Adezmapimod (SB 203580) 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。Adezmapimod hydrochloride 抑制 LCK，GSK3β 和 PKBα，IC50比 SAPK2a/p38 高 100-500 倍。Adezmapimod hydrochloride 是一种自噬 (autophagy) 和有丝分裂 (mitophagy) 激活剂。
| 生物活性 | Adezmapimod (SB 203580) hydrochloride is a selective and ATP-competitivep38 MAPKinhibitor withIC50s of 50 nM and 500 nM forSAPK2a/p38andSAPK2b/p38β2, respectively. Adezmapimod hydrochloride inhibits LCK, GSK3β and PKBα with IC50s of 100-500-fold higher than that for SAPK2a/p38. Adezmapimod hydrochloride is anautophagyandmitophagyactivator[1]. |
| IC50& Target[1] | p38 50 nM (IC50) | p38β2 500 nM (IC50) |
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体外研究
(In Vitro) | Adezmapimod hydrochloride (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 IC50of 3-5 μM[1].
Adezmapimod hydrochloride blocks PKB phosphorylation (IC503-5 μM). Adezmapimod hydrochloride 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[1].
Cell Proliferation Assay[1] | 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 IC50of 3-5 μM. |
Western Blot Analysis[1] | 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. |
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体内研究
(In Vivo) | Adezmapimod hydrochloride (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[1].
| Animal Model: | Six-week-old female atymic Nu/Nu mice CAL27 p38WT and p38TM tumors[1] | | 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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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| 溶解性数据 | In Vitro: DMSO : 100 mg/mL(241.60 mM;Need ultrasonic) H2O : 8.43 mg/mL(20.37 mM;Need ultrasonic and warming) 配制储备液 | 1 mM | 2.4160 mL | 12.0802 mL | 24.1604 mL | | 5 mM | 0.4832 mL | 2.4160 mL | 4.8321 mL | | 10 mM | 0.2416 mL | 1.2080 mL | 2.4160 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (6.04 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (6.04 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (6.04 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (6.04 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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