhibitor II,Apoptosis,inhibit,PF 543,Lysophospholipid Receptor,PAH,necrosis,SphK,Inhibitor,Autophagy,PF543,PF 543 hydrochloride,caspase-3/7,SK1,Sphingosine kinase,LPL Receptor,anti-inflammatory
- 中文名:
- PF-543
- 中文别名:
- 化合物PF-543;PF 543 盐酸盐;(R)-(1-(4-((3-甲基-5-((苯基磺酰基)甲基)苯氧基)甲基)苄基)吡咯烷-2-基)甲醇盐酸盐;(R)-(1-(4-((3-METHYL-5-((PHENYLSULFONYL)METHYL)PHENOXY)METHYL)BENZYL)PYRROLIDIN-2-YL)METHANOL HYDROCHLORIDE
- CBNumber:
- CB43355459
- 分子式:
- C27H32ClNO4S
- 分子量:
- 502.07
- MOL File:
- 1706522-79-3.mol
|
|
|
PF-543化学性质
-
熔点:
-
156-158oC (dec.)
-
|
-
储存条件:
-
under inert gas (nitrogen or Argon) at 2-8°C
-
|
-
溶解度:
-
DMSO, Methanol
-
|
-
形态:
-
Solid
-
|
-
颜色:
-
Beige
-
|
PF-543性质、用途与生产工艺
PF-543 是一种新型Sphingosine kinase 1 (SphK1， SK1) （鞘氨醇激酶）抑制剂，Ki为3.6 nM。PF-543 可诱导细胞凋亡、坏死和自噬。
| Target | Value |
SphK1
(Cell-free assay)
|
2.0 nM
|
SphK1
(Cell-free assay)
|
3.6 nM(Ki)
|
PF543是一种细胞渗透性羟基甲基吡咯烷化合物，其以可逆的，鞘氨醇竞争性方式抑制SphK-1/SphK1催化的鞘氨醇磷酸化，对S1P受体没有亲和力，对Sphk2 (10 μM下抑制6.8%)或 46种其他脂质和蛋白激酶(IC50 >10 μM)的抑制活性很弱。在SphK1过表达的1483头颈癌细胞中，PF-543减少10倍的内源性S1P水平，并成比例增加鞘氨醇水平。PF-543与SphK1可逆结合(k
off
t1/2=8.5 min)，具有高亲和力，结合常数(K
d
)为5 nM。PF543不影响1483，A549，LN229，Jurkat，U937和MCF-7细胞的增殖和存活，尽管会使细胞中S1P/鞘氨醇比率发生巨大改变。在全血中，PF-543是有效的S1P形成抑制剂，表明鞘氨醇激酶的SphK1亚型是人血中S1P的主要来源。
PF-543
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/01/16 | S7177 | PF-543
PF-543 | 1706522-79-3 | 5mg | 794.43元 |
| 2024/01/16 | S7177 | PF-543 hydrochloride | 1706522-79-3 | 10mM (1mL in DMSO) | 958.23元 |
1706522-79-3, PF-543 相关搜索:
- 药靶配体
- PF 543 盐酸盐
- (R)-(1-(4-((3-METHYL-5-((PHENYLSULFONYL)METHYL)PHENOXY)METHYL)BENZYL)PYRROLIDIN-2-YL)METHANOL HYDROCHLORIDE
- 化合物PF-543
- (R)-(1-(4-((3-甲基-5-((苯基磺酰基)甲基)苯氧基)甲基)苄基)吡咯烷-2-基)甲醇盐酸盐
- 1706522-79-3
- Nrf-2,PF543 hydrochloride,anti-cancer,sphingosine-competitive,S1P,Sphingosine Kinase 1 Inhibitor II,Apoptosis,inhibit,PF 543,Lysophospholipid Receptor,PAH,necrosis,SphK,Inhibitor,Autophagy,PF543,PF 543 hydrochloride,caspase-3/7,SK1,Sphingosine kinase,LPL Receptor,anti-inflammatory
- WNKWAZFYPZMDGJ-VQIWEWKSSA-N
- (2R)-1-[[(4-[[3-Methyl-5-[(phenylsulfonyl)methyl]phenoxy]methyl]phenyl]methyl]-2-pyrrolidinemethanol hydrochloride
- PF 543 HCl
- PF-543 Hydrochloride
DISCONTINUED