Dorsomorphin (Compound C) (Synonyms: Compound C) |
Catalog No.GC17243 |
Dorsomorphin (Compound C) is an agent that used as a cell-permeable AMPK inhibitor.
Products are for research use only. Not for human use. We do not sell to patients.
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.
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 | |
Synonyms | Compound C | ||
Chemical Name | 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 | ||
Formula | C24H25N5O | M.Wt | 399.49 |
Solubility | ≥ 8.49 mg/mL in DMSO with ultrasonic and warming | Storage | 4°C, protect from light |
General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. |
Prepare stock solution | |||
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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 |
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
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.
Nature Communications 13.1 (2022): 6108. PMID: 36245009 IF: 16.6009 -
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).
Cell Death & Disease 13.7 (2022): 622. PMID: 35851059 IF: 9.0002 -
Related Biological Data
Role of AMPK in the regulation of CTR1 expression by glucose restriction. (C) The AMPK inhibitor Compound C (40 μM) was used to verify the effect of AMPK on CTR1 expression for 24 h.
Compound C (AMPK inhibitor) was purchased from GlpBio (Shanghai,China).
Cancer Letters (2022): 215793. PMID: 35716782 IF: 8.6796 -
Related Biological Data
tPA regulates glycolysis through AMPK-Glut1 axis. (C) Protein expression of FN, p-AMPK, AMPK, Glut1, PCNA in the MRC-5 cells.
Dorsomorphin (Compound C, GC17243) were purchased from Glpbio Technology (Montclair, CA, USA).
Ecotox Environ Safe 271 (2024): 115994. PMID: 38262094 IF: 6.7996 -
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.
Int J Mol Sci 24.15 (2023): 12329. PMID: 37569705 IF: 5.5999 -
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);
Am J Cancer Res 14.3 (2024): 1121. PMID: 38590396 IF: 5.2999
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