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Dorsomorphin (Compound C)
僅限科研使用
Dorsomorphin (Compound C)
別名: BML-275,Compound C
Dorsomorphin是一種有效的，可逆選擇性 AMPK 抑制劑，無細(xì)胞試驗(yàn)中 Ki 為 109 nM，對(duì)幾個(gè)結(jié)構(gòu)相關(guān)的激酶，包括ZAPK，SYK，PKCθ，PKA，和 JAK3沒有顯著的抑制作用。 也會(huì)抑制 I型BMP receptors ALK2，ALK3和ALK6 的活性。Dorsomorphin被應(yīng)用于促進(jìn)特定細(xì)胞分化和誘導(dǎo)癌細(xì)胞自噬。如需進(jìn)行細(xì)胞實(shí)驗(yàn)，建議選擇可水溶產(chǎn)品 S7306 Dorsomorphin (Compound C) 2HCl。
Dorsomorphin (Compound C) Chemical Structure
CAS: 866405-64-3
產(chǎn)品質(zhì)控
批次：
純度：
99.99%
99.99
Dorsomorphin (Compound C)相關(guān)產(chǎn)品
| 相關(guān)產(chǎn)品 | Dorsomorphin Dihydrochloride AICAR (Acadesine) A-769662 GSK621 WZ4003 Phenformin HCl Ex229 (Compound 991) BAY-3827 HTH-01-015 O-304 Lixumistat (IM156) MK-8722 Danthron MK-3903 BAM 15 Phospho-AMPKα1 (Ser496) Antibody [K3H21] | 點(diǎn)擊展開 |
|---|---|---|
| 相關(guān)化合物庫(kù) | 激酶抑制劑庫(kù) PI3K/Akt 抑制劑庫(kù) 凋亡分子化合物庫(kù) 細(xì)胞周期化合物庫(kù) NF-κB信號(hào)通路庫(kù) | 點(diǎn)擊展開 |
相關(guān)信號(hào)通路圖
細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例
| 細(xì)胞系 | 實(shí)驗(yàn)類型 | 給藥濃度 | 孵育時(shí)間 | 活性描述 | 文獻(xiàn)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 | ||
| 點(diǎn)擊查看更多細(xì)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(xì)胞試驗(yàn)中 Ki 為 109 nM，對(duì)幾個(gè)結(jié)構(gòu)相關(guān)的激酶，包括ZAPK，SYK，PKCθ，PKA，和 JAK3沒有顯著的抑制作用。 也會(huì)抑制 I型BMP receptors ALK2，ALK3和ALK6 的活性。Dorsomorphin被應(yīng)用于促進(jìn)特定細(xì)胞分化和誘導(dǎo)癌細(xì)胞自噬。如需進(jìn)行細(xì)胞實(shí)驗(yàn)，建議選擇可水溶產(chǎn)品 S7306 Dorsomorphin (Compound C) 2HCl。 | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| 靶點(diǎn) |
|
| 體外研究(In Vitro) | ||||
| 體外研究活性 | 在肝細(xì)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。 HT-29細(xì)胞中，Dorsomorphin對(duì)AMPK活性的抑制幾乎完全抑制自噬蛋白質(zhì)水解。 此外，Dorsomorphin選擇性抑制BMP I型受體ALK2，ALK3和ALK6，從而阻斷BMP介導(dǎo)的SMAD1/5/8磷酸化，靶點(diǎn)基因轉(zhuǎn)錄和成骨分化。 |
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|---|---|---|---|---|
| 實(shí)驗(yàn)圖片 | 檢測(cè)方法 | 檢測(cè)指標(biāo) | 實(shí)驗(yàn)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(dá)的基礎(chǔ)水平，并增加血清鐵的濃度。 Dorsomorphin (0.2 mg/kg, i.v.)顯著減少LPS處理的大鼠胸主動(dòng)脈中VCAM-1和ICAM-1的表達(dá)。 |
|
|---|---|---|
| 動(dòng)物實(shí)驗(yàn) | Animal Models | 富含鐵的小鼠 |
| Dosages | ~10 mg/kg | |
| Administration | i.v. | |
|
化學(xué)信息&溶解度
| 分子量 | 399.49 | 分子式 | C24H25N5O |
| CAS號(hào) | 866405-64-3 | SDF | Download Dorsomorphin (Compound C) SDF |
| Smiles | C1CCN(CC1)CCOC2=CC=C(C=C2)C3=CN4C(=C(C=N4)C5=CC=NC=C5)N=C3 | ||
| 儲(chǔ)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(huì)降低化合物溶解度，請(qǐng)使用新開封DMSO) Water : Insoluble Ethanol : Insoluble |
摩爾濃度計(jì)算器 |
|
體內(nèi)溶解配方 現(xiàn)配現(xiàn)用，請(qǐng)按從左到右的順序依次添加，澄清后再加入下一溶劑 |
動(dòng)物體內(nèi)配方計(jì)算器 | |||||
實(shí)驗(yàn)計(jì)算
摩爾濃度計(jì)算器
動(dòng)物體內(nèi)配方計(jì)算器（澄清溶液）
第一步：請(qǐng)輸入基本實(shí)驗(yàn)信息（考慮到實(shí)驗(yàn)過程中的損耗，建議多配一只動(dòng)物的藥量）
mg/kg
g
μL
只
第二步：請(qǐng)輸入動(dòng)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(qǐng)聯(lián)系Selleck為您提供正確的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
計(jì)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(qǐng)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(jìn)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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