1. Stem Cell/Wnt Epigenetics PI3K/Akt/mTOR TGF-beta/Smad Autophagy
  2. Organoid AMPK TGF-β Receptor Autophagy
  3. Dorsomorphin

Dorsomorphin  (Synonyms: Compound C; BML-275)

目录号: HY-13418A 纯度: 99.91%
COA 产品使用指南

Dorsomorphin (Compound C) 是一种选择性,ATP 竞争性的 AMPK 抑制剂 (在没有 AMP 的情况下,Ki 为 109 nM)。Dorsomorphin 选择性抑制 BMP I 型受体 ALK2ALK3ALK6。Dorsomorphin 还能够逆转 Urolithin A (HY-100599) 导致的自噬 (autophagy) 激活和抗炎作用。

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Dorsomorphin Chemical Structure

Dorsomorphin Chemical Structure

CAS No. : 866405-64-3

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Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 436 篇科研文献

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IHC

    Dorsomorphin purchased from MCE. Usage Cited in: Life Sci. 2019 Jul 15;229:46-56.  [Abstract]

    Expression of APOE and COX5A in HUVECs treated with or without rhIL-17A (50 ng/mL) and Compound C (5 μM) is measured by western blot.

    Dorsomorphin purchased from MCE. Usage Cited in: Redox Biol. 2018 Jul;17:180-191.  [Abstract]

    MDA-MB-231 cells are cultured in poly-HEMA coated dishes and treated with Compound C or GL-V9 for 36 h. The expression of AMPK and p-AMPK in Compound C treated cells are assayed by Western blotting.

    Dorsomorphin purchased from MCE. Usage Cited in: Redox Biol. 2018 Oct;19:339-353.  [Abstract]

    Western blotting assay of AMPK, p-AMPK, PGC-1α, p-PGC-1α levels in nucleus pulposus (NP) cells stimulated with AGEs (200 μg/mL) in the presence or absence of A-769662 (50 μM), RAGE antibody (10 μg/mL), nicotinamide mononucleotide (NMN, 100 μM) or Compound C (50 uM).

    Dorsomorphin purchased from MCE. Usage Cited in: Biomed Pharmacother. 2018 Oct;106:1390-1395.  [Abstract]

    Effect of Compound C on the AMPK/Foxo1/miR-143-3p axis in Ang II-treated H9c2 cells.

    Dorsomorphin purchased from MCE. Usage Cited in: Biomed Pharmacother. 2018 Oct;106:1390-1395.  [Abstract]

    Effect of Compound C on cell viability, cell surface area, and apoptosis in Ang II-treated H9c2 cells.

    Dorsomorphin purchased from MCE. Usage Cited in: Biomed Pharmacother. 2018 Feb 19;100:417-425.  [Abstract]

    HaCaT cells are pre-incubated with Compound C (CC) (10 μM) and U0126 (10 μM), pharmacological inhibitors of AMPKα, ERK, respectively, for 1 h before treatment with DA8 and DA14 (DAs).

    Dorsomorphin purchased from MCE. Usage Cited in: Liver Int. 2018 Dec;38(12):2248-2259.  [Abstract]

    Cells are treated with 5 μM Dorsomorphin dihydrochloride (Compound C) for 3 hours to inhibit AMPK activity. Next, 2.5 μM CTD is applied for 24 hours. Cells are then collected for apoptosis assays and western blotting.

    Dorsomorphin purchased from MCE. Usage Cited in: J Agric Food Chem. 2018 Nov 7;66(44):11757-11766.  [Abstract]

    The number of GFP-LC3 dots are reduced significantly after inhibiting STAT3 (AG-490) signaling.

    Dorsomorphin purchased from MCE. Usage Cited in: J Agric Food Chem. 2018 Jul 5;66(26):6772-6781.  [Abstract]

    Effects of Compound C on capsiate-treated HepG2 cells in high fat environment. The expressions of key metabolic regulators and lipid metabolism-related proteins are quantified by densitometry, and the relative intensities are expressed in the bar chart.

    Dorsomorphin purchased from MCE. Usage Cited in: J Agric Food Chem. 2018 Jul 5;66(26):6772-6781.  [Abstract]

    Effects of Compound C on capsiate-treated HepG2 cells in high fat environment. The expressions of glucose metabolism-related proteins are quantified by densitometry, and the relative intensities are expressed in the bar chart.

    Dorsomorphin purchased from MCE. Usage Cited in: Front Pharmacol. 2018 Jul 16;9:761.  [Abstract]

    Epithelial cells from colon tissue are extracted from mice in each group (n=6-8 per group) and protein level of p-AMPK (Thr172) and AMPKα1/2 are measured by western blot.

    Dorsomorphin purchased from MCE. Usage Cited in: J Cell Physiol. 2018 May;233(5):3945-3954.  [Abstract]

    Fraxinellone-prompted phosphorylation of AMPK is blocked by Compound C (CC).

    Dorsomorphin purchased from MCE. Usage Cited in: Front Pharmacol. 2018 Feb 5;9:68.  [Abstract]

    CT26 cells are treated with CC for 4 h and detected phosphorylation levels of AMPK.

    Dorsomorphin purchased from MCE. Usage Cited in: J Cell Physiol. 2018 Dec;233(12):9701-9715.  [Abstract]

    HUVECs are pretreated with Compound C (5, 10, or 20 μM) for 18 hr or AICAR (1, 2, or 4 mM) for 1 hr, and then exposed to LSS for 30 min.

    Dorsomorphin purchased from MCE. Usage Cited in: Front Pharmacol. 2018 Aug 29;9:986.  [Abstract]

    AMPK and p38 phosphorylation is confirmed after Compound C (CC) and SB203580 treatment of Gomisin A (G.A)-treated CT26 cells.

    Dorsomorphin purchased from MCE. Usage Cited in: J Am Heart Assoc. 2018 Jun 12;7(12). pii: e008389.  [Abstract]

    Representative immunoblots of LC3 in Hippo and cortical brain tissue after CA/CPR. β-Actin serves as a loading control. J, Optical densities of LC3-II and LC3-I protein bands are quantitated. Cc indicates compound C.

    Dorsomorphin purchased from MCE. Usage Cited in: J Am Heart Assoc. 2018 Jun 12;7(12). pii: e008389.  [Abstract]

    Representative photomicrographs of immunohistochemistry for MAP2, Nissl, Iba-1, and GFAP in the hippocampal CA1 region of the sham-operated, sham-treated with Met (Met-a), and the experimental groups (Veh, Mettreated group, compound C [Cc]–treated group, Met+Cc-treated group, CQ–treated group, and Met+CQ-treated group) at 7 days after return of spontaneous circulation.

    Dorsomorphin purchased from MCE. Usage Cited in: Int J Mol Med. 2018 May;41(5):2535-2544.  [Abstract]

    Cells are treated with AICAR and AICAR (A++, 10 μM) + Compound C (C++, 1 μM) for 24 h, after which western blot analysis is performed.

    Dorsomorphin purchased from MCE. Usage Cited in: J Immunol Res. 2018 Dec 24;2018:9807139.  [Abstract]

    Western blot analysis of p-AMPK, AMPK, Bcl2 and Bax, LC3B and P62 expression in liver tissues.

    Dorsomorphin purchased from MCE. Usage Cited in: PLoS One. 2018 Aug 1;13(8):e0200897.  [Abstract]

    Phosphorylation of AMPK (Thr172) in HTOZ cells pretreated with Compound C at different concentrations (0-20 μM) for 1 hour prior to the presence of norUDCA at 200 μM for additional 1 hour is determined by western blotting analyses.

    Dorsomorphin purchased from MCE. Usage Cited in: Acta Biochim Biophys Sin (Shanghai). 2018 Feb 1;50(2):144-155.  [Abstract]

    Raw264.7 macrophages with serum deprivation are treated with 50 μM Rg1 for 48 h in absence or presence of compound C (10 mM) or AICAR (250 μM). Western blots of the protein expressions of Atg5, Beclin1, LC3, and p62/SQSMT1.

    Dorsomorphin purchased from MCE. Usage Cited in: Med Sci Monit. 2018 Jul 25;24:5168-5177.  [Abstract]

    The levels of p-S6K and S6K in 16HBE cells after treatment of BRL 49653/Troglitazone or/and Compound C are detected by western blot. The levels of p62 and LC3 in 16HBE cells after treatment of BRL 49653/Troglitazone or/and Compound C are detected by western blot.

    Dorsomorphin purchased from MCE. Usage Cited in: Biochem Biophys Res Commun. 2018 Sep 5;503(2):428-435.  [Abstract]

    Western blotting showing AMPK/m-TOR/ULK1 pathway relative protein (AMPK, p-AMPK, mTOR, p-mTOR, ULK1 and p-ULK1) levels in low glucose (LG), LG+Compound C (CC), HG and HG+CC groups.

    Dorsomorphin purchased from MCE. Usage Cited in: J Cardiovasc Pharmacol. 2018 Oct;72(4):167-175.  [Abstract]

    Foam cells are incubated with or without Compound C (10 μM) before the addition of CTRP9. According to the Western blot, the relative protein levels of p-AMPK, p-mTOR, LC3 II, and p62 are analyzed, respectively.

    Dorsomorphin purchased from MCE. Usage Cited in: Cell Physiol Biochem. 2018;50(5):1891-1902.  [Abstract]

    AMPK inhibitor dorsomorphin treatment reduces the protein expression of PGC-1α.

    Dorsomorphin purchased from MCE. Usage Cited in: Cell Physiol Biochem. 2018;48(1):227-236.  [Abstract]

    Inhibition of AMPK with Compound C (CC) attenuates the protective effects of FNDC5 on the oxLDL-induced AMPK dephosphorylation and fibrosis in LX-2 cells.

    Dorsomorphin purchased from MCE. Usage Cited in: Cell Death Dis. 2017 May 18;8(5):e2798.  [Abstract]

    Involvement of the AMPK/AKT/GSK3β pathway in Nrf2 nuclear translocation by Betulin. Cells are treated with 3 μM compound C (Comp.C) for 18 h before treatment with betulin (36 μM) for 6 h. Cell lysates are immunoblotted for the phosphorylation of AMPK, Akt, GSK3β and Nrf2.

    Dorsomorphin purchased from MCE. Usage Cited in: Mol Oncol. 2017 Aug;11(8):1035-1049.  [Abstract]

    Inhibition of AMPK reverses PD 0332991-induced autophagy and apoptosis. Hep3B cells are incubated with AMPK inhibitor (Compound C, 2.5 μM) for 4 h and then treated with PD 0332991 for 24 h. Apoptotic cells are determined by flow cytometry.

    Dorsomorphin purchased from MCE. Usage Cited in: Biochem Pharmacol. 2017 Aug 15;138:49-60.  [Abstract]

    Blockade of AMPK signals by AMPK α2 siRNA or AMPK inhibitor (Dorsomorphin; 2.5 μM, pretreatment 2 hours) treatment counteracts the apoptotic effects of Cantharidin at 2.5 μM. Data are representative of at least two independent experiments. Blocking AMPK signaling by knockdown of AMPK or Dorsomorphin (AMPK kinase inhibitor) treatment markedly reverses the apoptotic effect of Cantharidin, indicating that AMPK activation is required for the anti-HCC activity of Cantharidin.

    Dorsomorphin purchased from MCE. Usage Cited in: Am J Chin Med. 2017;45(6):1309-1325.  [Abstract]

    Activity of MMP-2 and MMP-9 in water extract (WAF)- and ethanol extract (EtAF)-treated CT26 cells after CC (20 μM) pretreatment for 4 h.

    Dorsomorphin purchased from MCE. Usage Cited in: Int J Mol Sci. 2017 May 19;18(5). pii: E1063.  [Abstract]

    Inhibition of sirt1 and AMPK blocked Rb2-induced hepatic autophagy. HepG2 cells are pretreated with 50 µM Rb2 for 4 h in the presence or absence of the sirt1 inhibitor EX-528 (EX) and the specific AMPK inhibitor Compound C (CC), and then subjected to OA (1 mM for HepG2 and 2 mM for primary mouse hepatocytes) exposure for 12 h. For lipid content determination, intracellular TG are stained by Oil red O (ORO). ORO is then eluted with isopropanol and the optical absorbance of the eluate is measured

    Dorsomorphin purchased from MCE. Usage Cited in: Free Radic Biol Med. 2016 Nov 9;101:401-412.  [Abstract]

    Effect of EsA on AMPK activation is necessary for AKT/GSK3β-mediated Nrf2 activity and cytoprotection. Cells are treated with 3 μM Compound C for 18 h, followed by treatment with EsA for 6 h, and then cell lysates are immunoblotted to assess the phosphorylation of AMPK, Akt and GSK3β and Nrf2.

    Dorsomorphin purchased from MCE. Usage Cited in: Biochem Pharmacol. 2016 Dec 15;122:42-61.  [Abstract]

    Inhibition of SREBPs processing by AHI is dependent on LKB-1/AMPK/mTOR pathway. (A) HepG2 cells are incubated with or without MHY1485 or Rapamycin for 1 h, the cells are switched to medium D in the presence of vehicle, or AHI. (B) HepG2 cells are incubated with or without Compound C for 1 h, the cells are switched to medium D in the presence of vehicle, or AHI.

    Dorsomorphin purchased from MCE. Usage Cited in: Oncotarget. 2016 Apr 5;7(14):18085-94.  [Abstract]

    MACC1 is up-regulated by ACh through p-AMPK. A. ACh stimulates AMPK phosphorylation via M3R. B. Inhibition of AMPK activity by Dorsomorphin (8 μM) suppresses the induction of MACC1 expression by ACh. p-AMPK levels increase after ACh stimulation, and pretreatment of UK-88525 attenuates the ACh-induced increase of p-AMPK.
    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Dorsomorphin (Compound C) is a selective and ATP-competitive AMPK inhibitor (Ki=109 nM in the absence of AMP). Dorsomorphin (BML-275) selectively inhibits BMP type I receptors ALK2, ALK3, and ALK6. Dorsomorphin can reverse autophagy activation and anti-inflammatory effect of Urolithin A (HY-100599)[1][2].

    IC50 & Target[1][2]

    AMPK

    109 nM (Ki)

    ACVR1

     

    BMPR1A

     

    ALK6

     

    Autophagy

     

    体外研究
    (In Vitro)

    Dorsomorphin (compound C) (0-10 μM,18 h) 以剂量依赖性方式抑制人纤维肉瘤 HT1080 细胞中 2DG 诱导的 GRP78 启动子活性,但对衣霉素诱导的 GRP78 启动子活性几乎没有影响。Dorsomorphin (compound C) C 还抑制葡萄糖戒断诱导的 GRP78 启动子活性。Dorsomorphin (化合物 C) 对 2DG 诱导的 PERK 激活没有影响,并降低 HT1080 细胞中基础和 2DG 诱导的 AMPK 磷酸化水平[2]

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Western Blot Analysis[2]

    Cell Line: Human fibrosarcoma HT1080 cells
    Concentration: 0-10 μM.
    Incubation Time: 18 hours.
    Result: Suppressed 2DG-induced GRP78 promoter activity in a dose-dependent manner and also suppressed GRP78 promoter activity induced by glucose withdrawal.
    体内研究
    (In Vivo)

    Dorsomorphin (化合物 C:10 mg/kg,静脉注射一次) 处理导致总血清铁浓度增加 60%,降低成年小鼠铁调素表达的基础水平并增加血清铁浓度[3]
    Dorsomorphin (化合物 C:0.2 mg/kg,静脉注射,LPS 注射前 30 分钟) 降低注射 LPS 的大鼠主动脉中的 ICAM-1 和 VCAM-1 表达[4]
    Dorsomorphin (化合物 C;25 mg/kg;腹腔注射;在雄性 BALB/c 小鼠中) 在注射脂多糖 (LPS) 之前进行处理,与仅接受 LPS 处理的动物相比,显著降低了致死率[5]

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Model: Wild-type (WT) C57BL/6 adult mice that are fed a standard iron-replete diet express high levels of hepcidin[3].
    Dosage: 10 mg/kg.
    Administration: Intravenously once.
    Result: Led to a 60% increase in total serum iron concentrations.
    Effective in reducing basal levels of hepcidin expression and increasing serum iron concentrations in adult mice.
    Animal Model: Male Sprague-Dawley rats, 8 weeks of age (body weight 230-250 g)[4].
    Dosage: 0.2 mg/kg.
    Administration: I.V., 30 min before LPS injection.
    Result: Reduced ICAM-1 and VCAM-1 expression in LPS-injected rat aorta.
    Animal Model: Male BALB/c mice at 6-7 weeks of age weighing 20-22 g[5]
    Dosage: 25 mg/kg
    Administration: Injection i.p.; 60 min before LPS challenge
    Result: Treatment of mice with 25 mg/kg before LPS injection significantly reduced lethality in contrast to animals treated with LPS challenge only.
    分子量

    399.49

    Formula

    C24H25N5O

    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, protect from light

    *In solvent : -80°C, 2 years; -20°C, 1 year (protect from light)

    溶解性数据
    In Vitro: 

    1M HCl 中的溶解度 : 50 mg/mL (125.16 mM; 超声助溶; 酸性条件溶解 (HCL 调节,pH≈1))

    DMSO 中的溶解度 : 33.33 mg/mL (83.43 mM; ultrasonic and adjust pH to 2 with 1M HCl; 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 : < 0.1 mg/mL (insoluble)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 2.5032 mL 12.5160 mL 25.0319 mL
    5 mM 0.5006 mL 2.5032 mL 5.0064 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, 2 years; -20°C, 1 year (protect from light)。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

    • 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:

    以下溶解方案,请直接配置工作液。建议现用现配,在短期内尽快用完。 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: 50% PEG300    50% Saline

      Solubility: 10 mg/mL (25.03 mM); 悬浊液; Need ultrasonic and warming and heat to 35°C

    • 方案 二

      请依序添加每种溶剂: 0.5% CMC/saline water

      Solubility: 10 mg/mL (25.03 mM); 悬浊液; 超声助溶

    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
    计算结果
    工作液所需浓度 : mg/mL
    纯度 & 产品资料

    纯度: 99.91%

    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, 2 years; -20°C, 1 year (protect from light)。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO / 1M HCl 1 mM 2.5032 mL 12.5160 mL 25.0319 mL 62.5798 mL
    5 mM 0.5006 mL 2.5032 mL 5.0064 mL 12.5160 mL
    10 mM 0.2503 mL 1.2516 mL 2.5032 mL 6.2580 mL
    15 mM 0.1669 mL 0.8344 mL 1.6688 mL 4.1720 mL
    20 mM 0.1252 mL 0.6258 mL 1.2516 mL 3.1290 mL
    25 mM 0.1001 mL 0.5006 mL 1.0013 mL 2.5032 mL
    30 mM 0.0834 mL 0.4172 mL 0.8344 mL 2.0860 mL
    40 mM 0.0626 mL 0.3129 mL 0.6258 mL 1.5645 mL
    50 mM 0.0501 mL 0.2503 mL 0.5006 mL 1.2516 mL
    60 mM 0.0417 mL 0.2086 mL 0.4172 mL 1.0430 mL
    80 mM 0.0313 mL 0.1564 mL 0.3129 mL 0.7822 mL
    1M HCl 100 mM 0.0250 mL 0.1252 mL 0.2503 mL 0.6258 mL
    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:
    Dorsomorphin
    目录号:
    HY-13418A
    需求量: