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869185-85-3

中文名稱(chēng) 869185-85-3
英文名稱(chēng) SB 203580 (hydrochloride)
CAS 869185-85-3
分子式 C21H17ClFN3OS
分子量 413.896
MOL 文件 869185-85-3.mol
更新日期 2023/03/20 15:41:25
869185-85-3 結(jié)構(gòu)式 869185-85-3 結(jié)構(gòu)式

基本信息

中文別名
化合物 T21675
英文別名
RWJ 64809 hydrochloride
SB 203580, Hydrochloride - CAS 869185-85-3 - Calbiochem
RWJ 64809 HYDROCHLORIDE
SB203580 HYDROCHLORIDE
SB-203580 HYDROCHLORIDE

物理化學(xué)性質(zhì)

儲(chǔ)存條件-20C
溶解度insoluble in EtOH; insoluble in H2O; ≥20.7 mg/mL in DMSO
形態(tài)亮黃色固體
顏色Light yellow to yellow
水溶解性Soluble to 25 mM in water
穩(wěn)定性吸濕性

安全數(shù)據(jù)

危險(xiǎn)性符號(hào)(GHS)GHS hazard pictograms
GHS07
警示詞警告
危險(xiǎn)性描述H302-H315-H319-H335
海關(guān)編碼2933399990

常見(jiàn)問(wèn)題列表

生物活性
SB 203580 hydrochloride (RWJ 64809 hydrochloride) 是一種選擇性的,ATP 競(jìng)爭(zhēng)性的 p38 MAPK 抑制劑,對(duì) SAPK2a/p38 和 SAPK2b/p38β2 的 IC50 分別為 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 是一種自噬 (autophagy) 和有絲分裂 (mitophagy) 激活劑。
靶點(diǎn)

p38

50 nM (IC 50 )

p38β2

500 nM (IC 50 )

體外研究

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.
體內(nèi)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).
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