Art. -Nr.: HY-12043

SB 525334

Name: SB 525334
Brand: MedChemExpress
SKU: HY-12043
Price: 65.00 USD
Availability: InStock
Rating: 5 (23 reviews)

23 Cited Publications

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Based on 23 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.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Reinheit : 99.97%
CAS. Nr.: 356559-20-1
Formel: C₂₁H₂₁N₅
Molecular Weight:343.42

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

SB 525334 Chemical Structure

CAS. Nr.: 356559-20-1

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (23)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll (1)
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

SB 525334 is a potent and selective transforming growth factor β1 receptor (ALK5) inhibitor with an IC₅₀ of 14.3 nM.

IC₅₀ & Target

IC50: 14.3 nM (ALK5)^[1]

Alle TGF-β Receptor Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
Sf9	IC₅₀	0.162 μM Compound: 3, SB-525334	Inhibition of human recombinant GST-fused ALK5 expressed in Sf9 cells Inhibition of human recombinant GST-fused ALK5 expressed in Sf9 cells	[PMID: 20472445]

In Vitro

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. Further protocols information, click here.

Cell Proliferation Assay^[2]

View Protocol

Cell Line:

PASMC cells
Concentration:

1 μM
Incubation Time:

Pre-incubated for 15 minutes (before stimulating with 0.625 ng/ml of TGF-β1), assessed after 6 days
Result:

Inhibited TGF-β1-mediated proliferation of familial iPAH PASMCs at an IC₅₀ of 295 nM.

In Vivo

SB525334 (3-30 mg/kg; p.o.; daily from days 17 to 35) significantly reverses pulmonary arterial pressure in a rat model of pulmonary arterial hypertension (PAH)^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Adult male Sprague-Dawley rats (MCT rat model of pulmonary hypertension)^[2]
Dosage:

3, 30 mg/kg
Administration:

Oral administration; daily from days 17 to 35
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

CAS. Nr. 356559-20-1
Appearance Solid
Molecular Weight 343.42
Formel C₂₁H₂₁N₅
Color Light yellow to yellow
SMILES

CC(C)(C1=NC(C2=CC=CC(C)=N2)=C(C3=CC=C4N=CC=NC4=C3)N1)C
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

J Hepatol

Transposon-based oncogene integration in Abcb4(Mdr2)-/- mice recapitulates high susceptibility to cholangiocarcinoma in primary sclerosing cholangitis. [Abstract]

2025 Jan;82(1):84-96. 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 Sep;11(34):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
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).
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
Antioxidants (Basel)

2026 Jul 2;15(7):836. PMID: 42510567
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
Pak Vet J

2026 Mar 11;46(3):544-555.
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
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
Biochim Biophys Acta Mol Basis Dis

Sustained anti-inflammatory effects of TGF-β1 on microglia/macrophages. [Abstract]

2018 Mar;1864(3):721-734. PMID: 29269050

SB 525334 purchased from MedChemExpress. Usage Cited in: Biochim Biophys Acta Mol Basis Dis. 2018 Mar;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.
Transl Oncol

A positive feedback loop between CDH11 and TGF-β signaling regulates migration and invasion of gastric cancer. [Abstract]

2026 May 13:69:102810. PMID: 42127732
Biochim Biophys Acta Mol Cell Res

TGF-β2 enhances glycolysis in chondrocytes via TβRI/p-Smad3 signaling pathway. [Abstract]

2024 Oct;1871(7):119788. PMID: 38879132
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
Am J Physiol Gastrointest Liver Physiol

High-oxygen gas-permeable culture improves viability and supports quantitative antifibrotic pharmacology in precision-cut liver slices. [Abstract]

2026 Aug 1;331(2):G216-G228. PMID: 42455056
Int J Hyperthermia

TGF-β1 inhibitor enhances the therapeutic effect of microwave ablation on hepatocellular carcinoma. [Abstract]

2024;41(1):2359496. PMID: 38909985
Biochem Biophys Res Commun

TGF-β3 enhances cell-to-cell communication in chondrocytes via the ALK5/p-Smad3 axis. [Abstract]

2022 Dec 25;636(Pt 1):64-74. PMID: 36332484
Parasitology

A combination of pirfenidone and TGF-β inhibition mitigates cystic echinococcosis-associated hepatic injury. [Abstract]

2021 Jun;148(7):767-778. PMID: 33583470
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
bioRxiv

2026 May 21.
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

Lösungsmittel & Löslichkeit

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.9119 mL

14.5594 mL

29.1189 mL

5 mM

0.5824 mL

2.9119 mL

5.8238 mL

10 mM

0.2912 mL

1.4559 mL

2.9119 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

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.

Working Solution

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.

Protocol 1

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

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Protokoll

All Cell Biology

Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (282 KB)
SDS (481 KB)
- English - EN (481 KB)
- Français - FR (481 KB)
- Deutsch - DE (481 KB)
- Norwegian - NO (481 KB)
- Español - ES (481 KB)
- Swedish - SV (481 KB)
- Italian - IT (481 KB)
- Korean - KR (481 KB)
- Portuguese - PT (481 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Bioz

Keywords

SB 525334

23 Cited Publications

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SB 525334

Publications Citing Use of MedChemExpress (MCE) SB 525334

Alle TGF-β Receptor Isoform-spezifische Produkte anzeigen