TGF-beta/Smad

シグナル伝達経路

研究分野

阻害剤の選択性比較

カタログ番号	製品カタログ	溶解度(25°C)
カタログ番号	製品カタログ	水	DMSO	アルコール
S1067	SB431542	<1 mg/mL	76 mg/mL	3 mg/mL
S2618	LDN-193189	<1 mg/mL	<1 mg/mL	<1 mg/mL
S2230	Galunisertib (LY2157299)	<1 mg/mL	74 mg/mL	<1 mg/mL
S2704	LY2109761	<1 mg/mL	2 mg/mL	<1 mg/mL
S1476	SB525334	<1 mg/mL	68 mg/mL	68 mg/mL
S8772	LY 3200882	<1 mg/mL	87 mg/mL	<1 mg/mL
S2186	SB505124	<1 mg/mL	67 mg/mL	67 mg/mL
S2907	Pirfenidone	<1 mg/mL	37 mg/mL	37 mg/mL
S2750	GW788388	<1 mg/mL	15 mg/mL	<1 mg/mL
S2805	LY364947	<1 mg/mL	1 mg/mL	<1 mg/mL
S7223	RepSox	<1 mg/mL	57 mg/mL	<1 mg/mL
S7507	LDN-193189 HCl	52 mg/mL	<1 mg/mL	<1 mg/mL
S7359	K02288	<1 mg/mL	70 mg/mL	<1 mg/mL
S7624	SD-208	<1 mg/mL	9 mg/mL	<1 mg/mL
S7627	LDN-214117	<1 mg/mL	83 mg/mL	83 mg/mL
S7959	SIS3 HCl	<1 mg/mL	97 mg/mL	24 mg/mL
S7530	Vactosertib (TEW-7197)	<1 mg/mL	79 mg/mL	43 mg/mL
S7146	DMH1	<1 mg/mL	22 mg/mL	<1 mg/mL
S7147	LDN-212854	<1 mg/mL	81 mg/mL	<1 mg/mL
S7148	ML347	<1 mg/mL	10 mg/mL	<1 mg/mL
S7658	Kartogenin	<1 mg/mL	63 mg/mL	5 mg/mL
S2308	Hesperetin	<1 mg/mL	60 mg/mL	<1 mg/mL
S8318	Alantolactone	<1 mg/mL	46 mg/mL	46 mg/mL

亜型選択性的な製品

TGF-beta/Smad製品

All (23) TGF-beta/Smad阻害剤(20) TGF-beta/Smad活性剤(1) TGF-beta/Smad化学物質(2) 新TGF-beta/Smad製品

製品コード	製品説明	文献中Selleckの製品使用例	お客様のフィードバック
S1067	SB431542 SB431542 is a potent and selective inhibitor of ALK5 with IC50 of 94 nM in a cell-free assay, 100-fold more selective for ALK5 than p38 MAPK and other kinases.	Nature, 2018, 557(7704):247-251 Nature, 2015, 524(7564):234-8 Nature, 2016, 10.1038/nature17408	Phase-contrast images of RPBJ- and HNF6-deficient hepatocyte spheroids embedded in collagen gels and cultured in the presence or absence of the TGFβ inhibitor SB-431542 (SB) for the indicated number of days.
S2618	LDN-193189 LDN-193189 is a selective BMP signaling inhibitor, inhibits the transcriptional activity of the BMP type I receptors ALK2 and ALK3 with IC50 of 5 nM and 30 nM in C2C12 cells, respectively, exhibits 200-fold selectivity for BMP versus TGF-β.	Cancer Cell, 2014, 26(4):521-33 J Clin Invest, 2015, 125(2):796-808 Int J Cancer, 2014, 136(5):E455-69	LDN induces signifiant cell death. OVCA429 cells were treated with vehicle (DMSO) or experimental drugs for 6 hr to capture different stages of cell death. OVCA429 cell viability was assessed in response to drug treatment for 6 hr by staining with AO (green) and EB (orange). For clarity the different fluorescent channels to detect AO, EB, and the over-lapping images are shown for 10 mM LDN treatment.
S2230	Galunisertib (LY2157299) Galunisertib (LY2157299) is a potent TGFβ receptor I (TβRI) inhibitor with IC50 of 56 nM in a cell-free assay. Phase 2/3.	Nat Immunol, 2016, 17(8):976-84 Nat Cell Biol, 2015, 17(3):340-9 Clin Cancer Res, 2018, 10.1158/1078-0432.CCR-18-1346	Treatment of HLE and HLF cells with TGFβRI inhibitor LY2157299 led to dose-dependent loss of GLI2 levels.
S2704	LY2109761 LY2109761 is a novel selective TGF-β receptor type I/II (TβRI/II) dual inhibitor with K_i of 38 nM and 300 nM in a cell-free assay, respectively; shown to negatively affect the phosphorylation of Smad2.	Leukemia, 2016, 30(3):640-8 Theranostics, 2018, 8(17):4733-4749 Cell Physiol Biochem, 2018, 50(3):963-972	C, Western blot analysis of serum cultured GB2 cells treated with each 20 μm inhibitor. The representative Western blot is shown for each protein and the bar charts represent the quantified values (mean ± s.d.) of three replicates. The fold changes were normalized by the relative densities regarding α-Tubulin.
S1476	SB525334 SB525334 is a potent and selective inhibitor of TGFβ receptor I (ALK5) with IC50 of 14.3 nM in a cell-free assay, 4-fold less potent to ALK4 than ALK5 and inactive to ALK2, 3, and 6.	Nature, 2017, 551(7678):105-109 Hypertension, 2013, 62(5):951-6 Cancer Lett, 2014, 355(1):130-40	Immunoprecipitation and immunoblotting of wild-type cells treated as indicated (n = 3 experiments). i=TGFβR inhibitor:SB525334.
S8772^新	LY 3200882 LY 3200882 is a potent, highly selective inhibitor of TGF-β receptor type 1 (TGFβRI). It potently inhibits TGFβ mediated SMAD phosphorylation in vitro in tumor and immune cells and in vivo in subcutaneous tumors in a dose dependent fashion.
S2186	SB505124 SB505124 is a selective inhibitor of TGFβR for ALK4, ALK5 with IC50 of 129 nM and 47 nM in cell-free assays, respectively, also inhibits ALK7, but does not inhibit ALK1, 2, 3, or 6.	J Exp Clin Cancer Res, 2017, 36(1):54 Stem Cells, 2016, 10.1002/stem.2428 Osteoarthritis Cartilage, 2016, 24(2):345-53	(D): Fluorescence micrographs of SOX2/FOXA2 double-staining of the conditions mentioned above. The TGF-b inhibitor SB-505124 (1 mM) was additionally used together with the complete medium. Nuclei were counterstained with DAPI. Original magnification 310 or 340. Abbreviations: DAPI, 40,6-diamidino-2-phenylindole; RA, retinoic acid.
S2907	Pirfenidone Pirfenidone is an inhibitor for TGF-β production and TGF-β stimulated collagen production, reduces production of TNF-α and IL-1β, and also has anti-fibrotic and anti-inflammatory properties. Phase 3.	Am J Respir Crit Care Med, 2015, 192(4):455-67 Aging Cell, 2018, 10.1111/acel.12788 Oncogenesis, 2017, 6(9):e382	Immunofluorescence staining of myosin (red) when TGFb2 and TGFb3 were inhibited using pirfenidone. Nucleus was stained with DAPI (blue) Scale bars: 200 μm. Magnification: 100×.
S2750	GW788388 GW788388 is a potent and selective inhibitor of ALK5 with IC50 of 18 nM in a cell-free assay, also inhibits TGF-β type II receptor and activin type II receptor activities, but does not inhibit BMP type II receptor.	Int J Cancer, 2016, 138(10):2487-98 Oncogenesis, 2017, 6(9):e382 Int J Cancer, 2016, 138(10):2487-98	Combination treatment with GW788388 and IL-23 aiming to sustain Th17 cell levels increases spleen cell production of the inflammatory mediators IL-17 and TNF-a, the stimulatory mediators IL-2, IFN-g and RANTES, and the inhibitory mediator IL-10. Starting from Week 6 of 4NQO administration, when premalignant oral lesions were detectable on the tongue, mice were initiated on treatment with diluent, GW788388, IL-23 or both GW788388 and IL-23. After 2 months of these treatments, spleens were collected and cultured on anti-CD3 for 3 days. Supernatants were collected and used for measurement of the inflammatory mediators IL-17, TNF-a and IL-6 (a); stimulatory mediators IL-2, IFN-g and RANTES (b); and inhibitory mediators, TGF-b, IL-4 and IL-10 (c). =p<0.05, =p<0.01, **=p<0.001.
S2805	LY364947 LY364947 is a potent ATP-competitive inhibitor of TGFβR-I with IC50 of 59 nM in a cell-free assay, shows 7-fold selectivity over TGFβR-II.	Cancer Lett, 2017, 403:86-97 Aging (Albany NY), 2016, 8(10):2337-2354 Int J Oncol, 2017, 10.3892/ijo.2017.3903	Treatment with TGF-β-I (LY364947) and TGF-β-ab decreases the p-Smad2 level.
S7223	RepSox RepSox is a potent and selective inhibitor of the TGFβR-1/ALK5 with IC50 of 23 nM and 4 nM for ATP binding to ALK5 and ALK5 autophosphorylation in cell-free assays, respectively.	Cell Rep, 2018, 24(5):1355-1362 Protein Cell, 2017, 8(4):273-283 Dev Biol, 2017, 421(2):149-160	(C) Generation of pluripotent stem cell from Yamanaka factors-induced OG2-MEFs under treatment of diverse chemical compounds. Images of GFP+ colonies were taken on day 10 post-infection. VPA, 0.5 mmol/L. CHIR99021, 3 μmol/L. Repsox, 1 μmol/L. (D) Quantification of GFP+ colonies in (C). All figures are representative of three independent experiments (n = 3). All data are presented as mean ± SD. P < 0.05, *P < 0.01 vs. DMSO
S7507	LDN-193189 HCl LDN193189 HCl is the hydrochloride salt of LDN193189, which is a selective BMP signaling inhibitor, and inhibits the transcriptional activity of the BMP type I receptors ALK2 and ALK3 with IC50 of 5 nM and 30 nM in C2C12 cell lines, respectively, 200-fold selectivity for BMP versus TGF-β.	Proc Natl Acad Sci USA, 2013, 110(52):E5039-48 Biomed Pharmacother, 2018, 103:588-597 RSC Adv, 2018, 10.1039/C8RA00750K	LDN induces signifiant cell death. OVCA429 cells were treated with vehicle (DMSO) or experimental drugs for 6 hr to capture different stages of cell death. OVCA429 cell viability was assessed in response to drug treatment for 6 hr by staining with AO (green) and EB (orange). For clarity the different fluorescent channels to detect AO, EB, and the over-lapping images are shown for 10 mM LDN treatment.
S7359	K02288 K02288 is a potent, and selective type I BMP receptor inhibitor with IC50 of 1.1, 1.8, 6.4 nM for ALK2, ALK1 and ALK6, showing weaker inhibition on other ALKs (3, 4, 5) and ActRIIA.	Cancer Invest, 2017, 10.1080/07357907.2017.1378671	A549 cells were transfected with miR-205 inhibitor (IHT-205, 100 nM). Forty hours after transfection, the cells were seeded on transwell plates and treated with or without inhibitor K02288 (10 nM), AG1478 (1 µM), SB431542 (10 µM) for 10 hours. Migrated cells were quantified. All data are shown as mean± SD. N =3. All experiments have been repeated at least 3times independently.
S7624	SD-208 SD-208 is a selective TGF-βRI (ALK5) inhibitor with IC50 of 48 nM, >100-fold selectivity over TGF-βRII.
S7627	LDN-214117 LDN-214117 is a potent and selective BMP type I receptor kinase ALK2 inhibitor with IC50 of 24 nM.
S7959	SIS3 HCl SIS3, 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.	Cell Physiol Biochem, 2017, 44(6):2201-2211 Lab Invest, 2018, 10.1038/s41374-018-0091-y Cell Tissue Res, 2017, 369(3):603-610	Cultured cardiac fibroblasts infected with vector lentiviruses or EphrinB2 overexpressing lentiviruses were stimulated with specific antagonist against Stat3 (Stattic, 2.5μM) and/or Smad3 (SIS3, 1μM), respectively. The expression level of α-SMA was quantified via western blotting. In vitro experiments repeat 3 times, P<0.05, *P<0.01.
S7530	Vactosertib (TEW-7197) Vactosertib (TEW-7197) is a highly potent, selective, and orally bioavailable TGF-β receptor ALK4/ALK5 inhibitor with IC50 of 13 nM and 11 nM, respectively. Phase 1.	Lab Invest, 2017, 97(3):232-242 Oncol Rep, 2017, 37(3):1419-1429	Representative immunofluorescent images of HuL6 cells treated with EW-7197, TGF-β1, both, or neither for 72 h. Scale bars, 20 μm.
S7146	DMH1 DMH1 is a selective BMP receptor inhibitor with IC50 of 107.9 nM for ALK2, exhibiting no inhibition on AMPK, ALK5, KDR (VEGFR-2) or PDGFR.	Hum Gene Ther, 2018, 10.1089/hum.2017.255 Anticancer Res, 2017, 37(8):4319-4327	The combined treatment with miR-140-5p mimics and some common chemotherapeutics did not have any effect on the SK-MES1 cell line, whereas miR-140-5p and DMH1 and cisplatin decreased the proliferation of the A549 cells. Data are presented as mean±SEM of three individual experiments undertaken in triplicate. t-Test was used to assess significance with *p<0.05.
S7147	LDN-212854 LDN-212854 is a potent and selective BMP receptor inhibitor with IC50 of 1.3 nM for ALK2, about 2-, 66-, 1641-, and 7135-fold selectivity over ALK1, ALK3, ALK4, and ALK5, respectively.
S7148	ML347 ML347 is a selective BMP receptor inhibitor with IC50 of 32 nM for ALK2, >300-fold selectivity over ALK3. Also inhibits ALK1 activity with IC50 of 46 nM.	Stem Cells International, 2019, 10.1155/2019/4254759
S7658	Kartogenin Kartogenin is an activator of the smad4/smad5 pathway, and promotes the selective differentiation of multipotent mesenchymal stem cells into chondrocytes.	Genome Med, 2017, 10.1186/s13073-017-0407-3
S2308	Hesperetin Hesperetin is a bioflavonoid and, to be more specific, a flavanone.
S8318	Alantolactone Alantolactone, a naturally occurring eudesmane-type sesquiterpene lactone (SL), could induce activin/SMAD3 signaling and disrupt Cripto-1/activin receptor type II A interaction.	Onco Targets Ther, 2017, 10:1767-1776	Colon cancer cell lines (A) SW620, (B) HCT116, and (C) HT29 were treated with different concentrations (60, 12, 2.4, 0.48, and 0.098 μM) of nifuroxazide (nifu), niclosamide (nicl), cryptotanshinone (cry), and a lantolactone (ala), respectively, for 72 h. Cell proliferation in each group was detected by MTT assay. (D) HCT116, SW620, and HT29 cell lines were suppressed with niclosamide treatment at different concentrations (20, 10, 5, 2.5, and 1.25 μM) for 72 h. Subsequently, cell proliferation in each group was detected by MTT assay. The data were obtained from 3 independent experiments.

製品コード	製品説明	文献中Selleckの製品使用例	お客様のフィードバック
S1067	SB431542 SB431542 is a potent and selective inhibitor of ALK5 with IC50 of 94 nM in a cell-free assay, 100-fold more selective for ALK5 than p38 MAPK and other kinases.	Nature, 2018, 557(7704):247-251 Nature, 2015, 524(7564):234-8 Nature, 2016, 10.1038/nature17408	Phase-contrast images of RPBJ- and HNF6-deficient hepatocyte spheroids embedded in collagen gels and cultured in the presence or absence of the TGFβ inhibitor SB-431542 (SB) for the indicated number of days.
S2618	LDN-193189 LDN-193189 is a selective BMP signaling inhibitor, inhibits the transcriptional activity of the BMP type I receptors ALK2 and ALK3 with IC50 of 5 nM and 30 nM in C2C12 cells, respectively, exhibits 200-fold selectivity for BMP versus TGF-β.	Cancer Cell, 2014, 26(4):521-33 J Clin Invest, 2015, 125(2):796-808 Int J Cancer, 2014, 136(5):E455-69	LDN induces signifiant cell death. OVCA429 cells were treated with vehicle (DMSO) or experimental drugs for 6 hr to capture different stages of cell death. OVCA429 cell viability was assessed in response to drug treatment for 6 hr by staining with AO (green) and EB (orange). For clarity the different fluorescent channels to detect AO, EB, and the over-lapping images are shown for 10 mM LDN treatment.
S2230	Galunisertib (LY2157299) Galunisertib (LY2157299) is a potent TGFβ receptor I (TβRI) inhibitor with IC50 of 56 nM in a cell-free assay. Phase 2/3.	Nat Immunol, 2016, 17(8):976-84 Nat Cell Biol, 2015, 17(3):340-9 Clin Cancer Res, 2018, 10.1158/1078-0432.CCR-18-1346	Treatment of HLE and HLF cells with TGFβRI inhibitor LY2157299 led to dose-dependent loss of GLI2 levels.
S2704	LY2109761 LY2109761 is a novel selective TGF-β receptor type I/II (TβRI/II) dual inhibitor with K_i of 38 nM and 300 nM in a cell-free assay, respectively; shown to negatively affect the phosphorylation of Smad2.	Leukemia, 2016, 30(3):640-8 Theranostics, 2018, 8(17):4733-4749 Cell Physiol Biochem, 2018, 50(3):963-972	C, Western blot analysis of serum cultured GB2 cells treated with each 20 μm inhibitor. The representative Western blot is shown for each protein and the bar charts represent the quantified values (mean ± s.d.) of three replicates. The fold changes were normalized by the relative densities regarding α-Tubulin.
S1476	SB525334 SB525334 is a potent and selective inhibitor of TGFβ receptor I (ALK5) with IC50 of 14.3 nM in a cell-free assay, 4-fold less potent to ALK4 than ALK5 and inactive to ALK2, 3, and 6.	Nature, 2017, 551(7678):105-109 Hypertension, 2013, 62(5):951-6 Cancer Lett, 2014, 355(1):130-40	Immunoprecipitation and immunoblotting of wild-type cells treated as indicated (n = 3 experiments). i=TGFβR inhibitor:SB525334.
S8772^新	LY 3200882 LY 3200882 is a potent, highly selective inhibitor of TGF-β receptor type 1 (TGFβRI). It potently inhibits TGFβ mediated SMAD phosphorylation in vitro in tumor and immune cells and in vivo in subcutaneous tumors in a dose dependent fashion.
S2186	SB505124 SB505124 is a selective inhibitor of TGFβR for ALK4, ALK5 with IC50 of 129 nM and 47 nM in cell-free assays, respectively, also inhibits ALK7, but does not inhibit ALK1, 2, 3, or 6.	J Exp Clin Cancer Res, 2017, 36(1):54 Stem Cells, 2016, 10.1002/stem.2428 Osteoarthritis Cartilage, 2016, 24(2):345-53	(D): Fluorescence micrographs of SOX2/FOXA2 double-staining of the conditions mentioned above. The TGF-b inhibitor SB-505124 (1 mM) was additionally used together with the complete medium. Nuclei were counterstained with DAPI. Original magnification 310 or 340. Abbreviations: DAPI, 40,6-diamidino-2-phenylindole; RA, retinoic acid.
S2907	Pirfenidone Pirfenidone is an inhibitor for TGF-β production and TGF-β stimulated collagen production, reduces production of TNF-α and IL-1β, and also has anti-fibrotic and anti-inflammatory properties. Phase 3.	Am J Respir Crit Care Med, 2015, 192(4):455-67 Aging Cell, 2018, 10.1111/acel.12788 Oncogenesis, 2017, 6(9):e382	Immunofluorescence staining of myosin (red) when TGFb2 and TGFb3 were inhibited using pirfenidone. Nucleus was stained with DAPI (blue) Scale bars: 200 μm. Magnification: 100×.
S2750	GW788388 GW788388 is a potent and selective inhibitor of ALK5 with IC50 of 18 nM in a cell-free assay, also inhibits TGF-β type II receptor and activin type II receptor activities, but does not inhibit BMP type II receptor.	Int J Cancer, 2016, 138(10):2487-98 Oncogenesis, 2017, 6(9):e382 Int J Cancer, 2016, 138(10):2487-98	Combination treatment with GW788388 and IL-23 aiming to sustain Th17 cell levels increases spleen cell production of the inflammatory mediators IL-17 and TNF-a, the stimulatory mediators IL-2, IFN-g and RANTES, and the inhibitory mediator IL-10. Starting from Week 6 of 4NQO administration, when premalignant oral lesions were detectable on the tongue, mice were initiated on treatment with diluent, GW788388, IL-23 or both GW788388 and IL-23. After 2 months of these treatments, spleens were collected and cultured on anti-CD3 for 3 days. Supernatants were collected and used for measurement of the inflammatory mediators IL-17, TNF-a and IL-6 (a); stimulatory mediators IL-2, IFN-g and RANTES (b); and inhibitory mediators, TGF-b, IL-4 and IL-10 (c). =p<0.05, =p<0.01, **=p<0.001.
S2805	LY364947 LY364947 is a potent ATP-competitive inhibitor of TGFβR-I with IC50 of 59 nM in a cell-free assay, shows 7-fold selectivity over TGFβR-II.	Cancer Lett, 2017, 403:86-97 Aging (Albany NY), 2016, 8(10):2337-2354 Int J Oncol, 2017, 10.3892/ijo.2017.3903	Treatment with TGF-β-I (LY364947) and TGF-β-ab decreases the p-Smad2 level.
S7223	RepSox RepSox is a potent and selective inhibitor of the TGFβR-1/ALK5 with IC50 of 23 nM and 4 nM for ATP binding to ALK5 and ALK5 autophosphorylation in cell-free assays, respectively.	Cell Rep, 2018, 24(5):1355-1362 Protein Cell, 2017, 8(4):273-283 Dev Biol, 2017, 421(2):149-160	(C) Generation of pluripotent stem cell from Yamanaka factors-induced OG2-MEFs under treatment of diverse chemical compounds. Images of GFP+ colonies were taken on day 10 post-infection. VPA, 0.5 mmol/L. CHIR99021, 3 μmol/L. Repsox, 1 μmol/L. (D) Quantification of GFP+ colonies in (C). All figures are representative of three independent experiments (n = 3). All data are presented as mean ± SD. P < 0.05, *P < 0.01 vs. DMSO
S7507	LDN-193189 HCl LDN193189 HCl is the hydrochloride salt of LDN193189, which is a selective BMP signaling inhibitor, and inhibits the transcriptional activity of the BMP type I receptors ALK2 and ALK3 with IC50 of 5 nM and 30 nM in C2C12 cell lines, respectively, 200-fold selectivity for BMP versus TGF-β.	Proc Natl Acad Sci USA, 2013, 110(52):E5039-48 Biomed Pharmacother, 2018, 103:588-597 RSC Adv, 2018, 10.1039/C8RA00750K	LDN induces signifiant cell death. OVCA429 cells were treated with vehicle (DMSO) or experimental drugs for 6 hr to capture different stages of cell death. OVCA429 cell viability was assessed in response to drug treatment for 6 hr by staining with AO (green) and EB (orange). For clarity the different fluorescent channels to detect AO, EB, and the over-lapping images are shown for 10 mM LDN treatment.
S7359	K02288 K02288 is a potent, and selective type I BMP receptor inhibitor with IC50 of 1.1, 1.8, 6.4 nM for ALK2, ALK1 and ALK6, showing weaker inhibition on other ALKs (3, 4, 5) and ActRIIA.	Cancer Invest, 2017, 10.1080/07357907.2017.1378671	A549 cells were transfected with miR-205 inhibitor (IHT-205, 100 nM). Forty hours after transfection, the cells were seeded on transwell plates and treated with or without inhibitor K02288 (10 nM), AG1478 (1 µM), SB431542 (10 µM) for 10 hours. Migrated cells were quantified. All data are shown as mean± SD. N =3. All experiments have been repeated at least 3times independently.
S7624	SD-208 SD-208 is a selective TGF-βRI (ALK5) inhibitor with IC50 of 48 nM, >100-fold selectivity over TGF-βRII.
S7627	LDN-214117 LDN-214117 is a potent and selective BMP type I receptor kinase ALK2 inhibitor with IC50 of 24 nM.
S7959	SIS3 HCl SIS3, 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.	Cell Physiol Biochem, 2017, 44(6):2201-2211 Lab Invest, 2018, 10.1038/s41374-018-0091-y Cell Tissue Res, 2017, 369(3):603-610	Cultured cardiac fibroblasts infected with vector lentiviruses or EphrinB2 overexpressing lentiviruses were stimulated with specific antagonist against Stat3 (Stattic, 2.5μM) and/or Smad3 (SIS3, 1μM), respectively. The expression level of α-SMA was quantified via western blotting. In vitro experiments repeat 3 times, P<0.05, *P<0.01.
S7530	Vactosertib (TEW-7197) Vactosertib (TEW-7197) is a highly potent, selective, and orally bioavailable TGF-β receptor ALK4/ALK5 inhibitor with IC50 of 13 nM and 11 nM, respectively. Phase 1.	Lab Invest, 2017, 97(3):232-242 Oncol Rep, 2017, 37(3):1419-1429	Representative immunofluorescent images of HuL6 cells treated with EW-7197, TGF-β1, both, or neither for 72 h. Scale bars, 20 μm.
S7146	DMH1 DMH1 is a selective BMP receptor inhibitor with IC50 of 107.9 nM for ALK2, exhibiting no inhibition on AMPK, ALK5, KDR (VEGFR-2) or PDGFR.	Hum Gene Ther, 2018, 10.1089/hum.2017.255 Anticancer Res, 2017, 37(8):4319-4327	The combined treatment with miR-140-5p mimics and some common chemotherapeutics did not have any effect on the SK-MES1 cell line, whereas miR-140-5p and DMH1 and cisplatin decreased the proliferation of the A549 cells. Data are presented as mean±SEM of three individual experiments undertaken in triplicate. t-Test was used to assess significance with *p<0.05.
S7147	LDN-212854 LDN-212854 is a potent and selective BMP receptor inhibitor with IC50 of 1.3 nM for ALK2, about 2-, 66-, 1641-, and 7135-fold selectivity over ALK1, ALK3, ALK4, and ALK5, respectively.
S7148	ML347 ML347 is a selective BMP receptor inhibitor with IC50 of 32 nM for ALK2, >300-fold selectivity over ALK3. Also inhibits ALK1 activity with IC50 of 46 nM.	Stem Cells International, 2019, 10.1155/2019/4254759

製品コード	製品説明	文献中Selleckの製品使用例	お客様のフィードバック
S7658	Kartogenin Kartogenin is an activator of the smad4/smad5 pathway, and promotes the selective differentiation of multipotent mesenchymal stem cells into chondrocytes.	Genome Med, 2017, 10.1186/s13073-017-0407-3

製品コード

製品説明

文献中Selleckの製品使用例

お客様のフィードバック

S7658

Kartogenin

Kartogenin is an activator of the smad4/smad5 pathway, and promotes the selective differentiation of multipotent mesenchymal stem cells into chondrocytes.

Genome Med, 2017, 10.1186/s13073-017-0407-3

製品コード	製品説明	文献中Selleckの製品使用例	お客様のフィードバック
S2308	Hesperetin Hesperetin is a bioflavonoid and, to be more specific, a flavanone.
S8318	Alantolactone Alantolactone, a naturally occurring eudesmane-type sesquiterpene lactone (SL), could induce activin/SMAD3 signaling and disrupt Cripto-1/activin receptor type II A interaction.	Onco Targets Ther, 2017, 10:1767-1776	Colon cancer cell lines (A) SW620, (B) HCT116, and (C) HT29 were treated with different concentrations (60, 12, 2.4, 0.48, and 0.098 μM) of nifuroxazide (nifu), niclosamide (nicl), cryptotanshinone (cry), and a lantolactone (ala), respectively, for 72 h. Cell proliferation in each group was detected by MTT assay. (D) HCT116, SW620, and HT29 cell lines were suppressed with niclosamide treatment at different concentrations (20, 10, 5, 2.5, and 1.25 μM) for 72 h. Subsequently, cell proliferation in each group was detected by MTT assay. The data were obtained from 3 independent experiments.

製品コード

製品説明

文献中Selleckの製品使用例

お客様のフィードバック

S2308

Hesperetin

Hesperetin is a bioflavonoid and, to be more specific, a flavanone.

S8318

Alantolactone

Alantolactone, a naturally occurring eudesmane-type sesquiterpene lactone (SL), could induce activin/SMAD3 signaling and disrupt Cripto-1/activin receptor type II A interaction.

Onco Targets Ther, 2017, 10:1767-1776