869185-85-3
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- CAS号:
- 869185-85-3
- 英文名:
- SB 203580 (hydrochloride)
- 英文别名:
- RWJ 64809 hydrochloride;Adezmapimod (hydrochloride);Adezmapimod (SB-203580) hydrochloride;SB 203580, Hydrochloride - CAS 869185-85-3 - Calbiochem;RWJ 64809 HYDROCHLORIDE;SB203580 HYDROCHLORIDE;SB-203580 HYDROCHLORIDE
- 中文名:
- 869185-85-3
- 中文别名:
- 化合物 T21675;SB 203580盐酸盐
- CBNumber:
- CB52592405
- 分子式:
- C21H17ClFN3OS
- 分子量:
- 413.9
- MOL File:
- 869185-85-3.mol
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869185-85-3化学性质
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储存条件:
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-20C
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溶解度:
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insoluble in EtOH; insoluble in H2O; ≥20.7 mg/mL in DMSO
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形态:
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Bright yellow solid
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水溶解性:
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Soluble to 25 mM in water
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稳定性:
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Hygroscopic
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869185-85-3性质、用途与生产工艺
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。
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p38
50 nM (IC
50
)
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p38β2
500 nM (IC
50
)
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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
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Cell Line:
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CT6, BA/F3 cell line F7, and PBMC/T cells
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Concentration:
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0-30 μM
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Incubation Time:
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Preincubated with 0-30 μM SB203580 for 1 h and cultured for 24 h in the presence of 20 ng/mL IL-2
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Result:
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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.
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Western Blot Analysis
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Cell Line:
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CT6 cells, activated human T cells, and BA/F3 F7 cells
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Concentration:
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0-30 μM
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Incubation Time:
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Preincubated with 0-30 μM SB203580 for 1 h before stimulating with 20 ng/mL IL-2 for 5 min
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Result:
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Inhibited the phosphorylation of PKB at Ser473 in a dose-dependent manner.
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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.
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Animal Model:
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Six-week-old female atymic Nu/Nu mice CAL27 p38WT and p38TM tumors
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Dosage:
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5 mg/kg/day
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Administration:
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Intra peritoneal injected daily for 16 consecutive days
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Result:
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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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869185-85-3
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 |
|---|
| 2024/04/30 | HY-10256A | Adezmapimod hydrochloride | | 5 mg | 330元 |
| 2024/04/30 | HY-10256A | 869185-85-3
Adezmapimod hydrochloride | 869185-85-3 | 10mM * 1mLin DMSO | 363元 |
869185-85-3, 869185-85-3 相关搜索:
- 药靶配体
- C21H17ClFN3OS
- SB 203580盐酸盐
- 化合物 T21675
- 869185-85-3
- Adezmapimod (SB-203580) hydrochloride
- Adezmapimod (hydrochloride)
- SB 203580, Hydrochloride - CAS 869185-85-3 - Calbiochem
- RWJ 64809 HYDROCHLORIDE;SB203580 HYDROCHLORIDE;SB-203580 HYDROCHLORIDE
- RWJ 64809 hydrochloride