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PI3K/Akt/mTOR
AMPK inhibitor
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TGF-beta/Smad inhibitor
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Autophagy activator
Dorsomorphin
僅限科研使用
Dorsomorphin
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(jié)構(gòu)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
產(chǎn)品質(zhì)控
批次：
純度：
99.99%
99.99
Dorsomorphin相關產(chǎn)品
| 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 |
|---|---|---|
| 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 |
|---|---|---|---|---|---|
| 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) | |||||
生物活性
| 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(jié)構(gòu)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。 | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| 靶點 |
|
| 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(zhì)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(zhuǎn)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 | pAMPK / AMPK / pACC / ACC / pRaptor / HIF1α Id1 / Id2 / Id3 |
|
29531259 | |
| Immunofluorescence | p-AMPK / Sirt1 / p66Shc |
|
28728079 | |
| 體內(nèi)研究(In Vivo) | ||
| 體內(nèi)研究活性 | Dorsomorphin (10 mg/kg)降低成年小鼠體內(nèi)鐵調(diào)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] |
|
|---|---|---|
| 動物實驗 | Animal Models | 富含鐵的小鼠 |
| Dosages | ~10 mg/kg | |
| Administration | i.v. | |
化學信息&溶解度
| 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(nèi)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(nèi)配方計算器 | ||||
實驗計算
動物體內(nèi)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(nèi)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(jié)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(nèi)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(nèi)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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