SIS3 HCl, a novel specific inhibitor of Smad3, inhibits TGF-β and activin signaling by suppressing Smad3 phosphorylation without affecting the MAPK/p38, ERK, or PI3-kinase signaling pathways.
Chemical Formula: C28H28ClN3O3
Exact Mass: 489.1819
Molecular Weight: 490.0
Elemental Analysis: C, 68.63; H, 5.76; Cl, 7.23; N, 8.58; O, 9.80
2-Propen-1-one,1-(3,4-dihydro-6,7-dimethoxy-2(1H)-isoquinolinyl)-3-(1-methyl-2-phenyl-1H-pyrrolo[2,3-b]pyridin-3-yl)-, hydrochloride (1:1), (2E)-
InChi Code: InChI=1S/C28H27N3O3.ClH/c1-30-27(19-8-5-4-6-9-19)22(23-10-7-14-29-28(23)30)11-12-26(32)31-15-13-20-16-24(33-2)25(34-3)17-21(20)18-31;/h4-12,14,16-17H,13,15,18H2,1-3H3;1H/b12-11+;
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
Shelf Life: >3 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: 2934.99.03.00
(E)-SIS3 (0.3-10 μM; for 1 hour) attenuates the TGF-beta1-induced phosphorylation of Smad3 and interaction of Smad3 with Smad4.
(E)-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.
(E)-SIS3 (10 μM; 24 hours) significantly reduces both α-SMA and palladin expression that is enhanced by TWEAK in Primary human dermal fibroblasts.
(E)-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.
- Jinnin M, et al. Mol Pharmacol. 2006, 69(2):597-607.
- Li J, et al. Diabetes. 2010, 59(10):2612-24.
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