1. Stem Cell/Wnt MAPK/ERK Pathway Autophagy
  2. Organoid p38 MAPK Autophagy Mitophagy
  3. Adezmapimod hydrochloride

Adezmapimod hydrochloride  (Synonyms: SB 203580 hydrochloride; RWJ 64809 hydrochloride)

目录号: HY-10256A 纯度: 99.68%
COA 产品使用指南

Adezmapimod (SB 203580) hydrochloride 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 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。

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Adezmapimod hydrochloride Chemical Structure

Adezmapimod hydrochloride Chemical Structure

CAS No. : 869185-85-3

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10 mM * 1 mL in DMSO ¥363
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Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 399 篇科研文献

WB
IF
IHC

    Adezmapimod hydrochloride purchased from MCE. Usage Cited in: Biomaterials. 2018 Aug;175:19-29.  [Abstract]

    Western blotting analysis showing the related protein expression (MHC, MyoD, p38α, phospho-p38α) of C2C12 myoblasts after incubated for 6 days in DM containing 40 μg/mL AuNPs and Au-AgNPs in the presence or absence of SB203580 (SB).

    Adezmapimod hydrochloride purchased from MCE. Usage Cited in: PLoS Biol. 2018 May 11;16(5):e2004225.  [Abstract]

    Representative western blots of p-CREB (Ser133) and UCP-1 in iWAT from C57BL/6J mice after 4 wk of SB203580 treatment. These mice are exposed to cold for 2 d before analysis.

    Adezmapimod hydrochloride purchased from MCE. Usage Cited in: J Neuroinflammation. 2018 Jun 15;15(1):184.  [Abstract]

    Representative immunoblots of total lysates from BV2 cells treated with MPP+or/and U0126 (10 μM), SP600125 (SP, 10 μM) and SB203580 (SB, 10 μM) using the antibodies against DICER.

    Adezmapimod hydrochloride purchased from MCE. Usage Cited in: Phytomedicine. 2018 Mar 15;42:152-163.  [Abstract]

    Cells are pretreated with SP600125 (20 μM), SB203580 (20 μM) or U0126 (20 μM) in presence or absence of KLA, then incubated with LPS (1 μg/mL) for certain time. Cell lysates are subjected to western blot.

    Adezmapimod hydrochloride purchased from MCE. Usage Cited in: Biomed Pharmacother. 2018 Oct 3;108:1294-1302.  [Abstract]

    As for both 0 g and 3 g groups, the p-p38&p38 is downregulated by inhibitors SB203580, SP600125, and U0126.

    Adezmapimod hydrochloride purchased from MCE. Usage Cited in: Biomed Pharmacother. 2018 Oct 3;108:1294-1302.  [Abstract]

    As for both 0 g and 3 g groups, the p-ERK1/2/ERK1/2 is notably reduced by inhibitors SB203580, SP600125, and U0126.

    Adezmapimod hydrochloride purchased from MCE. Usage Cited in: Biomed Pharmacother. 2018 Oct 3;108:1294-1302.  [Abstract]

    As for both 0 g and 3 g groups, the p-JNK1&JNK1 is downregulated by inhibitors SB203580, SP600125, and U0126.

    Adezmapimod hydrochloride purchased from MCE. Usage Cited in: Biomed Pharmacother. 2018 Oct 3;108:1294-1302.  [Abstract]

    The protein level of MMP-9 is downregulated by inhibitors SB203580, SP600125, and U0126.

    Adezmapimod hydrochloride purchased from MCE. Usage Cited in: Biomed Pharmacother. 2018 Oct 3;108:1294-1302.  [Abstract]

    The protein levels of IL-1β and TNF-α are sharply downregulated by the addition of inhibitors SB203580, SP600125, and U0126.

    Adezmapimod hydrochloride purchased from MCE. Usage Cited in: Br J Pharmacol. 2018 Dec;175(23):4338-4352.  [Abstract]

    Treatment of macrophages with inhibitor of p38 (SB203580) or JNK (SP600125) inhibits the synthesis of pro-IL-1β in ZFP91-overexpressing THP-1 cells.

    Adezmapimod hydrochloride purchased from MCE. Usage Cited in: Front Immunol. 2018 Dec 7;9:2854.  [Abstract]

    Neutrophils are pretreated with inhibitor of p38 MAPK (SB203580) and ERK1/2 (U0126), and the cells are then incubated with either SS2 ZY05719 or PMA for 3 h. Immunofluorescence is performed.

    Adezmapimod hydrochloride purchased from MCE. Usage Cited in: Acta Physiol (Oxf). 2018 Feb;222(2).  [Abstract]

    P38 inhibitor SB203580 pretreatment also decreases p-HSP27 and MMP9 levels induced by MICAL2-overexpression.

    Adezmapimod hydrochloride purchased from MCE. Usage Cited in: J Agric Food Chem. 2018 Jun 27;66(25):6317-6325.  [Abstract]

    HepG2 cells are pre-incubated with 20 µM SB203580, SP600125 and PD98059 for 1 h and then treated with tangeretin(20µM) for 24 h.

    Adezmapimod hydrochloride purchased from MCE. Usage Cited in: Am J Physiol Cell Physiol. 2018 Aug 1;315(2):C225-C235.  [Abstract]

    Western blot analysis shows that inhibiting MAPK cannot completely reverse increased expression of RNF2 and CDDP resistance of OC cells.

    Adezmapimod hydrochloride purchased from MCE. Usage Cited in: J Cell Mol Med. 2018 Nov;22(11):5450-5467.  [Abstract]

    Treatment with SB203580 significantly abolishes siPlectin-stimulated p38 activation.

    Adezmapimod hydrochloride purchased from MCE. Usage Cited in: FASEB J. 2019 Feb;33(2):2435-2450.  [Abstract]

    Bile acids (BAs) cause nuclear translocation of NF-kB p65, an effect that is abolished by SB203580.

    Adezmapimod hydrochloride purchased from MCE. Usage Cited in: J Endod. 2018 May;44(5):751-758.  [Abstract]

    p38 MAPK inhibition enhances DPC-Exos–induced tube formation. (A) p38 MAPK activity is measured by detecting Phospho-p38 MAPK. The ratio between Phospho-p38 MAPK and the p38 MAPK band is used for quantification. (B) The effects of VEGF-A and KDR expression after p38 MAPK inhibitor SB203580 treatment on DPC-Exos-stimulated HUVECs.

    Adezmapimod hydrochloride purchased from MCE. Usage Cited in: J Cell Biochem. 2018 Dec 2.  [Abstract]

    Western analysis of protein expression in the treatment of miR-543 and SB 203580.

    Adezmapimod hydrochloride purchased from MCE. Usage Cited in: J Cell Biochem. 2018 Nov;119(10):8450-8459.  [Abstract]

    Western blot results show a reduction in phosphorylated p38 MAPK in ADSCs after treatment with 20 μM SB203580, 20 μM SP600125, or 20 μM PD98059 for 1 hour.

    Adezmapimod hydrochloride purchased from MCE. Usage Cited in: BMC Pulm Med. 2018 Nov 27;18(1):178.  [Abstract]

    P-p38 and P-Hsp27 are detected by western blotting with the treatment of LPS, SB203580 and SB203580+ LPS.

    Adezmapimod hydrochloride purchased from MCE. Usage Cited in: BMC Pulm Med. 2018 Nov 27;18(1):178.  [Abstract]

    P-p38 and P-Hsp27 are detected by western blotting with the treatment of LPS, SB203580 and SB203580+ LPS.

    Adezmapimod hydrochloride purchased from MCE. Usage Cited in: Cell Physiol Biochem. 2018;46(5):1779-1792.  [Abstract]

    Western blot bands of p38, phospho-p38, ZO-1, Clau-din-1, and Occludin. JNK inhibitor SP600125 and p38 inhibitor SB203580 are used.

    Adezmapimod hydrochloride purchased from MCE. Usage Cited in: Cell Death Differ. 2017 Mar;24(3):492-499.  [Abstract]

    LPS stimulates ICER expression via p38-CREB pathway. Effect of MAPK and IKK inhibitors on LPS-induced CREB phosphorylation in peritoneal macrophages.

    Adezmapimod hydrochloride purchased from MCE. Usage Cited in: Cancer Lett. 2017 Feb 16;393:22-32.  [Abstract]

    Effects of p38 MAPK inhibitor (SB203580), ERK inhibitor (U0126), JNK inhibitor (SP600125), caspase inhibitor (Z-VAD-FMK) and NAC on SGC-7901 and MGC-803 treated with DOX/VCPA combination treatment. VCPA pretreatment strategy is the same as above. SB203580 (20 μM), U0126 (10 μM), SP600125 (20 μM), Z-VAD-FMK (10 μM) and NAC (5 mM) are treated 2 h before DOX (2 μg/mL) added into the culture, respectively. MAPK pathway protein levels are determined.

    Adezmapimod hydrochloride purchased from MCE. Usage Cited in: Free Radic Biol Med. 2017 Nov;112:49-59.  [Abstract]

    Cells are pre-treated with ERK (U1026) and p38 (SB203580) inhibitors, followed by GL-V9 treatment for 24 h. Western blot is performed to analyze NAG-1 expression.

    Adezmapimod hydrochloride purchased from MCE. Usage Cited in: Hum Mol Genet. 2017 Sep 15;26(18):3553-3563.  [Abstract]

    Immunofluorescence analysis for expression of the I-cell marker ΔNP63 on proximal sections of ureters explanted from E12.5 wildtype (control) embryos and cultured for 6 d in the presence of solvent (DMSO) (A), the AKT inhibitor (AKT-i) MK2206 (B), the P38 inhibitor (P38-i) SB203580 (C), the ERK1/2 inhibitor (ERK1/2-i) PD98059 (D) or combinations as indicated (E and F).

    Adezmapimod hydrochloride purchased from MCE. Usage Cited in: Biochem Cell Biol. 2017 Feb;95(1):64-68.  [Abstract]

    The involvement of the p38 MAPK signaling pathways in lactoferrin-induced differentiation of HaCaT keratinocytes. HaCaT cells are differentiated in the presence or absence of 10 μM bovine Lactoferrin for 5 days. PD98059 (40 μM), SB203580 (10 μM), or LY294002 (10 μM) are added at the same time. Cell differentiation is evaluated by the expression levels of Involucrin and Filaggrin. GAPDH is used as a loading control.

    Adezmapimod hydrochloride purchased from MCE. Usage Cited in: Biomed Res. 2017; 28 (8): 3383-3386

    Effects of various protease inhibitors on HO-1 and P-gp protein expressions.

    Adezmapimod hydrochloride purchased from MCE. Usage Cited in: Int J Clin Exp Med. 2017;10(9):13542-13549.

    SB203580 decreases the expression ratio of p-p38 and p38 to inhibit activation of p38 MARK pathway.

    Adezmapimod hydrochloride purchased from MCE. Usage Cited in: China Biotechnology. 2017, 37(12): 40-48.

    The Western blot analysis of HOG1 and Phospho-HOG1.

    Adezmapimod hydrochloride purchased from MCE. Usage Cited in: Oncotarget. 2017 Oct 19;8(60):101965-101983.  [Abstract]

    Representative western blot analysis of P-gp, p38 MAPK and phospho-p38 MAPK expression in MCF-7/MDR and K562/MDR cells treated with 10 μM SB203580 for 48 hr.

    Adezmapimod hydrochloride purchased from MCE. Usage Cited in: Oxid Med Cell Longev. 2017;2017:6175841.  [Abstract]

    Involvements of MAPK signaling pathway in CPS-induced apoptosis in ALI cultures of sheep bronchial epithelial cells. Cells are pretreated with SB203580 (a P38 inhibitor, 20 μM) for 1 h, followed by exposure to CPS (100 ng/mL) or MO (MOI = 30) for 48 h. Cell lysates are subjected to Western blotting analysis using indicated antibodies.

    Adezmapimod hydrochloride purchased from MCE. Usage Cited in: Chin Arch Otolaryngol Head Neck Surg. 2016,23(01):49-52.

    Effect of p38MAPK inhibitor on the soft palate reconstruction of the rats with chronic intermittent hypoxia.

    Adezmapimod hydrochloride purchased from MCE. Usage Cited in: J Mol Cell Cardiol. 2015 Dec;89(Pt B):268-79.  [Abstract]

    Dose response of MAPK and Akt inhibitors on cardiac fibroblast-derived exosomes (Exo)-induced activation of MAPKs and Akt. Neonatal rat cardiomyocytes are treated with or without Exo (50 μg/mL), U0126, SP600125, MK-2206, and SB023580 for 20 min and subjected to Western blot analysis. The results are from 4 separate experiments.

    查看 p38 MAPK 亚型特异性产品:

    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Adezmapimod (SB 203580) hydrochloride 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 hydrochloride inhibits LCK, GSK3β and PKBα with IC50s of 100-500-fold higher than that for SAPK2a/p38. Adezmapimod hydrochloride 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 hydrochloride (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) 可防止 IL-2 诱导的原代人 T 细胞、鼠 CT6 T 细胞或 BAF 增殖 F7 B 细胞的 IC50 为 3-5 μM[1]
    Adezmapimod hydrochloride 阻断 PKB 磷酸化 (IC50 3-5 μM)。Adezmapimod hydrochloride 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[1]

    MCE 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 hydrochloride (5 mg/kg/day; 连续16天每天腹膜内注射; 雌性无胸腺 Nu/Nu 小鼠) 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[1]

    MCE 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

    413.90

    Formula

    C21H17ClFN3OS

    CAS 号
    性状

    固体

    颜色

    Light yellow to yellow

    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, 1 years; -20°C, 6 months (sealed storage, away from moisture)

    溶解性数据
    In Vitro: 

    DMSO 中的溶解度 : 100 mg/mL (241.60 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

    H2O 中的溶解度 : 5 mg/mL (12.08 mM; 超声助溶)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 2.4160 mL 12.0802 mL 24.1604 mL
    5 mM 0.4832 mL 2.4160 mL 4.8321 mL
    查看完整储备液配制表

    * 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, 1 years; -20°C, 6 months (sealed storage, away from moisture)。-80°C储存时,请在1年内使用, -20°C储存时,请在6个月内使用。

    * 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

    • 摩尔计算器

    • 稀释计算器

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    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

    • 方案 一

      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); 澄清溶液

      此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

      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;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

      生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
    • 方案 二

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

      Solubility: ≥ 2.5 mg/mL (6.04 mM); 澄清溶液

      此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

      1 mL 工作液为例,取 100 μL 25.0 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。

      20% SBE-β-CD in Saline 的配制(4°C,储存一周):2 g SBE-β-CD(磺丁基醚 β-环糊精)粉末定容于 10 mL 的生理盐水中,完全溶解至澄清透明。
    动物溶解方案计算器
    请输入动物实验的基本信息:

    给药剂量

    mg/kg

    动物的平均体重

    g

    每只动物的给药体积

    μL

    动物数量

    由于实验过程有损耗,建议您多配一只动物的量
    请输入您的动物体内配方组成:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
    方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
    计算结果
    工作液所需浓度 : mg/mL
    储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。

    *In solvent : -80°C, 1 years; -20°C, 6 months (sealed storage, away from moisture)

    您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
    动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
    连续给药周期超过半月以上,请谨慎选择该方案。
    请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
    纯度 & 产品资料

    纯度: 99.71%

    参考文献

    完整储备液配制表

    * 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, 1 years; -20°C, 6 months (sealed storage, away from moisture)。-80°C储存时,请在1年内使用, -20°C储存时,请在6个月内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    H2O / DMSO 1 mM 2.4160 mL 12.0802 mL 24.1604 mL 60.4011 mL
    5 mM 0.4832 mL 2.4160 mL 4.8321 mL 12.0802 mL
    10 mM 0.2416 mL 1.2080 mL 2.4160 mL 6.0401 mL
    DMSO 15 mM 0.1611 mL 0.8053 mL 1.6107 mL 4.0267 mL
    20 mM 0.1208 mL 0.6040 mL 1.2080 mL 3.0201 mL
    25 mM 0.0966 mL 0.4832 mL 0.9664 mL 2.4160 mL
    30 mM 0.0805 mL 0.4027 mL 0.8053 mL 2.0134 mL
    40 mM 0.0604 mL 0.3020 mL 0.6040 mL 1.5100 mL
    50 mM 0.0483 mL 0.2416 mL 0.4832 mL 1.2080 mL
    60 mM 0.0403 mL 0.2013 mL 0.4027 mL 1.0067 mL
    80 mM 0.0302 mL 0.1510 mL 0.3020 mL 0.7550 mL
    100 mM 0.0242 mL 0.1208 mL 0.2416 mL 0.6040 mL

    * 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    产品名称:
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