Dorsomorphin 2HCl

别名: BML-275 2HCl,Compound C 2HCl

Dorsomorphin 2HCl是一种有效的,可逆的,选择性AMPK抑制剂,在无细胞试验中Ki为109 nM,对一些结构相关的激酶,包括ZAPK, SYK, PKCθ,PKA和JAK3没有显著的抑制作用。也会抑制I型BMP受体。Dorsomorphin 可诱导癌细胞系的自噬。

Dorsomorphin 2HCl Chemical Structure

Dorsomorphin 2HCl Chemical Structure

CAS: 1219168-18-9

规格 价格 库存 购买数量
10mg RMB 1218.36 现货
50mg RMB 3866.79 现货
200mg RMB 12203.1 现货
1g RMB 16134.3 现货
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客户使用Selleck的Dorsomorphin 2HCl发表文献469

产品质控

批次: 纯度: 99.98%
99.82

Dorsomorphin 2HCl相关产品

相关信号通路图

AMPK抑制剂选择性比较

细胞实验数据示例

细胞系 实验类型 给药浓度 孵育时间 活性描述 文献信息
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
点击查看更多细胞系数据

生物活性

产品描述 Dorsomorphin 2HCl是一种有效的,可逆的,选择性AMPK抑制剂,在无细胞试验中Ki为109 nM,对一些结构相关的激酶,包括ZAPK, SYK, PKCθ,PKA和JAK3没有显著的抑制作用。也会抑制I型BMP受体。Dorsomorphin 可诱导癌细胞系的自噬。
靶点
ALK2 [3] ALK3 [3] ALK6 [3] AMPK [1]
(Cell-free assay)
109 nM(Ki)
体外研究(In Vitro)
体外研究活性

Dorsomorphin抑制AICAR或者二甲双胍引起的ACC失活,也会减弱肝细胞中AICAR和二甲双胍增加脂肪酸氧化或抑制脂肪生成基因的作用。[1]

Dorsomorphin对AMPK活性的抑制几乎完全抑制了HT-29细胞中的自体吞噬的蛋白质水解作用。[2]

此外,Dorsomorphin选择性抑制BMP I型受体ALK2,ALK3和ALK6,并因此阻断BMP介导的SMAD1/5/8磷酸化作用,靶点基因转录和成骨分化。[3]

实验图片 检测方法 检测指标 实验图片 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
体内研究(In Vivo)
体内研究活性

在成年小鼠体内,Dorsomorphin (10 毫克/千克)降低肝杀菌肽表达的基础水平,并增加血清中铁离子浓度。[3]

Dorsomorphin (0.2 毫克/千克,静脉注射)显著减少LPS 处理的大鼠胸主动脉中VCAM-1 和 ICAM-1的表达。[4]

动物实验 Animal Models Iron-replete 小鼠
Dosages ~10 毫克/千克
Administration 静脉注射

化学信息&溶解度

分子量 472.41 分子式

C24H25N5O.2HCl

CAS号 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
储存条件(自收到货起)

体外溶解度
批次:

Water : 47 mg/mL

DMSO : Insoluble ( DMSO吸湿会降低化合物溶解度,请使用新开封DMSO)

Ethanol : Insoluble

摩尔浓度计算器

体内溶解度
批次:

现配现用,请按从左到右的顺序依次添加,澄清后再加入下一溶剂

动物体内配方计算器

实验计算

摩尔浓度计算器

质量 浓度 体积 分子量

动物体内配方计算器(澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)

mg/kg g μL

第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)

% DMSO % % Tween 80 % ddH2O
%DMSO %

计算结果:

工作液浓度: mg/ml;

DMSO母液配制方法: mg 药物溶于μL DMSO溶液(母液浓度mg/mL,:如该浓度超过该批次药物DMSO溶解度,请先联系Selleck);

体内配方配制方法:μL DMSO母液,加入μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入μL ddH2O,混匀澄清。

体内配方配制方法:μL DMSO母液,加入μL Corn oil,混匀澄清。

注意:1. 首先保证母液是澄清的;
2.一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。

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常见问题及建议解决方法

问题 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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