Adezmapimod(Synonyms: SB 203580; RWJ 64809)

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Adezmapimod (Synonyms: SB 203580; RWJ 64809) 纯度: 99.86%

Adezmapimod (SB 203580) 是一种选择性的,ATP 竞争性的 p38 MAPK 抑制剂,对 SAPK2a/p38SAPK2b/p38β2IC50 分别为 50 nM 和 500 nM。Adezmapimod 抑制 LCK,GSK3β 和 PKBα,IC50 比 SAPK2a/p38 高 100-500 倍。Adezmapimod 不抑制 JNK 活性,是一种自噬 (autophagy) 和线粒体自噬 (mitophagy) 激活剂。

Adezmapimod(Synonyms: SB 203580;  RWJ 64809)

Adezmapimod Chemical Structure

CAS No. : 152121-47-6

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10 mM * 1 mL in DMSO ¥660 In-stock
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Adezmapimod 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Immunology/Inflammation Compound Library
  • Kinase Inhibitor Library
  • MAPK Compound Library
  • Anti-Cancer Compound Library
  • Autophagy Compound Library
  • Anti-Aging Compound Library
  • Reprogramming Compound Library
  • Oxygen Sensing Compound Library
  • Pyroptosis Compound Library
  • Anti-Lung Cancer Compound Library
  • Neurodegenerative Disease-related Compound Library
  • Angiogenesis Related Compound Library
  • Mitochondria-Targeted Compound Library

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[1].

IC50 & Target[1]

p38

50 nM (IC50)

p38β2

500 nM (IC50)

体外研究
(In Vitro)

Adezmapimod (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 IC50 of 3-5 μM[1].
SB203580 blocks PKB phosphorylation (IC50 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[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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 IC50 of 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.

体内研究
(In Vivo)

Adezmapimod (SB 203580) (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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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).

分子量

377.43

Formula

C21H16FN3OS

CAS 号

152121-47-6

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 50 mg/mL (132.47 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.6495 mL 13.2475 mL 26.4950 mL
5 mM 0.5299 mL 2.6495 mL 5.2990 mL
10 mM 0.2649 mL 1.3247 mL 2.6495 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°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 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: 5% DMSO    40% PEG300    5% Tween-80    50% saline

    Solubility: ≥ 2.5 mg/mL (6.62 mM); Clear solution

  • 2.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 1.56 mg/mL (4.13 mM); Clear solution

    此方案可获得 ≥ 1.56 mg/mL (4.13 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 15.6 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。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 3.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 1.56 mg/mL (4.13 mM); Clear solution

    此方案可获得 ≥ 1.56 mg/mL (4.13 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 15.6 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 4.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 1.56 mg/mL (4.13 mM); Clear solution

    此方案可获得 ≥ 1.56 mg/mL (4.13 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 15.6 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Davies SP, et al. Specificity and mechanism of action of some commonly used protein kinase inhibitors. Biochem J. 2000 Oct 1;351(Pt 1):95-105.

    [2]. Lali FV, et al. The pyridinyl imidazole inhibitor SB203580 blocks phosphoinositide-dependent protein kinase activity, protein kinase B phosphorylation, and retinoblastoma hyperphosphorylation in interleukin-2-stimulated T cells independently of p38 mitogen-activated protein kinase. J Biol Chem. 2000 Mar 10;275(10):7395-402.

    [3]. Leelahavanichkul K, et al. A role for p38 MAPK in head and neck cancer cell growth and tumor-induced angiogenesis and lymphangiogenesis. Mol Oncol. 2014 Feb;8(1):105-18.

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