869185-85-3

生物活性靶点体外研究体内研究 869185-85-3 试剂级价格

869185-85-3

CAS号:869185-85-3
英文名:SB 203580 (hydrochloride)
中文名:869185-85-3
CBNumber:CB52592405
分子式:C21H17ClFN3OS
分子量:413.9
MOL File:869185-85-3.mol

869185-85-3化学性质

储存条件 :-20C
溶解度 :insoluble in EtOH; insoluble in H2O; ≥20.7 mg/mL in DMSO
形态 :Bright yellow solid
颜色 :Light yellow to yellow
水溶解性 :Soluble to 25 mM in water
稳定性 :Hygroscopic

安全信息

海关编码 :2933399990

869185-85-3性质、用途与生产工艺

生物活性 SB 203580 hydrochloride (RWJ 64809 hydrochloride) 是一种选择性的，ATP 竞争性的 p38 MAPK 抑制剂，对 SAPK2a/p38 和 SAPK2b/p38β2 的 IC50 分别为 50 nM 和 500 nM。SB 203580 hydrochloride 抑制 LCK，GSK3β 和 PKBα，IC50 比 SAPK2a/p38 高 100-500 倍。SB 203580 hydrochloride 是一种自噬 (autophagy) 和有丝分裂 (mitophagy) 激活剂。
靶点

p38

50 nM (IC ₅₀ )

p38β2

500 nM (IC ₅₀ )

体外研究

SB 203580 (preincubated with 0-30 μM for 1 h and cultured for 24 h in the presence of 20 ng/mL IL-2) prevents the IL-2-induced proliferation of primary human T cells, murine CT6 T cells, or BAF F7 B cells with an IC ₅₀ of 3-5 μM.
SB203580 blocks PKB phosphorylation (IC ₅₀ 3-5 μM). SB203580 inhibitsthe phosphorylation of Ser473 in a dose-dependent manner in both CT6 and activated human T cells and IL-2-responsive BA/F3 F7 B cells.

Cell Proliferation Assay

Cell Line:	CT6, BA/F3 cell line F7, and PBMC/T cells
Concentration:	0-30 μM
Incubation Time:	Preincubated with 0-30 μM SB203580 for 1 h and cultured for 24 h in the presence of 20 ng/mL IL-2
Result:	Prevented the IL-2-induced proliferation of primary human T cells, murine CT6 T cells, or BAF F7 B cells with an IC ₅₀ of 3-5 μM.

Western Blot Analysis

Cell Line:	CT6 cells, activated human T cells, and BA/F3 F7 cells
Concentration:	0-30 μM
Incubation Time:	Preincubated with 0-30 μM SB203580 for 1 h before stimulating with 20 ng/mL IL-2 for 5 min
Result:	Inhibited the phosphorylation of PKB at Ser473 in a dose-dependent manner.

体内研究

SB203580 (5 mg/kg/day; intra peritoneal injected daily for 16 consecutive days, in female atymic Nu/Nu mice) treatment, p38WT tumors show a significantly smaller tumor burden when compared with p38TM tumors that were treated in parallel.

Animal Model:	Six-week-old female atymic Nu/Nu mice CAL27 p38WT and p38TM tumors
Dosage:	5 mg/kg/day
Administration:	Intra peritoneal injected daily for 16 consecutive days
Result:	After 2 weeks treatment, CAL27 p38WT tumors were significantly smaller; CAL27 p38TM tumors were not affected by the p38 inhibitor (n=10).