SIS3
Based on 107 publication(s) in Google Scholar
SIS3 is a potent and selective inhibitor of Smad3 with an IC50 of 3 μM for Smad3 phosphorylation. SIS3 inhibits the myofibroblast differentiation of fibroblasts by TGF-β1.
For research use only. We do not sell to patients.
- Purity: 99.62%
- CAS No.: 521984-48-5
- Formula: C28H28ClN3O3
- Molecular Weight:489.99
-
Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Purity & Documentation
- References
-
Help & FAQs
-
Immunology/Inflammation Compound Library
HY-L007
-
Stem Cell Signaling Compound Library
HY-L017
-
TGF-beta/Smad Compound Library
HY-L018
-
Wnt/Hedgehog/Notch Compound Library
HY-L020
-
Anti-Aging Compound Library
HY-L034
-
Covalent Screening Library
HY-L036
-
Angiogenesis-Related Compound Library
HY-L088
-
Transcription Factor-Targeted Library
HY-L090
-
Targeted Diversity Library
HY-L099
-
Anti-Colorectal Cancer Compound Library
HY-L103
-
Anti-Prostate Cancer Compound Library
HY-L124
-
Anti-Pulmonary Fibrosis Compound Library
HY-L125
-
Osteogenesis Compound Library
HY-L131
-
Cancer Stem Cells Compound Library
HY-L135
-
Highly Selective Inhibitors Library
HY-L158
-
Bioactive Compound Library Max
HY-L181
-
Anti-Aging Compound Library Mini
HY-L034M
-
MCE Bioactive Compound Library
HY-L001V
-
Covalent Screening Library Plus
HY-L036P
-
Bioactive Compound Library
HY-L001
-
Anti-Fibrosis Compound Library
HY-L185
-
Cell Proliferation Compound Library
HY-L201
-
High-Throughput Bioactive Compound Library
HY-L205
Publications Citing Use of MedChemExpress (MCE) SIS3
More- Cancer Cell. 2024 Apr 8;42(4):682-700.e12. [Abstract]
- Bioact Mater. 2025 Oct 15:56:77-94. [Abstract]
- Nat Commun. 2025 Oct 3;16(1):8826. [Abstract]
- Cell Death Differ. 2021 Mar;28(3):1001-1012. [Abstract]
- Theranostics. 2021 May 13;11(14):7110-7125. [Abstract]
- Nucleic Acids Res. 2023 Apr 11;51(6):2655-2670. [Abstract]
- Cell Discov. 2025 Mar 11;11(1):22. [Abstract]
- Redox Biol. 2023 Jun:62:102709. [Abstract]
- MedComm (2020). 2025 Mar 27;6(4):e70148. [Abstract]
- J ImmunoTher Cancer. 2020 Aug;8(2):e000422. [Abstract]
- Cell Death Dis. 2025 Dec 8;16(1):880. [Abstract]
- Cell Death Dis. 2024 Dec 24;15(12):930. [Abstract]
- Cell Commun Signal. 2026 Feb 9;24(1):167. [Abstract]
- Cell Commun Signal. 2025 Dec 4;24(1):12. [Abstract]
- Cell Commun Signal. 2025 Nov 12;23(1):492. [Abstract]
- Cell Commun Signal. 2025 Sep 30;23(1):402. [Abstract]
- Chin Herb Med. 2025 Jul 23;17(4):744-755. [Abstract]
- EMBO Mol Med. 2024 Apr;16(4):870-884. [Abstract]
- BMC Med. 2021 Oct 15;19(1):247. [Abstract]
- Brain Behav Immun. 2021 Jul:95:154-167. [Abstract]
- J Transl Med. 2025 Jul 10;23(1):763. [Abstract]
- Biomed Pharmacother. 2025 May 1:187:118094. [Abstract]
- Biomed Pharmacother. 2023 Sep:165:115225. [Abstract]
- Biomed Pharmacother. 2023 Mar:159:114216. [Abstract]
- Cell Death Discov. 2021 Oct 4;7(1):273. [Abstract]
- Neural Regen Res. 2024 Jan;19(1):180-189. [Abstract]
- Antioxidants (Basel). 2022 Dec 15;11(12):2469. [Abstract]
- NPJ Regen Med. 2020 Oct 30;5(1):19. [Abstract]
- Oncogenesis. 2021 Oct 27;10(10):72. [Abstract]
- Phytother Res. 2023 Feb;37(2):717-730. [Abstract]
- Cell Mol Life Sci. 2025 Aug 8;82(1):303. [Abstract]
- Cancer Cell Int. 2024 Mar 25;24(1):114. [Abstract]
- Int J Mol Med. 2019 Feb;43(2):993-1002. [Abstract]
- Chin Med. 2022 Feb 21;17(1):25. [Abstract]
- J Invest Dermatol. 2019 Jan;139(1):224-234. [Abstract]
- Biochem Pharmacol. 2023 Oct:216:115796. [Abstract]
- Biochem Pharmacol. 2022 Jan:195:114846. [Abstract]
- Am J Chin Med. 2024;52(6):1795-1817. [Abstract]
- J Ethnopharmacol. 2023 May 10:307:116243. [Abstract]
- Life Sci. 2026 Mar 1:388:124173. [Abstract]
- Commun Biol. 2025 Jul 29;8(1):1127. [Abstract]
- Life Sci. 2025 May 22:376:123755. [Abstract]
- Commun Biol. 2025 Mar 8;8(1):396. [Abstract]
- Life Sci. 2023 May 1:320:121540. [Abstract]
- CNS Neurosci Ther. 2022 Nov;28(11):1883-1894. [Abstract]
- Front Pharmacol. 2021 Dec 16:12:774316. [Abstract]
- Front Pharmacol. 2018 Jun 21:9:660. [Abstract]
- mBio. 2025 Jul 31:e0136625. [Abstract]
- Int Immunopharmacol. 2024 Sep 18;142(Pt B):113186. [Abstract]
- Am J Physiol Cell Physiol. 2022 Jul 1;323(1):C133-C144. [Abstract]
- Clin Epigenetics. 2023 Nov 11;15(1):182. [Abstract]
- Front Cell Dev Biol. 2020 Sep 18:8:858. [Abstract]
- FASEB J. 2026 Feb 15;40(3):e71484. [Abstract]
- Drug Dev Res. 2025 Nov;86(7):e70175. [Abstract]
- J Cell Mol Med. 2025 Mar;29(5):e70486. [Abstract]
- J Cell Mol Med. 2024 Nov;28(22):e70214. [Abstract]
- Drug Dev Res. 2023 Dec;84(8):1751-1763. [Abstract]
- FASEB J. 2022 Dec;36(12):e22625. [Abstract]
- J Clin Transl Hepatol. 2023 Feb 28;11(1):1-14. [Abstract]
- J Cell Mol Med. 2021 Dec;25(24):11113-11127. [Abstract]
- Biochim Biophys Acta Mol Basis Dis. 2018 Nov;1864(11):3824-3836. [Abstract]
- iScience. 2023 May 29;26(7):106994. [Abstract]
- Tissue Eng Regen Med. 2022 Jun;19(3):577-588. [Abstract]
- Tissue Eng Regen Med. 2021 Dec;18(6):963-973. [Abstract]
- J Cell Physiol. 2024 Mar;239(3):e31062. [Abstract]
- J Cell Physiol. 2020 Jan;235(1):429-441. [Abstract]
- J Biol Chem. 2024 Feb;300(2):105605. [Abstract]
- Aquaculture. 15 September 2022, 738360.
- Sci Rep. 2022 Feb 23;12(1):3053. [Abstract]
- Fish Shellfish Immunol. 2020 Feb;97:455-464. [Abstract]
- Sci Rep. 2017 Sep 8;7(1):11006. [Abstract]
- Cytokine. 2026 Aug:204:157169. [Abstract]
- Biochim Biophys Acta Mol Cell Res. 2022 May 13;1869(9):119285. [Abstract]
- Parasit Vectors. 2020 Apr 3;13(1):164. [Abstract]
- Mol Med Rep. 2019 Aug;20(2):1605-1612. [Abstract]
- Cell Cycle. 2026 Dec 15;25(1):1-17. [Abstract]
- Am J Physiol Renal Physiol. 2023 May 1;324(5):F433-F445. [Abstract]
- Cell Transplant. 2023 Jan-Dec:32:9636897231177356. [Abstract]
- Cell Transplant. 2023 Jan-Dec:32:9636897231162526. [Abstract]
- Front Biosci (Landmark Ed). 2024 Sep 24;29(9):336. [Abstract]
- J Dent Sci. 2023 Apr;18(2):865-871. [Abstract]
- Cell Biol Int. 2023 Apr;47(4):754-767. [Abstract]
- Biol Reprod. 2025 Aug 7:ioaf179. [Abstract]
- Mol Immunol. 2018 Nov:103:173-181. [Abstract]
- J Cell Biochem. 2019 Oct;120(10):17872-17886. [Abstract]
- Immunol Lett. 2019 Feb:206:33-40. [Abstract]
- Brain Res. 2022 Jan 15:1775:147711. [Abstract]
- Tissue Cell. 2025 Jul 29:97:103061. [Abstract]
- Acta Histochem. 2023 Feb;125(2):152010. [Abstract]
- Am J Reprod Immunol. 2021 Mar;85(3):e13344. [Abstract]
- Biochem Biophys Res Commun. 2026 Apr 9:808:153453. [Abstract]
- Med Sci Monit. 2018 Nov 18:24:8290-8297. [Abstract]
- Am J Transl Res. 2021 Sep 15;13(9):10908-10921. [Abstract]
- Am J Transl Res. 2020 Feb 15;12(2):478-492. [Abstract]
- Curr Med Sci. 2024 Jun;44(3):519-528. [Abstract]
- Stem Cell Res. 2020 Dec;49:102099. [Abstract]
- Int J Clin Exp Med. 2016;9(8):15892-15899.
- bioRxiv. 2025 Jun 24.
- bioRxiv. 2025 May 05.
- Meharry Medical College. 2024.
- Research Square Preprint. 2023 Jun 19.
- Wright State University. 2023 Feb 23.
- Research Square Print. September 15th, 2022.
- J Pers Med. 2022 Mar 2;12(3):385. [Abstract]
- Research Square Preprint. 2021 May.
- Eur Rev Med Pharmacol Sci. 2021 Jan;25(2):787-794. [Abstract]
- Research Square Preprint. 2020 Nov.
Customer Validation & Images
-
WB
-
WB
-
WB
-
WB
-
WB
Biological Activity
IC50: 3 μM (Smad3 phosphorylation)[1]
SIS3 (0.3-10 μM; for 1 hour) attenuates the TGF-beta1-induced phosphorylation of Smad3 and interaction of Smad3 with Smad4[1].
SIS3 (0.1, 10, 50 μM; 30 min) significantly suppresses the expression of FN and α-SMA, but not that of Sphk2 provoked by TGF-β1[2].
SIS3 (10 μM; 24 hours) significantly reduces both α-SMA and palladin expression that is enhanced by TWEAK in Primary human dermal fibroblasts[3].
SIS3 significantly inhibits L4 development at five concentrations from as low as 2 μM to 50 μM (5 μM, 10 μM, 20 μM and 50 μM) in a dose-dependent manner[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:Human dermal fibroblasts
-
Concentration:0.3, 1, 3, 10 μM
-
Incubation Time:For 1 hour
-
Result:Attenuated the TGF-beta1-induced phosphorylation of Smad3 and interaction of Smad3 with Smad4.
Chemical Information
-
CAS No. 521984-48-5
-
Appearance Solid
-
Molecular Weight 489.99
-
Formula C28H28ClN3O3
-
Color Off-white to yellow
-
SMILES
[H]Cl.O=C(/C=C/C1=C(N(C2=NC=CC=C21)C)C3=CC=CC=C3)N4CC5=C(CC4)C=C(C(OC)=C5)OC
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)
Publications (107)
-
Journal Impact Factor
-
Most Recent
-
Cancer Cell
PDGFRα+ITGA11+ fibroblasts foster early-stage cancer lymphovascular invasion and lymphatic metastasis via ITGA11-SELE interplay. [Abstract]2024 Apr 8;42(4):682-700.e12. PMID: 38428409 -
Bioact Mater
Hydrogel delivering antifibrotic agent and nano-sonosensitizer enhances efficacy of sonodynamic therapy in osteosarcoma treatment. [Abstract]2025 Oct 15:56:77-94. PMID: 41141582 -
Nat Commun
The inner nuclear membrane protein LEMD3 organizes the 3D chromatin architecture to maintain vascular smooth muscle cell identity. [Abstract]2025 Oct 3;16(1):8826. PMID: 41044070 -
Cell Death Differ
Histone deacetylase 3 aberration inhibits Klotho transcription and promotes renal fibrosis. [Abstract]2021 Mar;28(3):1001-1012. PMID: 33024274 -
Theranostics
Local administration of liposomal-based Srpx2 gene therapy reverses pulmonary fibrosis by blockading fibroblast-to-myofibroblast transition. [Abstract]2021 May 13;11(14):7110-7125. PMID: 34093874 -
Nucleic Acids Res
2023 Apr 11;51(6):2655-2670. PMID: 36727462 -
Cell Discov
2025 Mar 11;11(1):22. PMID: 40064862 -
Redox Biol
Mitochondrial fusion induced by transforming growth factor-β1 serves as a switch that governs the metabolic reprogramming during differentiation of regulatory T cells. [Abstract]2023 Jun:62:102709. PMID: 37116255 -
MedComm (2020)
Transforming Growth Factor Beta2 Promotes Migration and Inhibits the Proliferation of Gastric Cancer Cells by Regulating the pSmad2/3-NDRG1 Signaling Pathway. [Abstract]2025 Mar 27;6(4):e70148. PMID: 40151835 -
J ImmunoTher Cancer
2020 Aug;8(2):e000422. PMID: 32753468 -
Cell Death Dis
2025 Dec 8;16(1):880. PMID: 41360769 -
Cell Death Dis
Ovarian cancer-derived TGF-β1 induces cancer-associated adipocytes formation by activating SMAD3/TRIB3 pathway to establish pre-metastatic niche. [Abstract]2024 Dec 24;15(12):930. PMID: 39719444 -
Cell Commun Signal
Secreted RCN3 acts as an early epithelial-fibroblast mediator via TGFβR1-Smad signaling in post-ALI pulmonary fibrosis. [Abstract]2026 Feb 9;24(1):167. PMID: 41664195 -
Cell Commun Signal
2025 Dec 4;24(1):12. PMID: 41345872 -
Cell Commun Signal
2025 Nov 12;23(1):492. PMID: 41225541 -
Cell Commun Signal
PDPN+LTBP1+ cancer-associated fibroblasts induce a liver pre-metastatic niche in gastric cancer via PDPN/YAP/LTBP1 and CCL11/CCR3 axis. [Abstract]2025 Sep 30;23(1):402. PMID: 41029689 -
Chin Herb Med
Rhein alleviates renal interstitial fibrosis by inhibiting Smad3 phosphorylation in TGF- β/Smad signalling pathway. [Abstract]2025 Jul 23;17(4):744-755. PMID: 41399800 -
EMBO Mol Med
2024 Apr;16(4):870-884. PMID: 38462666 -
BMC Med
HBeAg mediates inflammatory functions of macrophages by TLR2 contributing to hepatic fibrosis. [Abstract]2021 Oct 15;19(1):247. PMID: 34649530 -
Brain Behav Immun
Inhibition of Smad3 in macrophages promotes Aβ efflux from the brain and thereby ameliorates Alzheimer's pathology. [Abstract]2021 Jul:95:154-167. PMID: 33737172 -
J Transl Med
CCN5 negatively regulates TGF-β-induced endometriosis associated fibrosis through Wnt/β-catenin signaling via Smad3-dependent mechanism. [Abstract]2025 Jul 10;23(1):763. PMID: 40640862 -
Biomed Pharmacother
Transforming growth factor-β receptor I kinase plays a crucial role in oligodendrocyte regeneration after demyelination. [Abstract]2025 May 1:187:118094. PMID: 40315672 -
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 -
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 -
Cell Death Discov
LHPP suppresses colorectal cancer cell migration and invasion in vitro and in vivo by inhibiting Smad3 phosphorylation in the TGF-β pathway. [Abstract]2021 Oct 4;7(1):273. PMID: 34608127 -
Neural Regen Res
Photobiomodulation inhibits the expression of chondroitin sulfate proteoglycans after spinal cord injury via the Sox9 pathway. [Abstract]2024 Jan;19(1):180-189. PMID: 37488865 -
Antioxidants (Basel)
Oxidized High-Density Lipoprotein Induces Endothelial Fibrosis Promoting Hyperpermeability, Hypotension, and Increased Mortality. [Abstract]2022 Dec 15;11(12):2469. PMID: 36552677 -
NPJ Regen Med
2020 Oct 30;5(1):19. PMID: 33298919 -
Oncogenesis
2021 Oct 27;10(10):72. PMID: 34707087 -
Phytother Res
Ligustilide attenuates airway remodeling in COPD mice by covalently binding to MH2 domain of Smad3 in pulmonary epithelium, disrupting the Smad3-SARA interaction. [Abstract]2023 Feb;37(2):717-730. PMID: 36216328 -
Cell Mol Life Sci
PGC1α regulates the mitochondrial metabolism response to cyclic stretch, which inhibits neointimal hyperplasia. [Abstract]2025 Aug 8;82(1):303. PMID: 40779200 -
Cancer Cell Int
Domperidone inhibits cell proliferation via targeting MEK and CDK4 in esophageal squamous cell carcinoma. [Abstract]2024 Mar 25;24(1):114. PMID: 38528618 -
Int J Mol Med
MicroRNA-323 suppresses nerve cell toxicity in cerebral infarction via the transforming growth factor-β1/SMAD3 signaling pathway. [Abstract]2019 Feb;43(2):993-1002. PMID: 30535466
SIS3 purchased from MedChemExpress. Usage Cited in: Int J Mol Med. 2019 Feb;43(2):993-1002. [Abstract]
Western analysis of FN expression in HUVECs pretreated with PD98059 and SIS3.
-
Chin Med
Ginkgo biloba leaf extract mitigates cisplatin-induced chronic renal interstitial fibrosis by inhibiting the epithelial-mesenchymal transition of renal tubular epithelial cells mediated by the Smad3/TGF-β1 and Smad3/p38 MAPK pathways. [Abstract]2022 Feb 21;17(1):25. PMID: 35189929 -
J Invest Dermatol
2019 Jan;139(1):224-234. PMID: 30081003 -
Biochem Pharmacol
Upregulation of IL-37 in epithelial cells: A potential new mechanism of T cell inhibition induced by tacrolimus. [Abstract]2023 Oct:216:115796. PMID: 37690572 -
Biochem Pharmacol
SIS3 suppresses osteoclastogenesis and ameliorates bone loss in ovariectomized mice by modulating Nox4-dependent reactive oxygen species. [Abstract]2022 Jan:195:114846. PMID: 34801525 -
Am J Chin Med
Astragaloside I from Astragalus Attenuates Diabetic Kidney Disease by Regulating HDAC3/Klotho/TGF- β 1 Loop. [Abstract]2024;52(6):1795-1817. PMID: 39347955 -
J Ethnopharmacol
Yishen Tongluo formula alleviates diabetic kidney disease through regulating Sirt6/TGF-β1/Smad2/3 pathway and promoting degradation of TGF-β1. [Abstract]2023 May 10:307:116243. PMID: 36791927 -
Life Sci
Galectin-9 in human trophoblast cells: Implications for maternal-fetal immune balance and pregnancy complications. [Abstract]2026 Mar 1:388:124173. PMID: 41544754 -
Commun Biol
Pantothenic acid ameliorates hepatic fibrosis by targeting IGFBP6 to regulate the TGF-β/SMADs pathway. [Abstract]2025 Jul 29;8(1):1127. PMID: 40730679 -
Life Sci
Targeting interferon regulatory factor 7 alleviates renal fibrosis by inhibiting macrophage-to-myofibroblast transition. [Abstract]2025 May 22:376:123755. PMID: 40412608 -
Commun Biol
Melatonin affects trophoblast epithelial-to-mesenchymal transition and oxidative damage resistance by modulating GDF15 expression to promote embryo implantation. [Abstract]2025 Mar 8;8(1):396. PMID: 40057595 -
Life Sci
Low dose Taxol ameliorated renal fibrosis in mice with diabetic kidney disease by downregulation of HIPK2. [Abstract]2023 May 1:320:121540. PMID: 36907324 -
CNS Neurosci Ther
Apigenin inhibits fibrous scar formation after acute spinal cord injury through TGFβ/SMADs signaling pathway. [Abstract]2022 Nov;28(11):1883-1894. PMID: 35906830 -
Front Pharmacol
The Preventive Effect of Decorin on Epidural Fibrosis and Epidural Adhesions After Laminectomy. [Abstract]2021 Dec 16:12:774316. PMID: 34975478 -
Front Pharmacol
2018 Jun 21:9:660. PMID: 29977207
SIS3 purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2018 Jun 21:9:660. [Abstract]
By Western blotting, the α-SMA and palladin proteins are determined in cells that are pretreated with NF-κB (JSH-23), Wnt/β-catenin (XAV939), EGFR (erlotinib), p38 MAPK (TAK-715), and Smad3 (SIS3) inhibitors and are followed by TWEAK stimulation.
-
mBio
2025 Jul 31:e0136625. PMID: 40742129 -
Int Immunopharmacol
The role of the PI3K/AKT/mTOR pathway in mediating PD-L1 upregulation during fibroblast transdifferentiation. [Abstract]2024 Sep 18;142(Pt B):113186. PMID: 39298817 -
Am J Physiol Cell Physiol
DOCK2 contributes to pulmonary fibrosis by promoting lung fibroblast to myofibroblast transition. [Abstract]2022 Jul 1;323(1):C133-C144. PMID: 35584329 -
Clin Epigenetics
Histone deacetylase 3 deletion in alveolar type 2 epithelial cells prevents bleomycin-induced pulmonary fibrosis. [Abstract]2023 Nov 11;15(1):182. PMID: 37951958 -
Front Cell Dev Biol
2020 Sep 18:8:858. PMID: 33072735 -
FASEB J
Nur77 Regulates the Phosphorylation of Smad3, Thereby Influencing Skeletal Muscle Fibrosis Caused by Obesity. [Abstract]2026 Feb 15;40(3):e71484. PMID: 41652518 -
Drug Dev Res
RBM15B/IGF2BP2-m6A Mediated Upregulation of FNBP1 Promotes the Progression of Glioblastoma by Promoting Smad3-Mediated Glycolysis. [Abstract]2025 Nov;86(7):e70175. PMID: 41086050 -
J Cell Mol Med
2025 Mar;29(5):e70486. PMID: 40052646 -
J Cell Mol Med
Sinomenine Ameliorated Microglial Activation and Neuropathic Pain After Chronic Constriction Injury Via TGF-β1/ALK5/Smad3 Signalling Pathway. [Abstract]2024 Nov;28(22):e70214. PMID: 39586784 -
Drug Dev Res
(E)-SIS3 suppressed osteosarcoma progression via promoting cell apoptosis, arresting cell cycle, and regulating the tumor immune microenvironment. [Abstract]2023 Dec;84(8):1751-1763. PMID: 37784254 -
FASEB J
Renal tubular epithelial cell necroptosis promotes tubulointerstitial fibrosis in patients with chronic kidney disease. [Abstract]2022 Dec;36(12):e22625. PMID: 36331546 -
J Clin Transl Hepatol
Upregulation of GLT25D1 in Hepatic Stellate Cells Promotes Liver Fibrosis via the TGF-β1/SMAD3 Pathway In Vivo and In vitro. [Abstract]2023 Feb 28;11(1):1-14. PMID: 36406310 -
J Cell Mol Med
Soluble TREM-1, as a new ligand for the membrane receptor Robo2, promotes hepatic stellate cells activation and liver fibrosis. [Abstract]2021 Dec;25(24):11113-11127. PMID: 34750987 -
Biochim Biophys Acta Mol Basis Dis
Sphingosine kinase 2 cooperating with Fyn promotes kidney fibroblast activation and fibrosis via STAT3 and AKT. [Abstract]2018 Nov;1864(11):3824-3836. PMID: 30251698
SIS3 purchased from MedChemExpress. Usage Cited in: Biochim Biophys Acta Mol Basis Dis. 2018 Nov;1864(11):3824-3836. [Abstract]
NRK-49F cells are preincubated with 100 nM, 10 μM, or 50 μM Smad3 inhibitor SIS3 for 30 min followed by TGF-β1 (2 ng/mL) stimulation for 12 h. Then, the expression of Sphk2, fibronectin, and α-SMA is determined by Western blotting.
-
iScience
SMYD3 induces sorafenib resistance by activating SMAD2/3-mediated epithelial-mesenchymal transition in hepatocellular carcinoma. [Abstract]2023 May 29;26(7):106994. PMID: 37534166 -
Tissue Eng Regen Med
IL-33 Promotes ST2-Dependent Fibroblast Maturation via P38 and TGF-β in a Mouse Model of Epidural Fibrosis. [Abstract]2022 Jun;19(3):577-588. PMID: 35195855 -
Tissue Eng Regen Med
Three-Dimensional Modeling of the Structural Microenvironment in Post-Traumatic War Wounds. [Abstract]2021 Dec;18(6):963-973. PMID: 34363599 -
J Cell Physiol
Periodontal ligament-associated protein-1 knockout mice regulate the differentiation of osteoclasts and osteoblasts through TGF-β1/Smad signaling pathway. [Abstract]2024 Mar;239(3):e31062. PMID: 37357387 -
J Cell Physiol
NMI promotes cell proliferation through TGFβ/Smad pathway by upregulating STAT1 in colorectal cancer. [Abstract]2020 Jan;235(1):429-441. PMID: 31230364 -
J Biol Chem
2024 Feb;300(2):105605. PMID: 38159857 -
-
Sci Rep
PD-L1 mediates lung fibroblast to myofibroblast transition through Smad3 and β-catenin signaling pathways. [Abstract]2022 Feb 23;12(1):3053. PMID: 35197539 -
Fish Shellfish Immunol
2020 Feb;97:455-464. PMID: 31870970 -
Sci Rep
Glycosylation-dependent galectin-1/neuropilin-1 interactions promote liver fibrosis through activation of TGF-β- and PDGF-like signals in hepatic stellate cells. [Abstract]2017 Sep 8;7(1):11006. PMID: 28887481 -
Cytokine
2026 Aug:204:157169. PMID: 42143915 -
Biochim Biophys Acta Mol Cell Res
Fibulin-3 regulates the inhibitory effect of TNF-α on chondrocyte differentiation partially via the TGF-β/Smad3 signaling pathway. [Abstract]2022 May 13;1869(9):119285. PMID: 35577279 -
Parasit Vectors
Identification and characterization of an R-Smad homologue (Hco-DAF-8) from Haemonchus contortus. [Abstract]2020 Apr 3;13(1):164. PMID: 32245505 -
Mol Med Rep
Carvedilol improves liver cirrhosis in rats by inhibiting hepatic stellate cell activation, proliferation, invasion and collagen synthesis. [Abstract]2019 Aug;20(2):1605-1612. PMID: 31257490
SIS3 purchased from MedChemExpress. Usage Cited in: Mol Med Rep. 2019 Aug;20(2):1605-1612. [Abstract]
SIS3 treatment decreases the TGFβ1-induced expression of Col I and FN.
-
Cell Cycle
Goosecoid facilitates the metastasis of pancreatic adenocarcinoma by enhancing EMT and stemness via regulating TGF-β/SMAD2/3 signaling. [Abstract]2026 Dec 15;25(1):1-17. PMID: 41532321 -
Am J Physiol Renal Physiol
Tacrolimus Induces Fibroblast to Myofibroblast Transition via a TGFβ-Dependent Mechanism to Contribute to Renal Fibrosis. [Abstract]2023 May 1;324(5):F433-F445. PMID: 36927118 -
Cell Transplant
Dexamethasone Induces Senescence-Associated Changes in Trabecular Meshwork Cells by Increasing ROS Levels Via the TGFβ/Smad3-NOX4 Axis. [Abstract]2023 Jan-Dec:32:9636897231177356. PMID: 37265069 -
Cell Transplant
Elevated Angiotensin-II Levels Contribute to the Pathogenesis of Open-Angle Glaucoma Via Inducing the Expression of Fibrosis-Related Genes in Trabecular Meshwork Cells Through a ROS/NOX4/SMAD3 Axis. [Abstract]2023 Jan-Dec:32:9636897231162526. PMID: 36999649 -
Front Biosci (Landmark Ed)
β-Adrenoceptor Signaling Activation Improves Bladder Fibrosis by Inhibiting Extracellular Matrix Deposition of Bladder Outlet Obstruction. [Abstract]2024 Sep 24;29(9):336. PMID: 39344310 -
J Dent Sci
Specific inhibitor of Smad3 (SIS3) alleviated submandibular gland fibrosis and dysfunction after dominant duct ligation in mice. [Abstract]2023 Apr;18(2):865-871. PMID: 37021213 -
Cell Biol Int
Crosstalk between myofibroblasts and macrophages: A regulative factor of valvular fibrosis in calcific aortic valve disease. [Abstract]2023 Apr;47(4):754-767. PMID: 36542640 -
Biol Reprod
Activin A promotes bovine pituitary FSH synthesis and secretion through the cooperative action of the SMAD signaling pathway and FOXO3†. [Abstract]2025 Aug 7:ioaf179. PMID: 40795281 -
Mol Immunol
TGF-β1-Induced Airway Smooth Muscle Cell Proliferation Involves TRPM7-Dependent Calcium Influx via TGFβR/SMAD3. [Abstract]2018 Nov:103:173-181. PMID: 30290314
SIS3 purchased from MedChemExpress. Usage Cited in: Mol Immunol. 2018 Nov:103:173-181. [Abstract]
TRPM7 mRNA and protein expressions are effectively suppressed by LY2109761 and SIS3 in ASMCs compared with those in 10 ng/mL TGF-β1-stimulated cells.
-
J Cell Biochem
β-Adrenoceptor signaling regulates proliferation and contraction of human bladder smooth muscle cells under pathological hydrostatic pressure. [Abstract]2019 Oct;120(10):17872-17886. PMID: 31161623 -
Immunol Lett
A dual role of TGF-β in human osteoclast differentiation mediated by Smad1 versus Smad3 signaling. [Abstract]2019 Feb:206:33-40. PMID: 30543834
SIS3 purchased from MedChemExpress. Usage Cited in: Immunol Lett. 2019 Feb:206:33-40. [Abstract]
Monocytes were cultured with 20 ng/mL M-CSF with or without 10 ng/mL TGF-β1 for 2 days, with SB431542 (1 or 50 μM) or SIS3 (2.5 μM) having been added 30 min beforehand. Whole-cell lysates were subjected to SDS-PAGE and immunoblotted.
-
Brain Res
Umbilical cord mesenchymal stem cells promote neurological repair after traumatic brain injury through regulating Treg/Th17 balance. [Abstract]2022 Jan 15:1775:147711. PMID: 34793756 -
Tissue Cell
IMUP promotes fatty acid metabolism and lung cancer progression by regulating TGF-β/SMAD3 signaling pathway. [Abstract]2025 Jul 29:97:103061. PMID: 40749423 -
Acta Histochem
Low dose TGF-β1 can improve vohwinkel syndrome by promoting the proliferation of keratinocytes. [Abstract]2023 Feb;125(2):152010. PMID: 36738515 -
Am J Reprod Immunol
Baicalein inhibits FURIN-MT1-MMP-mediated invasion of ectopic endometrial stromal cells in endometriosis possibly by reducing the secretion of TGFB1. [Abstract]2021 Mar;85(3):e13344. PMID: 32910833 -
Biochem Biophys Res Commun
Macrophage erythropoietin receptor signaling drives macrophage-myofibroblast transition via JAK2/STAT3 and TGF-β1/Smad3 pathways to exacerbate pulmonary fibrosis in mice. [Abstract]2026 Apr 9:808:153453. PMID: 41719615 -
Med Sci Monit
Carvedilol Ameliorates Intrahepatic Angiogenesis, Sinusoidal Remodeling and Portal Pressure in Cirrhotic Rats. [Abstract]2018 Nov 18:24:8290-8297. PMID: 30448852 -
Am J Transl Res
Baicalin promotes chondrocyte viability and the synthesis of extracellular matrix through TGF-β/Smad3 pathway in chondrocytes. [Abstract]2021 Sep 15;13(9):10908-10921. PMID: 34650772 -
Am J Transl Res
Fatty acid extracts facilitate cutaneous wound healing through activating AKT, ERK, and TGF-β/Smad3 signaling and promoting angiogenesis. [Abstract]2020 Feb 15;12(2):478-492. PMID: 32194897 -
Curr Med Sci
TL1A Promotes Fibrogenesis in Colonic Fibroblasts via the TGF-β1/Smad3 Signaling Pathway. [Abstract]2024 Jun;44(3):519-528. PMID: 38842774 -
Stem Cell Res
2020 Dec;49:102099. PMID: 33296812 -
SIS3 purchased from MedChemExpress. Usage Cited in: Int J Clin Exp Med. 2016;9(8):15892-15899.
CNE1 cells are cultured with 3 μM SIS3 for 4 hs, and then washed by cold PBS and followed by the 10 ng/mL TGF-β treatments for 48 hs, respectively.
-
-
-
-
-
-
-
J Pers Med
Reducing the Excess Activin Signaling Rescues Muscle Degeneration in Myotonic Dystrophy Type 2 Drosophila Model. [Abstract]2022 Mar 2;12(3):385. PMID: 35330385 -
-
Eur Rev Med Pharmacol Sci
Expression of miR-207 in renal tissue of renal fibrosis rats and its correlation analysis with protein expression of TGF-β1 and Smad3. [Abstract]2021 Jan;25(2):787-794. PMID: 33577033 -
Solvent & Solubility
DMSO : 100 mg/mL (204.09 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). 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 (5.10 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
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.
Please enter the basic information of animal 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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)
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
-
Data Sheet (278 KB)
-
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)
-
Handling Instructions (2659 KB)
References
[1]. Jinnin M et al. Characterization of SIS3, a novel specific inhibitor of Smad3, and its effect on transforming growth factor-beta1-induced extracellular matrix expression. Mol Pharmacol. 2006 Feb;69(2):597-607. [Content Brief]
[2]. Zhu X, et al. Sphingosine kinase 2 cooperating with Fyn promotes kidney fibroblast activation and fibrosis via STAT3 and AKT. Biochim Biophys Acta Mol Basis Dis. 2018 Nov;1864(11):3824-3836. [Content Brief]
[3]. Liu J, et al. Topical TWEAK Accelerates Healing of Experimental Burn Wounds in Mice. Front Pharmacol. 2018 Jun 21;9:660. [Content Brief]
[4]. Li FF, et al. Identification and characterization of an R-Smad homologue (Hco-DAF-8) from Haemonchuscontortus. Parasit Vectors. 2020 Apr 3;13(1):164. [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 (sealed storage, away from moisture). 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 | 2.0409 mL | 10.2043 mL | 20.4086 mL | 51.0215 mL |
| 5 mM | 0.4082 mL | 2.0409 mL | 4.0817 mL | 10.2043 mL | |
| 10 mM | 0.2041 mL | 1.0204 mL | 2.0409 mL | 5.1021 mL | |
| 15 mM | 0.1361 mL | 0.6803 mL | 1.3606 mL | 3.4014 mL | |
| 20 mM | 0.1020 mL | 0.5102 mL | 1.0204 mL | 2.5511 mL | |
| 25 mM | 0.0816 mL | 0.4082 mL | 0.8163 mL | 2.0409 mL | |
| 30 mM | 0.0680 mL | 0.3401 mL | 0.6803 mL | 1.7007 mL | |
| 40 mM | 0.0510 mL | 0.2551 mL | 0.5102 mL | 1.2755 mL | |
| 50 mM | 0.0408 mL | 0.2041 mL | 0.4082 mL | 1.0204 mL | |
| 60 mM | 0.0340 mL | 0.1701 mL | 0.3401 mL | 0.8504 mL | |
| 80 mM | 0.0255 mL | 0.1276 mL | 0.2551 mL | 0.6378 mL | |
| 100 mM | 0.0204 mL | 0.1020 mL | 0.2041 mL | 0.5102 mL |
Powered by Bioz