Dorsomorphin (Compound C) (Synonyms: Compound C) |
Catalog No.GC17243 |
Dorsomorphin (Compound C) est un agent utilisé comme inhibiteur de l'AMPK, perméable aux cellules.
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) est un agent utilisé comme inhibiteur de l'AMPK, perméable aux cellules. Il peut restaurer les actions antiprolifératives de l'AICAR et de la metformine. De plus, dorsomorphine (Compound C) est également utilisé comme inhibiteur sélectif de la voie BMP. Le composé C pourrait inhiber plusieurs kinases autres que l'AMPK.
Les expériences in vitro montrent que le composé C inhibe l'activité de l'AMPK et la prolifération des cellules de gliome humain. Dorsomorphine (Compound C) réduit également l'apoptose des cellules induite par le cisplatine, et diminue l'expression de c-caspase 3 et de c-PARP lors du traitement par cisplatine.
Les études in vivo démontrent que le composé C atténue la néphrotoxicité induite par le cisplatine chez les souris, et soulage les niveaux de c-caspase 3 et de c-PARP induits par le cisplatine dans les tissus rénaux.
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.
Expériences cellulaires [1]: | |
Lignées cellulaires | BUMPT-306 |
Méthode de préparation | Les cellules ont été cultivées dans un milieu DMEM/F12 contenant 10 % de sérum bovin fœtal et 10 % de streptomycine. Ensuite, 20 μM de cisplatine ont été utilisés pour induire une apoptose évidente comme indiqué précédemment. |
Conditions de réaction | Les cellules ont été cultivées dans 20 μM de cisplatine en présence ou en l'absence de 20 mM de composé C pendant 24 h. Pour évaluer l'apoptose des cellules tubulaires rénales, une analyse morphologique et un immunoblot ont été utilisés pour analyser la caspase 3 clivée et le PARP. |
Domaines d'application | Dorsomorphine (Compound C) pourrait réduire l'apoptose des cellules induite par le cisplatine. De plus, le composé C diminue également l'expression de c-caspase 3 et de c-PARP lors du traitement par cisplatine, et l'effet protecteur du composé C était dose-dépendant. |
Expériences animales [1]: | |
Modèles animaux | Souris mâles C57BL/6 (8–10 semaines) |
Méthode de préparation | Les souris ont reçu une injection intrapéritonéale de cisplatine (30 mg/kg) une seule fois. Le groupe témoin de souris a été injecté avec la même dose de saline. La dorsomorphine (Compound C) a été dissoute dans du DMSO et injectée intrapéritonéale à 10 mg/kg 1 h avant l'injection de cisplatine. Les animaux sans composé C ont reçu un volume comparable de DMSO. Toutes les souris ont été euthanasiées après 72 h. |
Forme de dosage | 10 mg/kg |
Domaines d'application | Dorsomorphine (Compound C) pourrait réduire les dommages rénaux tubulaires sévères causés par le cisplatine chez les souris. Le composé C réduit également l'apoptose des cellules tubulaires rénales chez les souris. |
Références : [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 | |
Synonymes | 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. |
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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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Note: 1. Please make sure the liquid is clear before adding the next solvent.
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3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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Related Biological Data
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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).
Cell Death & Disease 13.7 (2022): 622. PMID: 35851059 IF: 9.0002 -
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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.
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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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