SB 525334
Based on 19 publication(s) in Google Scholar
SB 525334 is a potent and selective transforming growth factor β1 receptor (ALK5) inhibitor with an IC50 of 14.3 nM.
For research use only. We do not sell to patients.
- Purity: 99.97%
- CAS No.: 356559-20-1
- Formula: C21H21N5
- Molecular Weight:343.42
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Immunology/Inflammation Compound Library
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Publications Citing Use of MedChemExpress (MCE) SB 525334
More- J Hepatol. 2024 Jul 30:S0168-8278(24)02423-1. [Abstract]
- Nat Commun. 2025 Sep 30;16(1):8710. [Abstract]
- Adv Sci (Weinh). 2024 Jul 9:e2402327. [Abstract]
- J Control Release. 2021 Aug 10:336:40-53. [Abstract]
- Genome Med. 2025 Aug 15;17(1):90. [Abstract]
- Cell Commun Signal. 2018 Dec 7;16(1):97. [Abstract]
- Biomed Pharmacother. 2023 Sep:165:115225. [Abstract]
- Mol Cancer Ther. 2024 Oct 1;23(10):1404-1417. [Abstract]
- Commun Biol. 2025 Dec 13. [Abstract]
- Glia. 2014 Feb;62(2):185-98. [Abstract]
- Biochim Biophys Acta Mol Cell Res. 2024 Jun 13:119788. [Abstract]
- Biochim Biophys Acta. 2017 Dec 18;1864(3):721-734. [Abstract]
- Mol Med Rep. 2022 Nov;26(5):330. [Abstract]
- Mol Carcinog. 2025 Dec 15. [Abstract]
- Int J Hyperthermia. 2024;41(1):2359496. [Abstract]
- Ann Hematol. 2025 Feb;104(2):1165-1176. [Abstract]
- Parasitology. 2021 Jun;148(7):767-778. [Abstract]
- Biochem Biophys Res Commun. 2022 Dec 25;636(Pt 1):64-74. [Abstract]
- bioRxiv. 2026 May 21.
Customer Validation & Images
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IHC
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WB
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WB
Biological Activity
IC50: 14.3 nM (ALK5)[1]
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Cell Line
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Type | Value | Description | References |
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| Sf9 | IC50 |
0.162 μM
Compound: 3, SB-525334
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Inhibition of human recombinant GST-fused ALK5 expressed in Sf9 cells
Inhibition of human recombinant GST-fused ALK5 expressed in Sf9 cells
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[PMID: 20472445] |
SB525334 (1 μM; for 15 minutes before stimulating with 0.625 ng/ml of TGF-β1, assesses after 6 days) inhibits TGF-β1-mediated proliferation of familial idiopathic pulmonary arterial hypertension (iPAH) pulmonary artery smooth muscle cells (PASMCs) at an IC50 of 295 nM [2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:PASMC cells
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Concentration:1 μM
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Incubation Time:Pre-incubated for 15 minutes (before stimulating with 0.625 ng/ml of TGF-β1), assessed after 6 days
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Result:Inhibited TGF-β1-mediated proliferation of familial iPAH PASMCs at an IC50 of 295 nM.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Adult male Sprague-Dawley rats (MCT rat model of pulmonary hypertension)[2]
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Dosage:3, 30 mg/kg
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Administration:Oral administration; daily from days 17 to 35
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Result:Reduced the proportion of fully muscularized vessels to 28% at 3 mg/kg and returned fully muscularized vessel distribution beyond that seen at day 17 and approaching the phenotype observed in saline-exposed controls at 30 mg/kg.
Chemical Information
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CAS No. 356559-20-1
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Appearance Solid
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Molecular Weight 343.42
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Formula C21H21N5
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Color Light yellow to yellow
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SMILES
CC(C)(C1=NC(C2=CC=CC(C)=N2)=C(C3=CC=C4N=CC=NC4=C3)N1)C
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (19)
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Journal Impact Factor
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Most Recent
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J Hepatol
Transposon-based oncogene integration in Abcb4(Mdr2)-/- mice recapitulates high susceptibility to cholangiocarcinoma in primary sclerosing cholangitis. [Abstract]2024 Jul 30:S0168-8278(24)02423-1. PMID: 39089631 -
Nat Commun
Aberrant intermediate alveolar epithelial cells promote pathogenic activation of lung fibroblasts in preclinical fibrosis models. [Abstract]2025 Sep 30;16(1):8710. PMID: 41027873 -
Adv Sci (Weinh)
Stabilization of TGF-β Receptor 1 by a Receptor-Associated Adaptor Dictates Feedback Activation of the TGF-β Signaling Pathway to Maintain Liver Cancer Stemness and Drug Resistance. [Abstract]2024 Jul 9:e2402327. PMID: 38981014 -
J Control Release
Simultaneous blockage of contextual TGF-β by cyto-pharmaceuticals to suppress breast cancer metastasis. [Abstract]2021 Aug 10:336:40-53. PMID: 34119557 -
Genome Med
Aging increases susceptibility to liver fibrosis through enhanced NAT10-mediated ac4C modification of TGFβ1 mRNA. [Abstract]2025 Aug 15;17(1):90. PMID: 40817062 -
Cell Commun Signal
HMGB1/autophagy pathway mediates the atrophic effect of TGF-β1 in denervated skeletal muscle. [Abstract]2018 Dec 7;16(1):97. PMID: 30526602
SB 525334 purchased from MedChemExpress. Usage Cited in: Cell Commun Signal. 2018 Dec 7;16(1):97. [Abstract]
Immunofluorescence staining of LC3B and MHC in gastrocnemius in different groups (TGF-β1, TGF-β1+SB525334, SB525334, TGF-β1+CQ, TGF-β1+si-HMGB1) and HMGB1 staining of gastrocnemius.
SB 525334 purchased from MedChemExpress. Usage Cited in: Cell Commun Signal. 2018 Dec 7;16(1):97. [Abstract]
Western blot analysis of LC3B, p62, HMGB1 and MHC protein expression in gastrocnemius muscles with the treatment of groups (TGF-β1, TGF-β1+SB525334, SB525334, TGF-β1+CQ, TGF-β1+si-HMGB1).
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Biomed Pharmacother
The CD73 is induced by TGF-β1 triggered by nutrient deprivation and highly expressed in dedifferentiated human melanoma. [Abstract]2023 Sep:165:115225. PMID: 37517292 -
Mol Cancer Ther
AKT Inhibition Sensitizes to Polo-Like Kinase 1 Inhibitor Onvansertib in Prostate Cancer. [Abstract]2024 Oct 1;23(10):1404-1417. PMID: 38894678 -
Commun Biol
P38α MAPK-induced senescence in cranial suture progenitor cells promotes craniosynostosis. [Abstract]2025 Dec 13. PMID: 41390905 -
Glia
Activated microglia in a rat stroke model express NG2 proteoglycan in peri-infarct tissue through the involvement of TGF-β1. [Abstract]2014 Feb;62(2):185-98. PMID: 24311432 -
Biochim Biophys Acta Mol Cell Res
2024 Jun 13:119788. PMID: 38879132 -
Biochim Biophys Acta
2017 Dec 18;1864(3):721-734. PMID: 29269050
SB 525334 purchased from MedChemExpress. Usage Cited in: Biochim Biophys Acta. 2017 Dec 18;1864(3):721-734. [Abstract]
Microglial cells are incubated with or without TGF-β1 (5 ng/mL) and/or SB525334 (10 μM) for 24 h, followed by incubation with or without LPS for 24 h and subsequent NO determination.
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Mol Med Rep
COL1A1 expression induced by overexpression of both a 15‑amino acid peptide from the fibrinogen domain of tenascin‑X and integrin α11 in LX‑2 cells. [Abstract]2022 Nov;26(5):330. PMID: 36069233 -
Mol Carcinog
CCT6A Promotes Colon Cancer Cell Proliferation, Migration, and Invasion by Modulating Fatty Acid Metabolism and Activating the TGF-β1/Smad Signaling Pathway. [Abstract]2025 Dec 15. PMID: 41399140 -
Int J Hyperthermia
TGF-β1 inhibitor enhances the therapeutic effect of microwave ablation on hepatocellular carcinoma. [Abstract]2024;41(1):2359496. PMID: 38909985 -
Ann Hematol
TGFBI regulates the TGF-β pathway to affect the malignant progression and cisplatin sensitivity in diffuse large B-cell lymphoma. [Abstract]2025 Feb;104(2):1165-1176. PMID: 39856252 -
Parasitology
A combination of pirfenidone and TGF-β inhibition mitigates cystic echinococcosis-associated hepatic injury. [Abstract]2021 Jun;148(7):767-778. PMID: 33583470 -
Biochem Biophys Res Commun
2022 Dec 25;636(Pt 1):64-74. PMID: 36332484 -
Solvent & Solubility
DMSO : 50 mg/mL (145.59 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)
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 (7.28 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 (7.28 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.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: 20% SBE-β-CD in Saline adjusted to pH 3.5 with HCl
Solubility: 3 mg/mL (8.74 mM); Clear solution; Need ultrasonic and warming and heat to 60°C
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.
Purity & Documentation
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Data Sheet (282 KB)
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SDS (480 KB)
- English - EN (480 KB)
- Français - FR (480 KB)
- Deutsch - DE (480 KB)
- Norwegian - NO (480 KB)
- Español - ES (480 KB)
- Swedish - SV (480 KB)
- Italian - IT (480 KB)
- Portuguese - PT (480 KB)
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Handling Instructions (2659 KB)
References
[1]. Grygielko ET, et al. Inhibition of gene markers of fibrosis with a novel inhibitor of transforming growth factor-beta type I receptor kinase in puromycin-induced nephritis. J Pharmacol Exp Ther, 2005, 313(3), 943-951. [Content Brief]
[2]. Thomas M, et al. ALK5 mediates abnormal proliferation of vascular smooth muscle cells from patients with familial pulmonary arterial hypertension and is involved in the progression of experimental pulmonary arterial hypertension induced by monocrotaline. Am J Pathol, 2009, 174(2), 380-389. [Content Brief]
[3]. Laping NJ, et al. Tumor-specific efficacy of transforming growth factor-beta RI inhibition in Eker rats. Clin Cancer Res, 2007, 13(10), 3087-3899. [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 | 2.9119 mL | 14.5594 mL | 29.1189 mL | 72.7972 mL |
| 5 mM | 0.5824 mL | 2.9119 mL | 5.8238 mL | 14.5594 mL | |
| 10 mM | 0.2912 mL | 1.4559 mL | 2.9119 mL | 7.2797 mL | |
| 15 mM | 0.1941 mL | 0.9706 mL | 1.9413 mL | 4.8531 mL | |
| 20 mM | 0.1456 mL | 0.7280 mL | 1.4559 mL | 3.6399 mL | |
| 25 mM | 0.1165 mL | 0.5824 mL | 1.1648 mL | 2.9119 mL | |
| 30 mM | 0.0971 mL | 0.4853 mL | 0.9706 mL | 2.4266 mL | |
| 40 mM | 0.0728 mL | 0.3640 mL | 0.7280 mL | 1.8199 mL | |
| 50 mM | 0.0582 mL | 0.2912 mL | 0.5824 mL | 1.4559 mL | |
| 60 mM | 0.0485 mL | 0.2427 mL | 0.4853 mL | 1.2133 mL | |
| 80 mM | 0.0364 mL | 0.1820 mL | 0.3640 mL | 0.9100 mL | |
| 100 mM | 0.0291 mL | 0.1456 mL | 0.2912 mL | 0.7280 mL |
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