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PI3K/Akt/mTOR
AMPK inhibitor
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TGF-beta/Smad inhibitor
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Autophagy activator
Dorsomorphin Dihydrochloride
僅限科研使用
Dorsomorphin Dihydrochloride
別名: BML-275 2HCl,Compound C 2HCl
Dorsomorphin 2HCl是一種有效的，可逆的，選擇性AMPK抑制劑，在無細胞試驗中Ki為109 nM，對一些結構相關的激酶，包括ZAPK， SYK， PKCθ，PKA和JAK3沒有顯著的抑制作用。也會抑制I型BMP受體。Dorsomorphin 可誘導癌細胞系的自噬。
Dorsomorphin Dihydrochloride Chemical Structure
CAS: 1219168-18-9
產(chǎn)品質控
批次：
純度：
99.98%
99.98
Dorsomorphin Dihydrochloride相關產(chǎn)品
| 相關產(chǎn)品 | Dorsomorphin AICAR (Acadesine) A-769662 GSK621 WZ4003 ex229 (compound 991) Phenformin HCl HTH-01-015 BAY-3827 Danthron MK-3903 BAM 15 O-304 | 點擊展開 |
|---|---|---|
| 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 |
相關信號通路圖
細胞實驗數(shù)據(jù)示例
| 細胞系 | 實驗類型 | 給藥濃度 | 孵育時間 | 活性描述 | 文獻信息(PMID) |
|---|---|---|---|---|---|
| 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 | ||
| KB-3-1 | qHTS assay | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 31515284 | ||
| 點擊查看更多細胞系數(shù)據(jù) | |||||
生物活性
| 產(chǎn)品描述 | Dorsomorphin 2HCl是一種有效的，可逆的，選擇性AMPK抑制劑，在無細胞試驗中Ki為109 nM，對一些結構相關的激酶，包括ZAPK， SYK， PKCθ，PKA和JAK3沒有顯著的抑制作用。也會抑制I型BMP受體。Dorsomorphin 可誘導癌細胞系的自噬。 | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| 靶點 |
|
| 體外研究(In Vitro) | ||||
| 體外研究活性 | Dorsomorphin抑制AICAR或者二甲雙胍引起的ACC失活，也會減弱肝細胞中AICAR和二甲雙胍增加脂肪酸氧化或抑制脂肪生成基因的作用。[1] Dorsomorphin對AMPK活性的抑制幾乎完全抑制了HT-29細胞中的自體吞噬的蛋白質水解作用。[2] 此外，Dorsomorphin選擇性抑制BMP I型受體ALK2，ALK3和ALK6，并因此阻斷BMP介導的SMAD1/5/8磷酸化作用，靶點基因轉錄和成骨分化。[3] |
|||
|---|---|---|---|---|
| 實驗圖片 | 檢測方法 | 檢測指標 | 實驗圖片 | PMID |
| Western blot | p-SMAD / SMAD Id1 / Id2 / Id3 pAMPK / AMPK / pACC / ACC / pRaptor / HIF1α p-ERK / ERK / Bcl2 / BAX / Cleaved caspase-3 LC3B I/ LC3B II |
|
30808965 | |
| Immunofluorescence | MyHC Id1 / MyoD |
|
20689554 | |
| Growth inhibition assay | Cell viability (MM cells) Cell viability (glioma cell lines) |
|
25010525 | |
| 體內研究(In Vivo) | ||
| 體內研究活性 | 在成年小鼠體內，Dorsomorphin (10 毫克/千克)降低肝殺菌肽表達的基礎水平，并增加血清中鐵離子濃度。[3] Dorsomorphin (0.2 毫克/千克，靜脈注射)顯著減少LPS 處理的大鼠胸主動脈中VCAM-1 和 ICAM-1的表達。[4] |
|
|---|---|---|
| 動物實驗 | Animal Models | Iron-replete 小鼠 |
| Dosages | ~10 毫克/千克 | |
| Administration | 靜脈注射 | |
|
化學信息&溶解度
| 分子量 | 472.41 | 分子式 | C24H25N5O.2HCl |
| CAS號 | 1219168-18-9 | SDF | Download Dorsomorphin Dihydrochloride SDF |
| Smiles | C1CCN(CC1)CCOC2=CC=C(C=C2)C3=CN4C(=C(C=N4)C5=CC=NC=C5)N=C3.Cl.Cl | ||
| 儲存條件(自收到貨起) | |||
|
體外溶解度 |
Water : 47 mg/mL (99.48 mM) DMSO : Insoluble ( ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO) Ethanol : Insoluble |
摩爾濃度計算器 |
|
體內溶解配方 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 | |||||
實驗計算
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）
mg/kg
g
μL
只
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）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
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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如果有其他問題，請給我們留言。
* 必填項
常見問題及建議解決方法
問題 1:
Is there any information you may provide as to WHICH AMPK SUBUNIT this compound is targeting in the AMPK complex?
回答：
According to the reference (see link below), it should target the AMPK alpha subunit through ALCAR or metformin. http://www.ncbi.nlm.nih.gov/pubmed/20844250
