GW788388
Based on 17 publication(s) in Google Scholar
GW788388 is a potent and selective inhibitor of ALK5 with IC50 of 18 nM, and also inhibits TGF-β type II receptor and activin type II receptor activities, without inhibiting BMP type II receptor.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.92%
- CAS 番号: 452342-67-5
- 分子式: C25H23N5O2
- 分子量:425.48
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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生物活性
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化学情報
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溶剤 & 溶解度
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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Kinase Inhibitor Library
HY-L009
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TGF-beta/Smad Compound Library
HY-L018
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Reprogramming Compound Library
HY-L039
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MedChemExpress（MCE）の使用を引用している文献 GW788388
More- Nat Commun. 2026 Feb 12;17(1):1214. [Abstract]
- J Agric Food Chem. 2024 Jun 12;72(23):13138-13153. [Abstract]
- J Agric Food Chem. 2023 Oct 18;71(41):15170-15185. [Abstract]
- Cell Prolif. 2021 Jan;54(1):e12933. [Abstract]
- Org Lett. 2020 Aug 7;22(15):5726-5730. [Abstract]
- Org Lett. 2017 Jan 6;19(1):286-289. [Abstract]
- Int J Mol Sci. 2022 Oct 13;23(20):12219. [Abstract]
- Nat Prod Bioprospect. 2021 Feb;11(1):51-62. [Abstract]
- Bioorg Chem. 2021 Sep:114:105067. [Abstract]
- Bioorg Chem. 2020 Nov;104:104258. [Abstract]
- Lab Invest. 2019 Jul;99(8):1173-1192. [Abstract]
- J Funct Foods. December 2021, 104758.
- Phytochemistry. 2023 Nov:215:113849. [Abstract]
- Hum Exp Toxicol. 2022 Jan-Dec:41:9603271221075555. [Abstract]
- Toxicon. 2022 Feb:207:13-20. [Abstract]
- Phytochem Lett. 2024 Dec.
- Patent. US20180263995A1.
Customer Validation & Images
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WB
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WB
生物活性
IC50: 18 nM (ALK5)
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
446 nM
Compound: 9o
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Inhibition of TGF-beta1 signaling in human HEK293 cells transfected with luciferase and FAST-2 gene expression vector A3-LUX after 16 hrs by luciferase reporter gene assay
Inhibition of TGF-beta1 signaling in human HEK293 cells transfected with luciferase and FAST-2 gene expression vector A3-LUX after 16 hrs by luciferase reporter gene assay
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[PMID: 21783359] |
| HEK293 | IC50 |
>1000 nM
Compound: 9o
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Inhibition of Activin A in human HEK293 cells transfected with luciferase and FAST-2 gene expression vector A3-LUX after 16 hrs by luciferase reporter gene assay
Inhibition of Activin A in human HEK293 cells transfected with luciferase and FAST-2 gene expression vector A3-LUX after 16 hrs by luciferase reporter gene assay
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[PMID: 21783359] |
| HepG2 | IC50 |
0.093 μM
Compound: 13d, GW-788388
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Inhibition of TGF beta-induced transcription of firefly luciferase reporter gene in HepG2 cells
Inhibition of TGF beta-induced transcription of firefly luciferase reporter gene in HepG2 cells
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[PMID: 16570917] |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 452342-67-5
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性状 Solid
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分子量 425.48
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分子式 C25H23N5O2
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Color Off-white to gray
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SMILES
O=C(C1=CC=C(C=C1)C2=NC=CC(C3=CNN=C3C4=NC=CC=C4)=C2)NC5CCOCC5
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (17)
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Journal Impact Factor
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Most Recent
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Nat Commun
Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]2026 Feb 12;17(1):1214. PMID: 41680175 -
J Agric Food Chem
Novel Sesquiterpenoids with Renoprotective Activities from the Fruits of Alpinae oxyphylla as Potent TGF-β1/Smads Phosphorylation Inhibitors. [Abstract]2024 Jun 12;72(23):13138-13153. PMID: 38814319 -
J Agric Food Chem
2023 Oct 18;71(41):15170-15185. PMID: 37811859 -
Cell Prolif
FGF9 promotes mouse spermatogonial stem cell proliferation mediated by p38 MAPK signalling. [Abstract]2021 Jan;54(1):e12933. PMID: 33107118 -
Org Lett
Isolation, Total Synthesis, and Absolute Configuration Determination of Renoprotective Dimeric N-Acetyldopamine-Adenine Hybrids from the Insect Aspongopus chinensis. [Abstract]2020 Aug 7;22(15):5726-5730. PMID: 32525688 -
Org Lett
2017 Jan 6;19(1):286-289. PMID: 28029263
GW788388 purchased from MedChemExpress. Usage Cited in: Org Lett. 2017 Jan 6;19(1):286-289. [Abstract]
Compounds 1−4 inhibit fibrogenic action of TGF-β1 in rat renal proximal tubular cells. Cell lysates after treatments as indicated are immunoblotted with antibodies against fibronecitn, collagen I, α-SMA, and α-tubulin. GW: GW788388.
GW788388 purchased from MedChemExpress. Usage Cited in: Org Lett. 2017 Jan 6;19(1):286-289. [Abstract]
Cell lysates after various treatments are immunoblotted with antibodies against phosphorylated Smad2, phosphorylated Smad3, total Smad2/3, and β-actin. GW: GW788388.
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Int J Mol Sci
Androgen-Responsive Oncogenic lncRNA RP11-1023L17.1 Enhances c-Myc Protein Stability in Prostate Cancer. [Abstract]2022 Oct 13;23(20):12219. PMID: 36293081 -
Nat Prod Bioprospect
Neolignans and Norlignans from Insect Medicine Polyphaga plancyi and Their Biological Activities. [Abstract]2021 Feb;11(1):51-62. PMID: 32876846 -
Bioorg Chem
Isolation and identification of belamcandaoids A-N from Belamcanda chinensis seeds and their inhibition on extracellular matrix in TGF-β1 induced kidney proximal tubular cells. [Abstract]2021 Sep:114:105067. PMID: 34120020 -
Bioorg Chem
2020 Nov;104:104258. PMID: 32956876 -
Lab Invest
Endotoxemia-induced endothelial fibrosis inhibition improves hypotension, tachycardia, multiple organ dysfunction syndrome, cytokine response, oxidative stress, and survival. [Abstract]2019 Jul;99(8):1173-1192. PMID: 30911151 -
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Phytochemistry
Unusual acetylated flavonol glucuronides, oxyphyllvonides A-H with renoprotective activities from the fruits of Alpinae oxyphylla. [Abstract]2023 Nov:215:113849. PMID: 37673290 -
Hum Exp Toxicol
T-2 toxin induces articular cartilage damage by increasing the expression of MMP-13 via the TGF-β receptor pathway. [Abstract]2022 Jan-Dec:41:9603271221075555. PMID: 35213812 -
Toxicon
Transforming growth factor-β receptors mediates matrix degradation and abnormal hypertrophy in T-2 toxin-induced hypertrophic chondrocytes. [Abstract]2022 Feb:207:13-20. PMID: 34995556 -
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溶剤 & 溶解度
DMSO : 25 mg/mL (58.76 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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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: ≥ 2.5 mg/mL (5.88 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (5.88 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
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.
プロトコル
One week postsurgery, sham-operated (N=6) and infarcted animals (N=10) are randomized to treatment with the ALK5 inhibitor GW788388 (GSK) at a dosage of 50 mg/kg/day by gavage, which has been shown to significantly attenuate collagen overexpression in a rodent model of dimethylnitrosamine-induced liver disease. Untreated rats, that is, sham-operated (N=9) and MI animals (N=15), are gavaged with vehicle (1% carboxymethyl cellulose solution). Four animals with < 25% infarct size as determined postmortem by histology are excluded from further analyses.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
純度とドキュメンテーション
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データシート (277 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Petersen M, et al. Oral administration of GW788388, an inhibitor of TGF-beta type I and II receptor kinases, decreases renal fibrosis. Kidney Int, 2008, 73(6), 705-715. [Content Brief]
[2]. Tan SM, et al. Targeted inhibition of activin receptor-like kinase 5 signaling attenuates cardiac dysfunction following myocardial infarction. Am J Physiol Heart Circ Physiol, 2010, 298(5), H1415-1425. [Content Brief]
[3]. Gellibert F, et al. Discovery of 4-{4-[3-(pyridin-2-yl)-1H-pyrazol-4-yl]pyridin-2-yl}-N-(tetrahydro-2H- pyran-4-yl)benzamide (GW788388): a potent, selective, and orally active transforming growth factor-beta type I receptor inhibitor. J Med Chem. 2006, 49 [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 | 2.3503 mL | 11.7514 mL | 23.5029 mL | 58.7572 mL |
| 5 mM | 0.4701 mL | 2.3503 mL | 4.7006 mL | 11.7514 mL | |
| 10 mM | 0.2350 mL | 1.1751 mL | 2.3503 mL | 5.8757 mL | |
| 15 mM | 0.1567 mL | 0.7834 mL | 1.5669 mL | 3.9171 mL | |
| 20 mM | 0.1175 mL | 0.5876 mL | 1.1751 mL | 2.9379 mL | |
| 25 mM | 0.0940 mL | 0.4701 mL | 0.9401 mL | 2.3503 mL | |
| 30 mM | 0.0783 mL | 0.3917 mL | 0.7834 mL | 1.9586 mL | |
| 40 mM | 0.0588 mL | 0.2938 mL | 0.5876 mL | 1.4689 mL | |
| 50 mM | 0.0470 mL | 0.2350 mL | 0.4701 mL | 1.1751 mL |
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