首页 工具
登录
购物车
Dorsomorphin

Dorsomorphin

产品编号 T1977   CAS 866405-64-3
别名: Compound C, BML-275

Dorsomorphin (Compound C) 是一种选择性,ATP 竞争性的AMPK 抑制剂,可诱导自噬。它选择性抑制 BMP I 型受体ALK2、ALK3和ALK6。

TargetMol的所有产品和服务仅用于科学研究,不能被用于人体,我们也不向个人提供产品和服务。
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
其他形式的 Dorsomorphin:
产品目录号及名称: Dorsomorphin (T1977)
点击图片重新获取验证码
选择批次  
纯度: 99.48%
纯度: 98.77%
纯度: 98.31%
纯度: 98%
纯度: 98%
更多批次查询请联系客服
生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 Dorsomorphin (Compound C) is an effective and specific inhibitor of AMPK (AMP-activated protein kinase), which is induced by AICAR and metformin.
靶点活性 AMPK:109 nM(Ki)
体外活性 Dorsomorphin inhibits ACC inactivation by either AICAR or metformin, and also attenuates AICAR and metformin's effect to increase fatty acid oxidation or suppress lipogenic genes in hepatocytes. [1] Inhibition of AMPK activity by Dorsomorphin almost completely inhibits autophagic proteolysis in HT-29 cells. [2] in addition, Dorsomorphin selectively inhibits the BMP type I receptors ALK2, ALK3 and ALK6, and thus blocks BMP-mediated SMAD1/5/8 phosphorylation, target gene transcription and osteogenic differentiation. [3]
体内活性 Dorsomorphin (10 mg/kg) reduces basal levels of hepcidin expression and increases serum iron concentrations in adult mice. [3] Dorsomorphin (0.2 mg/kg, i.v.) significantly reduces VCAM-1 and ICAM-1 expression in the thoracic aorta of LPS-treated rats. [4]
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

T1977_2

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), Sonification/heating is 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

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
=
X
X
X
=
X
=
/
g/mol

输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. Zhou G, et al. J Clin Invest. 2001, 108(8), 1167-1174. 2. Meley D, et al. J Biol Chem. 2006, 281(46), 34870-34879. 3. Yu PB, et al. Nat Chem Biol. 2008, 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.
收起
HADA Hydrochloride QX77 Imatinib BAY 11-7082 Loperamide hydrochloride LG-100064 STO-609 Pterostilbene

相关化合物库

该产品包含在如下化合物库中:
TGF-β/Smad靶点化合物库 人代谢物化合物库 糖酵解化合物库 自噬库 NO PAINS 化合物库 抗氧化化合物库 HIF-1化合物库 抗纤维化化合物库 细胞因子抑制剂库 氧化还原化合物库

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
mg/kg
每只动物体重
g
给药体积
μL
动物数量
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
%
% Tween 80
% ddH2O
计算 重置

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

 

陶术
生物
TargetMol®中国区唯一合作伙伴
点击进入陶术生物官网陶术生物
联系我们
400-820-0310

上海市静安区江场三路238号8楼