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.	Cell Stem Cell, 2019, 24(3):447-461.e8. Immunity, 2019, 50(1):121-136.e5 Nat Commun, 2019, 10(1):928	Long-term response of SB431542 and SB203580 release from scaffold implants. Histological results of H&E staining showing the capsule thickness of the various treatments at 14 days. The scale bar shows 100 uM and is applicable to all images in the panel. In each bar graph the tissue and cellular response to SB431542 were found to be significant from the control. For each treatment group six animals were tested. Statistics are performed by ANOVA with Bonferroni comparisons and taken to be significant at ∗∗P < 0.01.
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.	Nat Commun, 2019, 10(1):928 J Neurosci, 2019, 39(12):2184-2194 Glia, 2019, 67(1):146-159	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.	Clin Cancer Res, 2019, 25(12):3617-3629 Cell Rep, 2019, 26(10):2667-2680 Cancers (Basel), 2019, 11(3)	Cells were treated in both formats with 10 uM of SB525334 (TGFβR1), SJN 2511 (TGFβR1), LY2157299 (TGFβR2, TGFβR1), Dorsomorphin (AMPK, ALK2, ALK3, ALK6), DMH-1 (ALK2), or GW5074 (c-raf), or 50 ng/ml of TGF-β. Microtissue or tissue-culture well fluorescence for each condition are shown after 3 days of culture for 393T5 cells, which proliferate slower in control conditions, so that the two cell lines undergo the same number of population doublings during each assay.
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.	J Pathol, 2019, 10.1002/path.5278 Ecotoxicol Environ Saf, 2019, 169:266-272 Theranostics, 2018, 8(17):4733-4749	The inhibition of TGF-β1 signaling pathways suppressed EBV-mediated EMT, and prevented the activation of Syk and Src signaling. The EBV-infected HCECs were treated with 100 nM of the dual TGF-β receptor I and II kinase inhibitor, LY2109761, for 48 hours. The EBV-infected HCECs were cultured with anti-TGF-β1 neutralizing antibody (5 ug/mL) or mouse IgG1 antibody (5 ug/mL) for 48 hours. Photographs were taken at x100 magnification by a digital camera.
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.	J Bone Miner Res, 2019, 10.1002/jbmr.3716 Free Radic Biol Med, 2019, 134:617-629 J Immunol, 2019, 202(4):1287-1300	LS 174T and SW480 cells were treated with SB525334 (1 umol/L) for 12 hours. HMGA2 expression was assessed by immunoblotting. Each experiment was repeated 3 times. Bars, SD; , P < 0.05; *, P < 0.01.
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.	Biochem Pharmacol, 2019, 168:1-13 J Exp Clin Cancer Res, 2018, 37(1):39 J Exp Clin Cancer Res, 2017, 36(1):54	(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.	Front Neurosci, 2019, 13:636 Eur Respir J, 2018, 52(3) Aging Cell, 2018, 10.1111/acel.12788	Ex vivo tissue spotting experiment of pirfenidone dilutions and MalDI imagingn approach of in vivo administered pirfenidone measured with MalDI-TOF mass spectrometer. ex vivo dilution series of pirfenidone (m/z 186.2?.1 Da) covered with CHCa matrix. In vivo treated liver cryosections measured by MalDI-TOF imaging using CHCa. Size bar corresponds to 2 mm.
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 Cardiol, 2018, 271:219-227 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.	Cells, 2019, 8(4) Cancer Lett, 2017, 403:86-97 Cell Chem Biol, 2017, 24(7):858-869	The cytoplasmic and nuclear proteins were separated and the protein expression levels were determined by performing western blotting. LY364947 (1 uM), which is a potent ATP-competitive inhibitor of TGF-βRI, was used as the positive control. GAPDH and PARP were used as cytosolic and nuclear markers, respectively.
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.	Toxicol Appl Pharmacol, 2019, 379:114685 Biomed Pharmacother, 2018, 103:588-597 Am J Transl Res, 2018, 10(10):3150-3161	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.	Int J Biol Sci, 2019, 15(2):430-440 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.	Immunity, 2019, 50(1):121-136.e5 Front Neurosci, 2019, 13:636 Respir Res, 2019, 20(1):164	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.	Exp Cell Res, 2018, 372(2):141-149 ACS Appl Mater Interfaces, 2017, 9(20):16803-16812 Lab Invest, 2017, 97(3):232-242	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 Mol Cancer, 2016, 15:27	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.	Cell Stem Cell, 2019, 24(3):447-461.e8. Immunity, 2019, 50(1):121-136.e5 Nat Commun, 2019, 10(1):928	Long-term response of SB431542 and SB203580 release from scaffold implants. Histological results of H&E staining showing the capsule thickness of the various treatments at 14 days. The scale bar shows 100 uM and is applicable to all images in the panel. In each bar graph the tissue and cellular response to SB431542 were found to be significant from the control. For each treatment group six animals were tested. Statistics are performed by ANOVA with Bonferroni comparisons and taken to be significant at ∗∗P < 0.01.
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.	Nat Commun, 2019, 10(1):928 J Neurosci, 2019, 39(12):2184-2194 Glia, 2019, 67(1):146-159	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.	Clin Cancer Res, 2019, 25(12):3617-3629 Cell Rep, 2019, 26(10):2667-2680 Cancers (Basel), 2019, 11(3)	Cells were treated in both formats with 10 uM of SB525334 (TGFβR1), SJN 2511 (TGFβR1), LY2157299 (TGFβR2, TGFβR1), Dorsomorphin (AMPK, ALK2, ALK3, ALK6), DMH-1 (ALK2), or GW5074 (c-raf), or 50 ng/ml of TGF-β. Microtissue or tissue-culture well fluorescence for each condition are shown after 3 days of culture for 393T5 cells, which proliferate slower in control conditions, so that the two cell lines undergo the same number of population doublings during each assay.
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.	J Pathol, 2019, 10.1002/path.5278 Ecotoxicol Environ Saf, 2019, 169:266-272 Theranostics, 2018, 8(17):4733-4749	The inhibition of TGF-β1 signaling pathways suppressed EBV-mediated EMT, and prevented the activation of Syk and Src signaling. The EBV-infected HCECs were treated with 100 nM of the dual TGF-β receptor I and II kinase inhibitor, LY2109761, for 48 hours. The EBV-infected HCECs were cultured with anti-TGF-β1 neutralizing antibody (5 ug/mL) or mouse IgG1 antibody (5 ug/mL) for 48 hours. Photographs were taken at x100 magnification by a digital camera.
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.	J Bone Miner Res, 2019, 10.1002/jbmr.3716 Free Radic Biol Med, 2019, 134:617-629 J Immunol, 2019, 202(4):1287-1300	LS 174T and SW480 cells were treated with SB525334 (1 umol/L) for 12 hours. HMGA2 expression was assessed by immunoblotting. Each experiment was repeated 3 times. Bars, SD; , P < 0.05; *, P < 0.01.
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.	Biochem Pharmacol, 2019, 168:1-13 J Exp Clin Cancer Res, 2018, 37(1):39 J Exp Clin Cancer Res, 2017, 36(1):54	(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.	Front Neurosci, 2019, 13:636 Eur Respir J, 2018, 52(3) Aging Cell, 2018, 10.1111/acel.12788	Ex vivo tissue spotting experiment of pirfenidone dilutions and MalDI imagingn approach of in vivo administered pirfenidone measured with MalDI-TOF mass spectrometer. ex vivo dilution series of pirfenidone (m/z 186.2?.1 Da) covered with CHCa matrix. In vivo treated liver cryosections measured by MalDI-TOF imaging using CHCa. Size bar corresponds to 2 mm.
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 Cardiol, 2018, 271:219-227 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.	Cells, 2019, 8(4) Cancer Lett, 2017, 403:86-97 Cell Chem Biol, 2017, 24(7):858-869	The cytoplasmic and nuclear proteins were separated and the protein expression levels were determined by performing western blotting. LY364947 (1 uM), which is a potent ATP-competitive inhibitor of TGF-βRI, was used as the positive control. GAPDH and PARP were used as cytosolic and nuclear markers, respectively.
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.	Toxicol Appl Pharmacol, 2019, 379:114685 Biomed Pharmacother, 2018, 103:588-597 Am J Transl Res, 2018, 10(10):3150-3161	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.	Int J Biol Sci, 2019, 15(2):430-440 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.	Immunity, 2019, 50(1):121-136.e5 Front Neurosci, 2019, 13:636 Respir Res, 2019, 20(1):164	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.	Exp Cell Res, 2018, 372(2):141-149 ACS Appl Mater Interfaces, 2017, 9(20):16803-16812 Lab Invest, 2017, 97(3):232-242	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 Mol Cancer, 2016, 15:27	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