产品
编 号：F179594
分子式：C21H16FN3OS
分子量：377.43
分子式：C21H16FN3OS
分子量：377.43
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
528
In-stock
5mg
300
In-stock
10mg
480
In-stock
50mg
1120
In-stock
100mg
1680
In-stock
结构图
CAS No: 152121-47-6
产品详情
生物活性：
Adezmapimod (SB 203580) is a selective and ATP-competitive p38 MAPK inhibitor with IC50s of 50 nM and 500 nM for SAPK2a/p38 and SAPK2b/p38β2, respectively. Adezmapimod inhibits LCK, GSK3β and PKBα with IC50s of 100-500-fold higher than that for SAPK2a/p38. Adezmapimod does not disrupt JNK activity and is an autophagy and mitophagy activator.
体内研究：
Adezmapimod (SB 203580) (5 mg/kg/天；每天腹膜内注射，连续 16 天，在雌性无染色体 Nu/Nu 小鼠中) 处理，与平行处理的 p38TM 肿瘤相比，p38WT 肿瘤的肿瘤负荷明显更小。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).
体外研究：
Adezmapimod (SB 203580) (用 0-30 μM 预孵育 1 小时并在 20 ng/mL IL-2 存在下培养 24 小时) 防止 IL-2 诱导的原代人 T 细胞、鼠 CT6 T 细胞增殖或 BAF F7 B 细胞，IC50 为 3-5 μM。 SB203580 阻断 PKB 磷酸化 (IC50 3-5 微米)。SB203580 在 CT6 和活化的人 T 细胞以及 IL-2 反应性 BA/F3 F7 B 细胞中以剂量依赖性方式抑制 Ser473 的磷酸化。
Adezmapimod (SB 203580) is a selective and ATP-competitive p38 MAPK inhibitor with IC50s of 50 nM and 500 nM for SAPK2a/p38 and SAPK2b/p38β2, respectively. Adezmapimod inhibits LCK, GSK3β and PKBα with IC50s of 100-500-fold higher than that for SAPK2a/p38. Adezmapimod does not disrupt JNK activity and is an autophagy and mitophagy activator.
体内研究：
Adezmapimod (SB 203580) (5 mg/kg/天；每天腹膜内注射，连续 16 天，在雌性无染色体 Nu/Nu 小鼠中) 处理，与平行处理的 p38TM 肿瘤相比，p38WT 肿瘤的肿瘤负荷明显更小。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).
体外研究：
Adezmapimod (SB 203580) (用 0-30 μM 预孵育 1 小时并在 20 ng/mL IL-2 存在下培养 24 小时) 防止 IL-2 诱导的原代人 T 细胞、鼠 CT6 T 细胞增殖或 BAF F7 B 细胞，IC50 为 3-5 μM。 SB203580 阻断 PKB 磷酸化 (IC50 3-5 微米)。SB203580 在 CT6 和活化的人 T 细胞以及 IL-2 反应性 BA/F3 F7 B 细胞中以剂量依赖性方式抑制 Ser473 的磷酸化。
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