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別名: BML-275,Compound C
Dorsomorphin是一種有效的,可逆選擇性 AMPK 抑制劑,無細胞試驗中 Ki 為 109 nM,對幾個結構相關的激酶,包括ZAPK,SYK,PKCθ,PKA,和 JAK3沒有顯著的抑制作用。 也會抑制 I型BMP receptors ALK2,ALK3和ALK6 的活性。Dorsomorphin被應用于促進特定細胞分化和誘導癌細胞自噬。如需進行細胞實驗,建議選擇可水溶產(chǎn)品 S7306 Dorsomorphin (Compound C) 2HCl。
Dorsomorphin Chemical Structure
CAS: 866405-64-3
相關產(chǎn)品 | Dorsomorphin 2HCl AICAR (Acadesine) A-769662 GSK621 WZ4003 ex229 (compound 991) Phenformin HCl HTH-01-015 BAY-3827 O-304 MK-3903 BAM 15 Danthron | 點擊展開 |
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相關化合物庫 | 激酶抑制劑庫 PI3K/Akt 抑制劑庫 凋亡分子化合物庫 細胞周期化合物庫 NF-κB信號通路庫 | 點擊展開 |
細胞系 | 實驗類型 | 給藥濃度 | 孵育時間 | 活性描述 | 文獻信息 |
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HepG2 | Function assay | 10 uM | 30 mins | Inhibition of BMPR1-mediated hepcidin mRNA expression in BMP2-stimulated human HepG2 cells at 10 uM treated 30 mins before BMP2 challenge measured after 16 hrs by qRT-PCR analysis | 18026094 |
Hep3B | Function assay | 10 uM | 30 mins | Inhibition of BMPR1-mediated hepcidin mRNA expression in IL6-stimulated human Hep3B cells at 10 uM treated 30 mins before IL6 challenge measured after 6 hrs by qRT-PCR analysis | 18026094 |
Hep3B | Function assay | 10 uM | 30 mins | Inhibition of BMPR1-mediated Id1 mRNA expression in IL6-stimulated human Hep3B cells at 10 uM treated 30 mins before IL6 challenge measured after 6 hrs by qRT-PCR analysis | 18026094 |
C2C12 | Function assay | 4 uM | Inhibition of BMPR1-mediated osteoblast differentiation in BMP4-stimulated mouse C2C12 cells assessed as decrease in alkaline phosphatase level at 4 uM by spectrophotometry | 18026094 | |
C2C12 | Function assay | 4 uM | Inhibition of BMPR1-mediated osteoblast differentiation in BMP6-stimulated mouse C2C12 cells assessed as decrease in alkaline phosphatase level at 4 uM by spectrophotometry | 18026094 | |
A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 29435139 | ||
DAOY | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 29435139 | ||
BT-37 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 29435139 | ||
RD | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 29435139 | ||
SK-N-SH | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 29435139 | ||
BT-12 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 29435139 | ||
MG 63 (6-TG R) | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 29435139 | ||
NB1643 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 29435139 | ||
OHS-50 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 29435139 | ||
Rh41 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells | 29435139 | ||
Rh30 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells | 29435139 | ||
SJ-GBM2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 29435139 | ||
SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 29435139 | ||
NB-EBc1 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 29435139 | ||
LAN-5 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 29435139 | ||
Rh18 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells | 29435139 | ||
點擊查看更多細胞系數(shù)據(jù) |
產(chǎn)品描述 | Dorsomorphin是一種有效的,可逆選擇性 AMPK 抑制劑,無細胞試驗中 Ki 為 109 nM,對幾個結構相關的激酶,包括ZAPK,SYK,PKCθ,PKA,和 JAK3沒有顯著的抑制作用。 也會抑制 I型BMP receptors ALK2,ALK3和ALK6 的活性。Dorsomorphin被應用于促進特定細胞分化和誘導癌細胞自噬。如需進行細胞實驗,建議選擇可水溶產(chǎn)品 S7306 Dorsomorphin (Compound C) 2HCl。 | ||||||||
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靶點 |
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體外研究(In Vitro) | ||||
體外研究活性 | 在肝細胞中,Dorsomorphin通過AICAR抑制ACC失活,并減弱AICAR增加脂肪酸氧化或抑制脂肪生成基因的作用。[1] HT-29細胞中,Dorsomorphin對AMPK活性的抑制幾乎完全抑制自噬蛋白質水解。[2] 此外,Dorsomorphin選擇性抑制BMP I型受體ALK2,ALK3和ALK6,從而阻斷BMP介導的SMAD1/5/8磷酸化,靶點基因轉錄和成骨分化。[3] |
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實驗圖片 | 檢測方法 | 檢測指標 | 實驗圖片 | PMID |
Western blot | pAMPK / AMPK / pACC / ACC / pRaptor / HIF1α Id1 / Id2 / Id3 | 29531259 | ||
Immunofluorescence | p-AMPK / Sirt1 / p66Shc | 28728079 |
體內研究(In Vivo) | ||
體內研究活性 | Dorsomorphin (10 mg/kg)降低成年小鼠體內鐵調素表達的基礎水平,并增加血清鐵的濃度。[3] Dorsomorphin (0.2 mg/kg, i.v.)顯著減少LPS處理的大鼠胸主動脈中VCAM-1和ICAM-1的表達。[4] |
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動物實驗 | Animal Models | 富含鐵的小鼠 |
Dosages | ~10 mg/kg | |
Administration | i.v. |
分子量 | 399.49 | 分子式 | C24H25N5O |
CAS號 | 866405-64-3 | SDF | Download Dorsomorphin SDF |
Smiles | C1CCN(CC1)CCOC2=CC=C(C=C2)C3=CN4C(=C(C=N4)C5=CC=NC=C5)N=C3 | ||
儲存條件(自收到貨起) | |||
體外溶解度 |
DMSO : 5 mg/mL ( (12.51 mM) Warmed with 50°C water bath; Ultrasonicated; ;DMSO吸濕會降低化合物溶解度,請使用新開封DMSO) Water : Insoluble Ethanol : Insoluble |
摩爾濃度計算器 |
體內溶解度 現(xiàn)配現(xiàn)用,請按從左到右的順序依次添加,澄清后再加入下一溶劑 |
動物體內配方計算器 |
動物體內配方計算器(澄清溶液)
第一步:請輸入基本實驗信息(考慮到實驗過程中的損耗,建議多配一只動物的藥量)
第二步:請輸入動物體內配方組成(配方適用于不溶于水的藥物;不同批次藥物配方比例不同,請聯(lián)系Selleck為您提供正確的澄清溶液配方)
計算結果:
工作液濃度: mg/ml;
DMSO母液配制方法: mg 藥物溶于μL DMSO溶液(母液濃度mg/mL,注:如該濃度超過該批次藥物DMSO溶解度,請先聯(lián)系Selleck);
體內配方配制方法:取μL DMSO母液,加入μL PEG300,混勻澄清后加入μL Tween 80,混勻澄清后加入μL ddH2O,混勻澄清。
體內配方配制方法:取μL DMSO母液,加入μL Corn oil,混勻澄清。
注意:1. 首先保證母液是澄清的;
2.一定要按照順序依次將溶劑加入,進行下一步操作之前必須保證上一步操作得到的是澄清的溶液,可采用渦旋、超聲或水浴加熱等物理方法助溶。
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