Dorsomorphin (Compound C) 2HCl

For research use only. Not for use in humans.

目录号:S7306 别名: BML-275 2HCl,Compound C 2HCl

Dorsomorphin (Compound C) 2HCl Chemical Structure

CAS No. 1219168-18-9

Dorsomorphin 2HCl (BML-275, Compound C) 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。

规格 价格 库存 购买数量  
RMB 1218.36 现货
RMB 3866.79 现货
有超大折扣

今日订购,明日送达,全国免运费!

全国免费电话:400-668-6834   |   Email:info@selleck.cn

客户使用Selleck生产的Dorsomorphin (Compound C) 2HCl发表文献290篇:

产品安全说明书

AMPK抑制剂选择性比较

生物活性

产品描述 Dorsomorphin 2HCl (BML-275, Compound C) 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

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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
mouse C2C12 cells M2q4cmZ2dmO2aX;uJIF{e2G7 MmXBOEDPxE1? MV;Jcohq[mm2aX;uJI9nKEKPUGKxMY1m\GmjdHXkJI9{fGWxYnzhd5Qh\GmoZnXy[Y51cWG2aX;uJIlvKEKPUEStd5RqdXWuYYTl[EBud3W|ZTDDNmMyOiClZXzsd{Bie3Onc4Pl[EBieyCmZXPy[YF{\SCrbjDhcItidGmwZTDwbI9{eGijdHHz[UBt\X[nbDDheEA1KHWPIHL5JJNx\WO2cn;wbI91d22ndIL5 MX[xPFAzPjB7NB?=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-SMAD / SMAD; 

PubMed: 30808965     


SMAD phosphorylation was assessed by Western blot after cells were treated with dorsomorphin (0 µM to 10 µM) from day 1 to day 3 or from day 3 to day 4.

Id1 / Id2 / Id3 ; 

PubMed: 25010525     


Dorsomorphin dramatically inhibited the expression of Ids. KMM cells were treated with 5 µM Dorsomorphin for 24 hours before harvesting. Expressions of Ids were detected by immunoblotting.

pAMPK / AMPK / pACC / ACC / pRaptor / HIF1α ; 

PubMed: 29531259     


PC-3 and LNCaP cells were treated with vehicle, 25 µM compound 8c, 25 µM compound 8c + 5 μM Dorsomorphin (8c + D) or 5 μM Dorsomorphin (D), for 1 hour or 24 hours and levels of the phosphorylated AMPK (pAMPK), phosphorylated ACC (pACC), phosphorylated Raptor (pRaptor) forms and HIF1α were determined by Western blot. Upper panel, representative Western blot of three different experiments. β-tubulin (β-Tub) serves as a loading control. Lower panel, densitometric analyses of bands represented as the mean of the ratio pAMPK/AMPK or pACC/ACC.

p-ERK / ERK / Bcl2 / BAX / Cleaved caspase-3; 

PubMed: 30155931     


Western blot analysis of the protein expression of ERK, p‐ERK, Bcl2, BAXand cleaved caspase‐3 in T98 cells stimulated by Compound C (0, 1, 5, 10 μmol/L) for 24 h.

LC3B I/ LC3B II; 

PubMed: 30155931     


The representative western blot analysis showed that stimulation by Compound C for 24 h decreased the ratio of LC3BI/IIin T98 cells in a dose-dependent manner. 

30808965 25010525 29531259 30155931
Immunofluorescence
MyHC; 

PubMed: 20689554     


Satellite cell-derived myoblasts were plated at high cell density (80–90% confluency) and cultured in proliferation medium for 2 days with or without Dorsomorphin. Immunostaining for MyHC showed that Dorsomorphin promoted myogenic differentiation and fusion in a dose-dependent manner. 

Id1 / MyoD ; 

PubMed: 20689554     


(a) Exposure to 3 μM Dorsomorphin for 6 h to inhibit BMP signalling resulted in a downregulation of Id1 expression in satellite cells associated with a myofibre. (b) Similarly, immunostaining of plated satellite cells after exposure to 3 μM Dorsomorphin for 18 h in proliferation medium also resulted in downregulation of Id1 protein. Scale bar equals 20 μm.

20689554
Growth inhibition assay
Cell viability (MM cells); 

PubMed: 25010525     


Dorsomorphin showed preferential toxicity to KMM (KSHV-transformed MM cells) cells. KMM cells or MM cells were seeded 4000 cells/well. 24 hours after seeding, medium was replaced with Dorsomorphin medium as indicated. Cell viability was measured by MTT assay 48 hours post Dorsomorphin treatment. Data were shown as mean ± s.e.m., n = 3. 

Cell viability (glioma cell lines); 

PubMed: 24419061     


Histogram showing the dose-dependent effect of Compound C (1, 2.5, 5 and 10μM) on the viability of three glioma cell lines. Numbers inside bars represent % dead cells.

25010525 24419061
体内研究 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]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

动物实验:[3]
- 合并
  • Animal Models: Iron-replete 小鼠
  • Dosages: ~10 毫克/千克
  • Administration: 静脉注射
    (Only for Reference)

溶解度 (25°C)

体外 Water 94 mg/mL (198.97 mM)
DMSO Insoluble
Ethanol Insoluble
体内 从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
PBS
15mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 472.41
化学式

C24H25N5O.2HCl

CAS号 1219168-18-9
储存条件 粉状
溶于溶剂
别名 BML-275 2HCl,Compound C 2HCl

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)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
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
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

技术支持

在订购、运输、储存和使用我们的产品的任何阶段,您遇到的任何问题,均可以通过拨打我们的热线电话400-668-6834,或者技术支持邮箱tech@selleck.cn,直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题,请给我们留言。

  • * 必填项

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

AMPK Signaling Pathway Map

相关AMPK产品

Tags: 购买Dorsomorphin (Compound C) 2HCl | Dorsomorphin (Compound C) 2HCl供应商 | 采购Dorsomorphin (Compound C) 2HCl | Dorsomorphin (Compound C) 2HCl价格 | Dorsomorphin (Compound C) 2HCl生产 | 订购Dorsomorphin (Compound C) 2HCl | Dorsomorphin (Compound C) 2HCl代理商
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID