Dorsomorphin (Compound C)
(Synonyms: 6-[4-[2-(1-哌啶基)乙氧基]苯基]-3-(4-吡啶基)吡唑并[1,5-A]嘧啶,Compound C) 目录号 : GC17243
Dorsomorphin(Compound C)是一种细胞渗透的AMPK抑制剂。
Cas No.:866405-64-3
Sample solution is provided at 25 µL, 10mM.
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Dorsomorphin (Compound C) is an agent that used as a cell-permeable AMPK inhibitor. It could rescue the antiproliferative actions of AICAR and metformin. Moreover, dorsomorphin (Compound C) is also used as a selective inhibitor of the BMP pathway. Compound C could inhibit a number of kinases other than AMPK.[1]
In vitro experiments indicate that Compound C inhibits AMPK activity and proliferation of human glioma cells. Dorsomorphin (Compound C) also reduces the apoptosis of cells induced by cisplatin, and decreases the expression of c-caspase3 and c-PARP in cisplatin treatment.
In vivo study demonstrate compound C attenuates cisplatin-induced nephrotoxicity in mice, and alleviates c-caspase 3 and c-PARP induced by cisplatin in kidney tissues.[1][2]
References:
[1].Liu X, et al. The AMPK inhibitor compound C is a potent AMPK-independent antiglioma agent. Mol Cancer Ther. 2014 Mar;13(3):596-605.
[2].Li F, et al. Compound C Protects Against Cisplatin-Induced Nephrotoxicity Through Pleiotropic Effects. Front Physiol. 2020 Dec 23;11:614244.
Dorsomorphin(Compound C)是一种细胞渗透的AMPK抑制剂。它可以挽救AICAR和二甲双胍的抗增殖作用。此外,dorsomorphin(Compound C)还被用作BMP通路的选择性抑制剂。 Compound C除了能够抑制AMPK之外,还能够抑制其他多种激酶。 [1]
体外实验表明,复合物C抑制AMPK活性和人脑胶质瘤细胞的增殖。Dorsomorphin(复合物C)还减少了顺铂诱导的细胞凋亡,并降低了顺铂治疗中c-caspase3和c-PARP的表达。
动物实验表明,化合物C可以减轻小鼠因顺铂引起的肾毒性,并且缓解了顺铂在肾脏组织中引起的c-caspase 3和c-PARP。[1][2]
Cell experiment [1]: | |
Cell lines |
BUMPT-306 |
Preparation Method |
Cells were cultured in DMEM/F12 medium containing 10% fetal bovine serum and 10% streptomycin. Then, 20 μM cisplatin was used to induce obvious apoptosis as previously indicated |
Reaction Conditions |
Cells were cultured in 20 μM of cisplatin in the presence or absence of 20 mM compound C for 24 h. To evaluate the renal tubular cells apoptosis, morphologic assay and immunoblot were used to analyze the cleaved caspase3 and PARP. |
Applications |
Dorsomorphin (Compound C) could reduce the apoptosis of cells induced by cisplatin. Moreover, compound C also decreases the expression of c-caspase3 and c-PARP in cisplatin treatment, and the protective effect of compound C was dose-dependent. |
Animal experiment [1]: | |
Animal models |
Male C57BL/6 mice (8–10 weeks) |
Preparation Method |
Mice were injected intraperitoneally with cisplatin (30 mg/kg) oncely. The control group of mice were injected with the same dose of saline. Dorsomorphin (Compound C) was dissolved in DMSO and injected intraperitoneally at 10 mg/kg 1 h before the injection of cisplatin. The no-compound C animals were administered with a comparable volume of DMSO. All the mice were euthanized at 72 h. |
Dosage form |
10 mg/kg |
Applications |
Dorsomorphin (Compound C) could reduce the severe renal tubular damage caused by cisplatin in mice. Compound C also reduces the apoptosis of renal tubular cells in mice. |
References: [1]. Li F, et al. Compound C Protects Against Cisplatin-Induced Nephrotoxicity Through Pleiotropic Effects. Front Physiol. 2020 Dec 23;11:614244. |
Cas No. | 866405-64-3 | SDF | |
别名 | 6-[4-[2-(1-哌啶基)乙氧基]苯基]-3-(4-吡啶基)吡唑并[1,5-A]嘧啶,Compound C | ||
化学名 | 6-[4-(2-piperidin-1-ylethoxy)phenyl]-3-pyridin-4-ylpyrazolo[1,5-a]pyrimidine | ||
Canonical SMILES | C1CCN(CC1)CCOC2=CC=C(C=C2)C3=CN4C(=C(C=N4)C5=CC=NC=C5)N=C3 | ||
分子式 | C24H25N5O | 分子量 | 399.49 |
溶解度 | ≥ 8.49 mg/mL in DMSO with ultrasonic and warming | 储存条件 | 4°C, protect from light |
General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
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1 mg | 5 mg | 10 mg |
1 mM | 2.5032 mL | 12.516 mL | 25.0319 mL |
5 mM | 0.5006 mL | 2.5032 mL | 5.0064 mL |
10 mM | 0.2503 mL | 1.2516 mL | 2.5032 mL |
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 | 只 | |||
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GLPBIO为您提供正确的澄清溶液配方) | ||||||||||
% DMSO % % Tween 80 % saline | ||||||||||
计算重置 |
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,
体内配方配制方法:取 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 saline,混匀澄清。
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。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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Related Biological Data
ATF4 is required for glucose deprivation-induced fructolysis. a, b U87 and LN229 cells treated without or with glucose deprivation for 18 hours in the absence or presence of indicated inhibitors were analyzed by quantitative PCR (a) and immunoblotting with indicated antibodies (b).Data were normalized with β-actin mRNA levels and presented as relative mRNA expression level (a).
GCN2-IN-2 (A-92) (#GC32771-5) and Compound C (#GC17243) were obtained from GLPBIO.
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Related Biological Data
MSCs activated autophagy by regulating the AKT/mTOR and AMPK/mTOR signaling pathways to reduce the intracellular mutant protein ataxin-3. D The effect of LY303511 and dorsomorphin on the expression of levels of p-AKT, p-mTOR, ataxin-3, and autophagy-related proteins after MSCs therapy.
Dorsomorphin (10 μM) was purchased from Glpbio (California, USA).
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Related Biological Data
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Compound C (AMPK inhibitor) was purchased from GlpBio (Shanghai,China).
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Related Biological Data
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Dorsomorphin (Compound C, GC17243) were purchased from Glpbio Technology (Montclair, CA, USA).
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Related Biological Data
Selection and mechanism of the MTND therapy.(a) The cell morphology (bright field image) of tumor cells in its normal state (without any drug treatment); (b) tumor cell morphology (bright field image) under other drug combinations (Retinoic acid, Dorsomorphin, Purmorphamine,P7C3-A20);
The cells were cultured in DMEM/F12 containing MTND (10 μM Forskolin,1 μM Dorsomorphin(Glpbio), 1 μM Purmorphamine, 3 μM CHIR99021 and 3 μM P7C3-A20) or 0.1% DMSO in control groups.
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Related Biological Data
p53/AMPK/mTOR pathway was required for S100P-mediated autophagy regulating chemosensitivity. F. HL-60 and Jurkat cells were transfected with S100P shRNA or control shRNA and then pre-treated with Compound C (20 μM) for 6 h.
Compound C and lysosomal protease inhibitors E64d, pepstatin A were purchased from GlpBio (Montclair, CA, USA);
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