RepSox
Based on 23 publication(s) in Google Scholar
RepSox (E-616452) is a potent and selective transforming growth factor-beta receptor I/activin like kinase 5 (TGF-β-RI/ALK5) inhibitor. RepSox inhibits ALK5 autophosphorylation with an IC50 value of 4 nM. RepSox can be used for the research of obesity and associated metabolic diseases such as type 2 diabetes.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.92%
- No. CAS: 446859-33-2
- Fòrmula: C17H13N5
- Peso molecular:287.32
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) RepSox
More- Signal Transduct Target Ther. 2026 Jul 29;11(1):309.
- Mil Med Res. 2020 Nov 1;7(1):52. [Abstract]
- Mil Med Res. 2020 Sep 6;7(1):42. [Abstract]
- Adv Sci (Weinh). 2023 Jul;10(21):e2301309. [Abstract]
- Sci Adv. 2021 Apr 14;7(16):eabb2213. [Abstract]
- Biomaterials. 2019 Feb:193:30-46. [Abstract]
- Nano Today. 2025 Apr.
- Acta Pharmacol Sin. 2024 Nov;45(11):2290-2299. [Abstract]
- J Tissue Eng. 2023 Jul 8:14:20417314231185858. [Abstract]
- Stem Cell Res Ther. 2020 Apr 16;11(1):157. [Abstract]
- Cell Rep. 2023 Dec 5;42(12):113541. [Abstract]
- Cell Mol Neurobiol. 2026 Apr 24. [Abstract]
- J Biol Eng. 2024 Jan 16;18(1):7. [Abstract]
- Int J Mol Sci. 2023 Oct 31;24(21):15804. [Abstract]
- J Cell Mol Med. 2021 Apr;25(7):3498-3510. [Abstract]
- Biomedicines. 2022 Apr 18;10(4):928. [Abstract]
- Biomedicines. 2020 Nov 9;8(11):485. [Abstract]
- Genes (Basel). 2024 Sep 13;15(9):1206. [Abstract]
- Int J Stem Cells. 2023 May 30;16(2):156-167. [Abstract]
- Biomed Pharmacother. 2023 Mar:159:114216. [Abstract]
- Brain Science Advances. 2022 Feb.
- ACS Comb Sci. 2019 Dec 9;21(12):805-816. [Abstract]
- Oncotarget. 2017 Jun 19;8(36):60159-60172. [Abstract]
Customer Validation & Images
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In Vivo Efficacy Study
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In Vivo Efficacy Study
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In Vivo Efficacy Study
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Histological Imaging/Staining
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WB
Actividad biológica
Descripciòn
IC50 & Target
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ALK5 4 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| HepG2 | IC50 |
0.01 μM
Compound: 19
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Stimulation of Transforming growth factor beta receptor I kinase in HepG2 cells
Stimulation of Transforming growth factor beta receptor I kinase in HepG2 cells
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[PMID: 15317461] |
| K562 | IC50 |
>100 μM
Compound: ALK5 inhibitor II
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Cytotoxicity against human K562 cells assessed as decrease in cell proliferation after 72 hrs by calcein AM staining-based assay
Cytotoxicity against human K562 cells assessed as decrease in cell proliferation after 72 hrs by calcein AM staining-based assay
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[PMID: 28135685] |
| MCF7 | IC50 |
>100 μM
Compound: ALK5 inhibitor II
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Cytotoxicity against human MCF7 cells assessed as decrease in cell proliferation after 72 hrs by calcein AM staining-based assay
Cytotoxicity against human MCF7 cells assessed as decrease in cell proliferation after 72 hrs by calcein AM staining-based assay
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[PMID: 28135685] |
| Sf9 | IC50 |
0.004 μM
Compound: 19
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Inhibition of recombinant Activin A receptor type II-like kinase (ALK5) expressed in baculovirus/Sf9 cells
Inhibition of recombinant Activin A receptor type II-like kinase (ALK5) expressed in baculovirus/Sf9 cells
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[PMID: 15317461] |
In Vitro
RepSox (compound 19) inhibits ALK5 autophosphorylation with an IC50 value of 4 nM[1].
RepSox (0-10?μM; 0-8 days) induces adipogenesis from mouse embryonic fibroblasts (MEFs) in fibroblast culture medium[2].
RepSox (0-10?μM; 0-8 days) promotes the differentiation of the brown fat precursor cells and induce browning of the white fat precursor cells[2].
RepSox(0-10?μM; 0-8 days) induces brown adipogenesis in primary mouse fibroblasts and fat precursor cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Mouse embryonic fibroblasts (MEFs)
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Concentration:3 μM
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Incubation Time:0-8 days
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Result:Showed upregulation of UCP1 protein levels.
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Cell Line:MEFs
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Concentration:3 μM
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Incubation Time:0-8 days
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Result:Increased the number of mitochondria in MEF-derived adipocytes and significantly increased UCP1 levels.
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Cell Line:MEFs
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Concentration:3 μM
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Incubation Time:0-8 days
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Result:Induced the activation of a network of genes controlling adipogenesis, energy expenditure, and the thermogenic program in MEFs.
Chemical Information
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No. CAS 446859-33-2
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Appearance Solid
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Peso molecular 287.32
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Fòrmula C17H13N5
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Color Light brown to yellow
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SMILES
CC1=NC(C2=NNC=C2C3=NC4=CC=CN=C4C=C3)=CC=C1
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Synonyms
E-616452; SJN 2511
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (23)
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Journal Impact Factor
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Most Recent
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Mil Med Res
Direct conversion of human fibroblasts into dopaminergic neuron-like cells using small molecules and protein factors. [Abstract]2020 Nov 1;7(1):52. PMID: 33129359
RepSox purchased from MedChemExpress. Usage Cited in: Mil Med Res. 2020 Nov 1;7(1):52. [Abstract]
Chemical induction of human lung fetal IMR-90 fibroblasts into neuron-like cells. Representative microscopy images depicting the morphological changes after Repsox (2 μmol/L, 14 d) induction. Scale bars=100 μm.
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Mil Med Res
Efficient and rapid conversion of human astrocytes and ALS mouse model spinal cord astrocytes into motor neuron-like cells by defined small molecules. [Abstract]2020 Sep 6;7(1):42. PMID: 32892745 -
Adv Sci (Weinh)
2023 Jul;10(21):e2301309. PMID: 37119499 -
Sci Adv
Chemical conversion of human epidermal stem cells into intestinal goblet cells for modeling mucus-microbe interaction and therapy. [Abstract]2021 Apr 14;7(16):eabb2213. PMID: 33853767
RepSox purchased from MedChemExpress. Usage Cited in: Sci Adv. 2021 Apr 14;7(16):eabb2213. [Abstract]
Western blotting of the control hESC and the RCBB (including 5 μM Repsox, 6-8 d)-induced cells.
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Biomaterials
Chemical induced conversion of mouse fibroblasts and human adipose-derived stem cells into skeletal muscle-like cells. [Abstract]2019 Feb:193:30-46. PMID: 30554025
RepSox purchased from MedChemExpress. Usage Cited in: Biomaterials. 2019 Feb:193:30-46. [Abstract]
Generation of RepSox (10 μM, 6 d) induced skeletal muscle like cells (CiSMLC) from mouse embryonic fibroblasts (MEFs). Immunohistochemical detection of CiSMLC with various skeletal muscle markers: MHC (MF20) and MyoD (Upper panel), α-actinin and its overlap with phase contrast image (middle panel), and Myogenin and its overlap with phase contrast images (lower panel). Magnified images in the inset are used to depict the detailed localization and co-expression and of these markers. All scale bars: 100 μm.
RepSox purchased from MedChemExpress. Usage Cited in: Biomaterials. 2019 Feb:193:30-46. [Abstract]
Generation of RepSox (10 μM, 6 d) induced skeletal muscle like cells (CiSMLC) from mouse embryonic fibroblasts (MEFs). Semi-quantitative RT-PCR analysis of various skeletal specific markers.
RepSox purchased from MedChemExpress. Usage Cited in: Biomaterials. 2019 Feb:193:30-46. [Abstract]
Representative flow cytometry analysis of α-actinin positive cells upon 4-factor (including RepSox 10 μM) treatment for indicated times (6-15 d).
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Acta Pharmacol Sin
In situ reprogramming of cardiac fibroblasts into cardiomyocytes in mouse heart with chemicals. [Abstract]2024 Nov;45(11):2290-2299. PMID: 38890526
RepSox purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2024 Nov;45(11):2290-2299. [Abstract]
Schemes of generating Fsp1-Cre:R26R-loxp-tdTomato mice and drug treatment to induce in situ transdifferentiation. Fsp1-Cre mice were crossed with R26Rloxp-tdTomato mice in which the expression of tdTomato is prevented by a loxP-flanked STOP cassette. The F1 mice would have the red fluorescent protein tdTomato expressed specifically in the fibroblasts. CRFVPTM were given once a week for 6 weeks. Immunofluorescence staining of the cryosections of the hearts from Fsp1-Cre:R26R-loxp-tdTomato mice treated with vehicle (b) or CRFVPTM (c) for 6 weeks. C: CHIR99021, 14 mg/kg; R: RepSox, 8.6 mg/kg; F: Forskolin, 61.6 mg/kg; V: VPA, 250 mg/kg; T: TTNPB, 1 mg/kg and M: Rolipram, 2.5 mg/kg; P: Parnate, 2.7 mg/kg, CRFTM by oral gavage and VP by intraperitoneal injection once a week for 6 weeks in mice at about 8 weeks of age.
RepSox purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2024 Nov;45(11):2290-2299. [Abstract]
Whole-heart imaging with light-sheet fluorescence microscopy after tissue clearing of the hearts from Fsp1-Cre:R26R-loxp-tdTomato mice treated with vehicle (a) or CRFVPTM (b). (C: CHIR99021, 14 mg/kg; R: RepSox, 8.6 mg/kg; F: Forskolin, 61.6 mg/kg; V: VPA, 250 mg/kg; T: TTNPB, 1 mg/kg and M: Rolipram, 2.5 mg/kg; P: Parnate, 2.7 mg/kg, CRFTM by oral gavage and VP by intraperitoneal injection once a week for 6 weeks in mice at about 8 weeks of age).
RepSox purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2024 Nov;45(11):2290-2299. [Abstract]
a Schemes of obtaining PDGFRα-DreER:R26R-rox-tdTomato mice and drug treatment to induce in situ cardiac reprogramming in PDGFRα-DreER:R26R-roxtdTomato mice. PDGFRα-DreER mice were mated with R26R-rox-tdTomato mice in which the expression of tdTomato is prevented by a roxflanked STOP cassette. The expression of tdTomato in fibroblasts was turned on by tamoxifen treatment. CRFVPTM were given once a week for 6 weeks. b Body weigh change of the mice after chemical treatment. Immunofluorescence staining of the cryosections of the hearts from PDGFRα-DreER:R26R-rox-tdTomato mice treated with vehicle (c) or CRFVPTM (d) for 6 weeks. (C: CHIR99021, 14 mg/kg; R: RepSox, 8.6 mg/kg; F: Forskolin, 61.6 mg/kg; V: VPA, 250 mg/kg; T: TTNPB, 1 mg/kg and M: Rolipram, 2.5 mg/kg; P: Parnate, 2.7 mg/kg, CRFTM by oral gavage and VP by intraperitoneal injection once a week for 6 weeks in mice at about 8 weeks of age).
RepSox purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2024 Nov;45(11):2290-2299. [Abstract]
Immunofluorescence staining of α-actinin in cryosections of hearts from Fsp1-Cre:R26R-loxp-tdTomato mice treated with 7 C cocktail (CRFVPTM) or cocktails by removing 1 compound from 7 C (7C-X) for 6 weeks in vivo with Fsp1-Cre:R26R-loxp-tdTomato mice. (C: CHIR99021, 14 mg/kg; R: RepSox, 8.6 mg/kg; F: Forskolin, 61.6 mg/kg; V: VPA, 250 mg/kg; T: TTNPB, 1 mg/kg and M: Rolipram, 2.5 mg/kg; P: Parnate, 2.7 mg/kg, CRFTM by oral gavage and VP by intraperitoneal injection once a week for 6 weeks in mice at about 8 weeks of age).
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J Tissue Eng
Extracellular matrix-derived peptide stimulates the generation of endocrine progenitors and islet organoids from iPSCs. [Abstract]2023 Jul 8:14:20417314231185858. PMID: 37435573 -
Stem Cell Res Ther
Characterisation of extraembryonic endoderm-like cells from mouse embryonic fibroblasts induced using chemicals alone. [Abstract]2020 Apr 16;11(1):157. PMID: 32299508 -
Cell Rep
ASCL1 characterizes adrenergic neuroblastoma via its pioneer function and cooperation with core regulatory circuit factors. [Abstract]2023 Dec 5;42(12):113541. PMID: 38060444 -
Cell Mol Neurobiol
The Small Chemical Compound Repsox Potentiates Oct4-Driven Astrocyte-to-Neural Stem Cell Reprogramming via Notch1/Hes1/Smurf2 Pathway. [Abstract]2026 Apr 24. PMID: 42029832 -
J Biol Eng
Tissue engineering RPE sheet derived from hiPSC-RPE cell spheroids supplemented with Y-27632 and RepSox. [Abstract]2024 Jan 16;18(1):7. PMID: 38229139 -
Int J Mol Sci
2023 Oct 31;24(21):15804. PMID: 37958789 -
J Cell Mol Med
TGF-β isoforms inhibit hepatitis C virus propagation in transforming growth factor beta/SMAD protein signalling pathway dependent and independent manners. [Abstract]2021 Apr;25(7):3498-3510. PMID: 33682288 -
Biomedicines
Generation of a Pure Culture of Neuron-like Cells with a Glutamatergic Phenotype from Mouse Astrocytes. [Abstract]2022 Apr 18;10(4):928. PMID: 35453678 -
Biomedicines
Exosome-Mediated Differentiation of Mouse Embryonic Fibroblasts and Exocrine Cells into β-Like Cells and the Identification of Key miRNAs for Differentiation. [Abstract]2020 Nov 9;8(11):485. PMID: 33182285 -
Genes (Basel)
CHIR99021 and Brdu Are Critical in Chicken iPSC Reprogramming via Small-Molecule Screening. [Abstract]2024 Sep 13;15(9):1206. PMID: 39336797 -
Int J Stem Cells
Strategic Application of Epigenetic Regulators for Efficient Neuronal Reprogramming of Human Fibroblasts. [Abstract]2023 May 30;16(2):156-167. PMID: 36823979 -
Biomed Pharmacother
Mechanical stress protects against chondrocyte pyroptosis through TGF-β1-mediated activation of Smad2/3 and inhibition of the NF-κB signaling pathway in an osteoarthritis model. [Abstract]2023 Mar:159:114216. PMID: 36634591 -
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ACS Comb Sci
Benzimidazolyl-pyrazolo[3,4- b]pyridinones, Selective Inhibitors of MOLT-4 Leukemia Cell Growth and Sea Urchin Embryo Spiculogenesis: Target Quest. [Abstract]2019 Dec 9;21(12):805-816. PMID: 31689077 -
Oncotarget
Phorbol esters dPPA/dPA promote furin expression involving transcription factor CEBPβ in neuronal cells. [Abstract]2017 Jun 19;8(36):60159-60172. PMID: 28947961
RepSox purchased from MedChemExpress. Usage Cited in: Oncotarget. 2017 Jun 19;8(36):60159-60172. [Abstract]
SH-SY5Y (A) and HEK293 cells (B) are treated with 25 μM RepSox (Rep) in absence or presence of dPA or dPPA for 72 h, and the Western blotting results show that dPA or dPPA increases the expression in the presence of RepSox. RepSox does not cause significant alteration of furin protein compared to control. The expression of furin remains significantly increased after dPA or dPPA in the presence of RepSox.
Solvente y solubilidad
In Vitro:
DMSO : 33.33 mg/mL (116.00 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 7.5 mg/mL (26.10 mM); Clear solution
This protocol yields a clear solution of ≥ 7.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (75.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 7.5 mg/mL (26.10 mM); Clear solution
This protocol yields a clear solution of ≥ 7.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (75.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Add each solvent one by one: 1% DMSO 99% Saline
Solubility: ≥ 0.33 mg/mL (1.15 mM); Clear solution
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (282 KB)
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SDS (420 KB)
- English - EN (420 KB)
- Français - FR (420 KB)
- Deutsch - DE (420 KB)
- Norwegian - NO (420 KB)
- Español - ES (420 KB)
- Swedish - SV (420 KB)
- Italian - IT (420 KB)
- Korean - KR (420 KB)
- Portuguese - PT (420 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Gellibert F, et al. Identification of 1,5-naphthyridine derivatives as a novel series of potent and selective TGF-beta type I receptor inhibitors. J Med Chem. 2004 Aug 26;47(18):4494-506. [Content Brief]
[2]. Wan-Zhi Tu, et al. RepSox, a small molecule inhibitor of the TGFβ receptor, induces brown adipogenesis and browning of white adipocytes. Acta Pharmacol Sin. 2019 Dec;40(12):1523-1531. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.4804 mL | 17.4022 mL | 34.8044 mL | 87.0110 mL |
| 5 mM | 0.6961 mL | 3.4804 mL | 6.9609 mL | 17.4022 mL | |
| 10 mM | 0.3480 mL | 1.7402 mL | 3.4804 mL | 8.7011 mL | |
| 15 mM | 0.2320 mL | 1.1601 mL | 2.3203 mL | 5.8007 mL | |
| 20 mM | 0.1740 mL | 0.8701 mL | 1.7402 mL | 4.3505 mL | |
| 25 mM | 0.1392 mL | 0.6961 mL | 1.3922 mL | 3.4804 mL | |
| 30 mM | 0.1160 mL | 0.5801 mL | 1.1601 mL | 2.9004 mL | |
| 40 mM | 0.0870 mL | 0.4351 mL | 0.8701 mL | 2.1753 mL | |
| 50 mM | 0.0696 mL | 0.3480 mL | 0.6961 mL | 1.7402 mL | |
| 60 mM | 0.0580 mL | 0.2900 mL | 0.5801 mL | 1.4502 mL | |
| 80 mM | 0.0435 mL | 0.2175 mL | 0.4351 mL | 1.0876 mL | |
| 100 mM | 0.0348 mL | 0.1740 mL | 0.3480 mL | 0.8701 mL |
RepSox Related Classifications
HY-13012 Related Classifications
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