WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 407168
CAS#: 1009104-85-1
Description: SMAD3 is a receptor-regulated intracellular protein that functions downstream of TGF-β and activin receptors and mediates their signaling, playing a role in cell proliferation, differentiation, apoptosis and formation of extracellular matrix. Smad3 Inhibitor, SIS3 is a cell-permeable pyrrolopyridine compound that selectively inhibits TGF-β1-dependent Smad3 phosphorylation and Smad3-mediated cellular signaling with no effect on Smad2, p38 MAPK, ERK, or PI 3-K signaling. It has been shown to reduce TGF-β1-induced type 1 procollagen expression and myofibroblast differentiation in normal dermal fibroblasts as well as scleroderma fibroblasts.
MedKoo Cat#: 407168
Name: SIS3
CAS#: 1009104-85-1
Chemical Formula: C27H26ClN3O3
Exact Mass:
Molecular Weight: 475.97
Elemental Analysis: C, 68.13; H, 5.51; Cl, 7.45; N, 8.83; O, 10.08
Synonym: 6,7-Dimethoxy-2-((2E)-3-(1-methyl-2-phenyl-1H-pyrrolo[2,3-b]pyridin-3-yl-prop-2-enoyl))-1,2,3,4-tetrahydroisoquinoline; Specific Inhibitor of Smad3; SIS3
IUPAC/Chemical Name: 1,2,3,4-Tetrahydro-6,7-dimethoxy-2-[(2E)-3-(1-phenyl-1H-pyrrolo[2,3-b]pyridin-3-yl)-1-oxo-2-propenyl]-isoquinoline hydrochloride
InChi Key: JGYPXYFVARTDSW-ASTDGNLGSA-N
InChi Code: InChI=1S/C27H25N3O3.ClH/c1-32-24-15-19-12-14-29(17-21(19)16-25(24)33-2)26(31)11-10-20-18-30(22-7-4-3-5-8-22)27-23(20)9-6-13-28-27;/h3-11,13,15-16,18H,12,14,17H2,1-2H3;1H/b11-10+;
SMILES Code: CN1C(=C(C2=C1N=CC=C2)C=CC(=O)N3CCC4=CC(=C(C=C4C3)OC)OC)C5=CC=CC=C5.Cl
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
The following data is based on the product molecular weight 475.97 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
1: Li LF, Lee CS, Liu YY, Chang CH, Lin CW, Chiu LC, Kao KC, Chen NH, Yang CT. Activation of Src-dependent Smad3 signaling mediates the neutrophilic inflammation and oxidative stress in hyperoxia-augmented ventilator-induced lung injury. Respir Res. 2015 Sep 16;16(1):112. doi: 10.1186/s12931-015-0275-6. PubMed PMID: 26377087; PubMed Central PMCID: PMC4574227.
2: Li J, Xiong J, Yang B, Zhou Q, Wu Y, Luo H, Zhou H, Liu N, Li Y, Song Z, Zheng Q. Endothelial Cell Apoptosis Induces TGF-β Signaling-Dependent Host Endothelial-Mesenchymal Transition to Promote Transplant Arteriosclerosis. Am J Transplant. 2015 Aug 4. doi: 10.1111/ajt.13406. [Epub ahead of print] PubMed PMID: 26372910.
3: Sundararaj K, Pleasant DL, Moschella PC, Panneerselvam K, Balasubramanian S, Kuppuswamy D. mTOR Complexes Repress Hypertrophic Agonist-Stimulated Expression of Connective Tissue Growth Factor in Adult Cardiac Muscle Cells. J Cardiovasc Pharmacol. 2015 Sep 14. [Epub ahead of print] PubMed PMID: 26371948.
4: Zhu Y, Tao H, Jin C, Liu Y, Lu X, Hu X, Wang X. Transforming growth factor β1 induces type II collagen and aggrecan expression via activation of extracellular signal regulated kinase 1/2 and Smad2/3 signaling pathways. Mol Med Rep. 2015 Oct;12(4):5573-9. doi: 10.3892/mmr.2015.4068. Epub 2015 Jul 9. PubMed PMID: 26165845.
5: Deng X, Jin K, Li Y, Gu W, Liu M, Zhou L. Platelet-Derived Growth Factor and Transforming Growth Factor β1 Regulate ARDS-Associated Lung Fibrosis Through Distinct Signaling Pathways. Cell Physiol Biochem. 2015;36(3):937-46. doi: 10.1159/000430268. Epub 2015 Jun 12. PubMed PMID: 26088859.
6: Wang Z, Xu W, Rong A, Lin Y, Qiu XL, Qu S, Lan XH. Neovibsanin B increases extracellular matrix proteins in optic nerve head cells via activation of Smad signalling pathway. Int J Clin Exp Pathol. 2015 Mar 1;8(3):3395-403. eCollection 2015. PubMed PMID: 26045877; PubMed Central PMCID: PMC4440186.
7: Yang H, Zhan L, Yang T, Wang L, Li C, Zhao J, Lei Z, Li X, Zhang HT. Ski prevents TGF-β-induced EMT and cell invasion by repressing SMAD-dependent signaling in non-small cell lung cancer. Oncol Rep. 2015 Jul;34(1):87-94. doi: 10.3892/or.2015.3961. Epub 2015 May 7. PubMed PMID: 25955797.
8: Sun YB, Qu X, Howard V, Dai L, Jiang X, Ren Y, Fu P, Puelles VG, Nikolic-Paterson DJ, Caruana G, Bertram JF, Sleeman MW, Li J. Smad3 deficiency protects mice from obesity-induced podocyte injury that precedes insulin resistance. Kidney Int. 2015 Aug;88(2):286-98. doi: 10.1038/ki.2015.121. Epub 2015 May 6. PubMed PMID: 25945408.
9: Yamamoto N, Otsuka T, Kondo A, Matsushima-Nishiwaki R, Kuroyanagi G, Kozawa O, Tokuda H. Rac limits TGF-β-induced VEGF synthesis in osteoblasts. Mol Cell Endocrinol. 2015 Apr 15;405:35-41. doi: 10.1016/j.mce.2015.02.002. Epub 2015 Feb 7. PubMed PMID: 25662279.
10: Li L, Yin Q, Tang X, Bai L, Zhang J, Gou S, Zhu H, Cheng J, Fu P, Liu F. C3a receptor antagonist ameliorates inflammatory and fibrotic signals in type 2 diabetic nephropathy by suppressing the activation of TGF-β/smad3 and IKBα pathway. PLoS One. 2014 Nov 25;9(11):e113639. doi: 10.1371/journal.pone.0113639. eCollection 2014. PubMed PMID: 25422985; PubMed Central PMCID: PMC4244104.
