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Dorsomorphin

产品编号 T1977 CAS 866405-64-3

别名: Compound C, BML-275

Dorsomorphin (BML-275) 是一种 AMPK 抑制剂 (Ki=109 nM)，具有选择性和 ATP 竞争性。Dorsomorphin 可以抑制 BMP I 型受体 ALK2、ALK3 和 ALK6。Dorsomorphin 可诱导自噬，具有抗肿瘤活性。

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Dorsomorphin Chemical Structure

Dorsomorphin, CAS 866405-64-3

规格	价格/CNY		货期	数量
5 mg	￥ 514		现货
10 mg	￥ 764		现货
50 mg	￥ 2,866		现货
100 mg	￥ 3,260		现货
200 mg	￥ 4,760		现货

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其他形式的 Dorsomorphin:

Dorsomorphin dihydrochloride
现货

选择批次

纯度: 99.48%

纯度: 98.77%

纯度: 98.31%

纯度: 98%

纯度: 98%

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	Dorsomorphin (BML-275) is an AMPK inhibitor (Ki=109 nM) that is selective and ATP-competitive. Dorsomorphin inhibits the BMP type I receptors ALK2, ALK3, and ALK6. Dorsomorphin induces autophagy, and possesses antitumor activity.
靶点活性	AMPK:109 nM(Ki)
体外活性	方法：人肿瘤细胞 HeLa 和 HCT116 用 Dorsomorphin (1.25-80 μM) 处理 24 h，使用 CCK-8 方法检测细胞活力。结果：Dorsomorphin 抑制 HeLa 和 HCT116 细胞的活力，IC50 值分别为 10.71 μM 和 11.34 μM。[1] 方法：ATL 患者来源的 PBMCs 细胞用 Dorsomorphin (5-25 μM) 处理 24 h，使用 Flow Cytometry 检测细胞凋亡情况。结果：Dorsomorphin 以剂量依赖的方式增加了急性和慢性型 ATL 患者 PBMC 中早期凋亡细胞的频率。[2]
体内活性	方法：为检测体内抗肿瘤活性，将 Dorsomorphin (10 mg/kg) 腹腔注射给携带人类肿瘤 S1T 的 NOD/SCID 小鼠，每天一次，持续二十八天。结果：Dorsomorphin 抑制了 NOD/SCID 小鼠中人 ATL 肿瘤异种移植物的生长。[2] 方法：为检测体内对 SMAD 活性的影响，将 Dorsomorphin (10 mg/kg) 单次腹腔注射给 iron-dextran 处理的 C57BL/6 小鼠。结果：Dorsomorphin 消除了 iron-dextran 引起的铁介导的肝脏 SMAD1/5/8 磷酸化的增加。[3]
激酶实验	HT1080 cells are seeded in 24-well plates (2×104 cells per well) and treated with Dorsomorphin in the presence or absence of glucose or 10 mM 2DG for 2 h. HT1080 cells that overexpressed the wild-type and dominant negative AMPKα1 are prepared by transfecting plasmid DNA (pAMPKα1-wt, pAMPKα1-D168A and pcFlag as a control) in 6-well plates, seeding in 24-well plate and treating with UPR inhibitors. Cells are lysed with cell lysis buffer (20 mM Tris-HCl, pH 7.5, 250 mM NaCl, 10% glycerol, 0.5% NP-40, 1 mM EDTA, 1 mM EGTA, 0.2 mM PMSF, 1 μg/mL pepstatin, 0.5 μg/mL leupeptin, 5 mM NaF, 2 mM Na3Vo4, 2 mM β-glycerophosphate, 1 mM DTT). Relative AMPK kinase activity (mean±SD of duplicate determinations) to control sample (vehicle or pcFlag under normal growth conditions) is determined using the CycLex AMPK kinase assay kit[2].
细胞实验	Dorsomorphin is dissolved in DMSO (10 mM) and stored,and then diluted with appropriate media (DMSO 0.5%) before use[2].HeLa and 786-O cells are treated with various concentrations of Dorsomorphin (0,0.3,1,3,10 μM ),Versipelostatin and Phenformin in the presence or absence of 10 mM 2DG or 1 μg/mL of Tunicamycin as a stressor for 30 h in 96-well plates.For the combination study,786-O cells are treated with various concentrations of UPR inhibitors in the presence or absence of 10 mM 2DG for 24 h.The medium is then replaced with fresh growth medium,and cells are cultured for a further 15 h.Subsequently,MTT is added to the culture medium,and the absorbance of each well is determined.For the viability assay under glucose-withdrawal conditions,HT1080 cells are treated with various concentrations of Dorsomorphin and phenformin in 12-well plates in the presence or absence of glucose for 18 h,seeded in 96-well plates with growth medium,and then cultured for a further 48 h before MTT is added.Relative cell survival (mean±SD of quadruplicate determinations) is calculated by setting each control absorbance from untreated cells as 100%.The effects of drug combinations at concentrations producing 80% cell growth inhibition (IC80) are analyzed using the isobologram method[2].

别名	Compound C, BML-275
化合物与蛋白结合的复合物	Crystal structure of Maternal Embryonic Leucine Zipper Kinase (MELK) in complex with dorsomorphin (Compound C)
分子量	399.49
分子式	C24H25N5O
CAS No.	866405-64-3

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 1.33 mg/mL (3.34 mM), Sonication and heating are recommended.

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.5032 mL	12.516 mL	25.0319 mL	62.5798 mL

计算器

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参考文献

1. Li N, et al. Dorsomorphin induces cancer cell apoptosis and sensitizes cancer cells to HSP90 and proteasome inhibitors by reducing nuclear heat shock factor 1 levels. Cancer Biol Med. 2019 May;16(2):220-233. 2. Aikawa A, et al. Cell death induced by dorsomorphin in adult T-cell leukemia/lymphoma is AMPK-independent. FEBS J. 2020 Sep;287(18):4005-4015. 3. Yu PB, et al. Dorsomorphin inhibits BMP signals required for embryogenesis and iron metabolism. Nat Chem Biol. 2008 Jan;4(1):33-41. 4. Kim YM, et al. Atherosclerosis. 2011, 219(1), 57-64. 5. Ma L, Gong F, Xu J, et al. Uncarboxylated osteocalcin reverses the high glucose‑induced inhibition of the osteogenic differentiation of MC3T3E1 cells via the GPRC6A/cAMP/PKA/AMPK signaling pathway[J]. International Journal of Molecular Medicine. 2021, 47(5): 1-11 6. He Y, Xu K, Wang Y, et al. AMPK as a potential pharmacological target for alleviating LPS-induced acute lung injury partly via NLRC4 inflammasome pathway inhibition[J]. Experimental Gerontology. 2019: 110661. 7. Yang, Feihong, et al. Vaspin alleviates myocardial ischaemia/reperfusion injury via activating autophagic flux and restoring lysosomal function [J]. Biochemical and biophysical research communications. 2018 Sep 5;503(2):501-507. 8. Wang X D, Yu W L, Sun Y. Activation of AMPK restored impaired autophagy and inhibited inflammation reaction by up-regulating SIRT1 in acute pancreatitis[J]. Life Sciences. 2021: 119435. 9. Wu Y, Zeng S, Wan B, et al. Sophoricoside attenuates lipopolysaccharide-induced acute lung injury by activating the AMPK/Nrf2 signaling axis[J]. International Immunopharmacology. 2021, 90: 107187

文献引用

1. Wang X, Hu W, Qu L, et al.Tricin promoted ATG-7 dependent autophagic degradation of α-synuclein and dopamine release for improving cognitive and motor deficits in Parkinson's disease.Pharmacological Research.2023: 106874. 2. Sun X, Liu Z, Zhou L, et al.Escin avoids hemorrhagic transformation in ischemic stroke by protecting BBB through the AMPK/Cav-1/MMP-9 pathway.Phytomedicine.2023: 155071. 3. Yang W, Sun X, Liu S, et al.TLR8 agonist Motolimod-induced inflammatory death for treatment of acute myeloid leukemia.Biomedicine & Pharmacotherapy.2023, 163: 114759. 4. Ding S, Lin Z, Zhang X, et al.Deficiency of angiopoietin‐like 4 enhances CD8+ T cell bioactivity via metabolic reprogramming for impairing tumour progression.Immunology.2023 5. Zhou Y, Zhang Y, Cheng H, et al.Therapeutic Effects of Omentin-1 on Pulmonary Fibrosis by Attenuating Fibroblast Activation via AMP-Activated Protein Kinase Pathway.Biomedicines.2022, 10(11): 2715. 6. Xie Q, Sun Y, Xu H, et al.Ferrostatin-1 improves BMSC survival by inhibiting ferroptosis.Archives of Biochemistry and Biophysics.2023: 109535. 7. Rao X S, Cong X X, Gao X K, et al. AMPK-mediated phosphorylation enhances the auto-inhibition of TBC1D17 to promote Rab5-dependent glucose uptake. Cell Death & Differentiation. 2021: 1-21. 8. Ma L, Gong F, Xu J, et al. Uncarboxylated osteocalcin reverses the high glucose‑induced inhibition of the osteogenic differentiation of MC3T3E1 cells via the GPRC6A/cAMP/PKA/AMPK signaling pathway. International Journal of Molecular Medicine. 2021 May;47(5):91. doi: 10.3892/ijmm.2021.4924. Epub 2021 Mar 31. 9. Bai G, Chen B, Xiao X, et al. Geniposide inhibits cell proliferation and migration in human oral squamous carcinoma cells via AMPK and JNK signaling pathways. Experimental and Therapeutic Medicine. 2022, 24(6): 1-10. 10. Cao B, Zhang Y, Chen J, et al. Neuroprotective effects of liraglutide against inflammation through the AMPK/NF-κB pathway in a mouse model of Parkinson's disease. Metabolic Brain Disease. 2022, 37(2): 451-462

11. Qu L, Wu J, Tang Y, et al. Licochalcone B, a Natural Autophagic Agent for Alleviating Oxidative Stress-Induced Cell Death in Neuronal Cells and Caenorhabditis elegans Models. Pharmaceuticals. 2022, 15(9): 1052. 12. Wu Y, Wang Y, Gao Z, et al. Ethyl ferulate protects against lipopolysaccharide-induced acute lung injury by activating AMPK/Nrf2 signaling pathway. Acta Pharmacologica Sinica. 2021, 42(12): 2069-2081. 13. Wang X D, Yu W L, Sun Y. Activation of AMPK restored impaired autophagy and inhibited inflammation reaction by up-regulating SIRT1 in acute pancreatitis. Life Sciences. 2021 Jul 15;277:119435. doi: 10.1016/j.lfs.2021.119435. Epub 2021 Mar 26. 14. Gao, Le, et al. Uncarboxylated osteocalcin promotes osteogenesis and inhibits adipogenesis of mouse bone marrow‑derived mesenchymal stem cells via the PKA‑AMPK‑SIRT1 axis. Experimental and Therapeutic Medicine. 22.2 (2021): 1-13. 15. He Y, Xu K, Wang Y, et al. AMPK as a potential pharmacological target for alleviating LPS-induced acute lung injury partly via NLRC4 inflammasome pathway inhibition. Experimental Gerontology. 2019: 110661. 16. Su J W, Li S F, Tao J J, et al. Estrogen protects against acidosis-mediated articular chondrocyte injury by promoting ASIC1a protein degradation. European Journal of Pharmacology. 2021: 174381. 17. Wu Y X, Jiang F J, Liu G, et al. Dehydrocostus Lactone Attenuates Methicillin-Resistant Staphylococcus aureus-Induced Inflammation and Acute Lung Injury via Modulating Macrophage Polarization. International Journal of Molecular Sciences. 2021, 22(18): 9754. 18. Wu Y, Zeng S, Wan B, et al. Sophoricoside attenuates lipopolysaccharide-induced acute lung injury by activating the AMPK/Nrf2 signaling axis. International Immunopharmacology. 2021, 90: 107187 19. Cao B, Zhang Y, Chen J, et al. Neuroprotective effects of liraglutide against inflammation through the AMPK/NF-κB pathway in a mouse model of Parkinson’s disease. Metabolic Brain Disease. 2021: 1-12. 20. Yang F, Xue L, Han Z, et al. Vaspin alleviates myocardial ischaemia/reperfusion injury via activating autophagic flux and restoring lysosomal function. Biochemical and Biophysical Research Communications. 2018, 503(2): 501-507 21. Wu A G, Pan R, Law B Y K, et al. Targeting autophagy as a therapeutic strategy for identification of liganans from Peristrophe japonica in Parkinson’s disease. Signal transduction and targeted therapy. 2021, 6(1): 1-3. 22. Jiang M, Xiao Y, Weigao E, et al. Characterization of the Zebrafish Cell Landscape at Single-Cell Resolution. Frontiers in Cell and Developmental Biology. 2021, 9.

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剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

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第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

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计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Dorsomorphin 866405-64-3 Autophagy Chromatin/Epigenetic PI3K/Akt/mTOR signaling Stem Cells AMPK TGF-beta/Smad BML275 AMP-activated protein kinase inhibit ATP-competitive Inhibitor BMP Transforming growth factor beta receptors Compound C type receptors BML 275 TGF-β Receptor BML-275 inhibitor

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