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.
- Int J Mol Med 54.3 (2024)：73.PMID:38963051
- Am J Cancer Res 14.3 (2024)：1121.PMID:38590396
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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]: | |
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Cell lines |
BUMPT-306 |
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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 |
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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. |
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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]: | |
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Animal models |
Male C57BL/6 mice (8–10 weeks) |
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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. |
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Dosage form |
10 mg/kg |
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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. |
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| 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
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Dorsomorphin (10 μM) was purchased from Glpbio (California, USA).
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Related Biological Data
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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.
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