NSC 95397

生物活性靶点体外研究 NSC 95397 试剂级价格

NSC 95397

CAS号:93718-83-3
英文名:NSC 95397
中文名:NSC 95397
CBNumber:CB7402539
分子式:C14H14O4S2
分子量:310.39
MOL File:93718-83-3.mol

NSC 95397化学性质

储存条件 :-20°C
溶解度 :DMSO: 16 mg/mL
形态 :Orange solid
颜色 :orange, solid
稳定性 :Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 1 month.

安全信息

危险品标志 :Xi
WGK Germany :3
危险等级 :IRRITANT

NSC 95397性质、用途与生产工艺

生物活性 NSC 95397 是一种有效的、选择性 Cdc25 双特异性磷酸酶抑制剂，对于 Cdc25A、Cdc25B 和 Cdc25C 的Ki值分别为32 nM、96 nM 和 40 nM。NSC 95397 对 hCdc25A、hCdc25C 和 hCdc25B 的IC50值分别为22.3 nM、56.9 nM和125 nM。NSC 95397 抑制 mitogen-activated protein kinase phosphatase-1 (MKP-1) 和增殖，并通过 MKP-1 和 ERK1/2 途径诱导结肠癌细胞凋亡。
靶点
Target Value
MKP-1
()
Cdc25A
(Cell-free assay) 22.3 nM
Cdc25A
(Cell-free assay) 32 nM(Ki)
Cdc25C
(Cell-free assay) 40 nM(Ki)
Cdc25B
(Cell-free assay) 56.9 nM

体外研究

NSC 95397 (0, 10, and 20 µM; 24 hour) decreases the cell viability of three colon cancer cell lines SW480, SW620, and DLD-1 in a concentration-dependent manner.
NSC 95397(10 μM; 24 hour) upregulates p21 while downregulates CDK4 and CDK6 were d in all three colon cancer cell lines SW480, SW620, and DLD-1 cells.
NSC 95397 (10 μM; 24 hour) reduces the phosphorylation of retinoblastoma protein (Rb) on Ser795 and Ser807/811.
NSC 95397 (20 μM; 24 hours) significantly increases cleaved caspase-9, -3, -7 and PARP levels.
NSC 95397 (10 μM; 6 hours) enhances the phosphorylation of its downstream ERK1/2 at Thr202/Tyr 204.

Cell Viability Assay

Cell Line:	Human colon cancer cell lines, SW480, SW620, and DLD-1
Concentration:	0, 10, and 20 µM
Incubation Time:	24 hours
Result:	The IC ₅₀ values of NSC 95397 for the cell growth of SW480, SW620, and DLD-1 cells were 9.9, 14.1 and 18.6 μM, respectively.

Western Blot Analysis

Cell Line:	SW480, SW620, and DLD-1 cells
Concentration:	10 μM
Incubation Time:	24 hours
Result:	p21 was upregulated while CDK4 and CDK6 were downregulated. Rduced the phosphorylation of Rb on Ser795 and Ser807/811