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Dorsomorphin 2HCl

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(xì)胞試驗(yàn)中Ki為109 nM，對(duì)一些結(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受體。Dorsomorphin 可誘導(dǎo)癌細(xì)胞系的自噬。

Dorsomorphin 2HCl Chemical Structure

Dorsomorphin 2HCl Chemical Structure

CAS: 1219168-18-9

規(guī)格 價(jià)格 庫存 購買數(shù)量
10mg 1218.36 現(xiàn)貨
50mg 3866.79 現(xiàn)貨
200mg 7770 現(xiàn)貨
1g 16134.3 現(xiàn)貨
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Dorsomorphin 2HCl相關(guān)產(chǎn)品

相關(guān)信號(hào)通路圖

AMPK Signaling Pathways

AMPK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
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(diǎn)擊查看更多細(xì)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(xì)胞試驗(yàn)中Ki為109 nM，對(duì)一些結(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受體。Dorsomorphin 可誘導(dǎo)癌細(xì)胞系的自噬。
靶點(diǎn)
ALK2 [3] ALK3 [3] ALK6 [3] AMPK [1]
(Cell-free assay)
109 nM(Ki)
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(huì)減弱肝細(xì)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(duì)AMPK活性的抑制幾乎完全抑制了HT-29細(xì)胞中的自體吞噬的蛋白質(zhì)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(dǎo)的SMAD1/5/8磷酸化作用，靶點(diǎn)基因轉(zhuǎn)錄和成骨分化。[3]
實(shí)驗(yàn)圖片 檢測方法 檢測指標(biāo) 實(shí)驗(yàn)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(nèi)研究(In Vivo)
體內(nèi)研究活性

在成年小鼠體內(nèi)，Dorsomorphin (10 毫克/千克)降低肝殺菌肽表達(dá)的基礎(chǔ)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(dòng)脈中VCAM-1 和 ICAM-1的表達(dá)。[4]
動(dòng)物實(shí)驗(yàn) Animal Models Iron-replete 小鼠
Dosages ~10 毫克/千克
Administration 靜脈注射

化學(xué)信息&溶解度

分子量 472.41 分子式

C24H25N5O.2HCl
CAS號(hào) 1219168-18-9 SDF Download Dorsomorphin 2HCl SDF
Smiles C1CCN(CC1)CCOC2=CC=C(C=C2)C3=CN4C(=C(C=N4)C5=CC=NC=C5)N=C3.Cl.Cl
儲(chǔ)存條件(自收到貨起)

體外溶解度
批次：

Water : 47 mg/mL (99.48 mM)

DMSO : Insoluble ( ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開封DMSO)

Ethanol : Insoluble

摩爾濃度計(jì)算器

體內(nèi)溶解度
批次：

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

質(zhì)量 濃度 體積 分子量

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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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 is this drug targeting in the AMPK complex?

回答：
According to the reference （see link below), Dorsomorphin(Compound C) should target the AMPK alpha subunit through ALCAR or metformin. http://www.ncbi.nlm.nih.gov/pubmed/20844250

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