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
S7710	R-268712	<1 mg/mL	73 mg/mL	18 mg/mL
S2186	SB505124	<1 mg/mL	67 mg/mL	67 mg/mL
S7306	Dorsomorphin (Compound C) 2HCl	94 mg/mL	<1 mg/mL	<1 mg/mL
S2907	Pirfenidone (S-7701)	<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 (E-616452)	<1 mg/mL	57 mg/mL	'''<1 mg/mL
S7507	LDN-193189 2HCl	52 mg/mL	<1 mg/mL	'''<1 mg/mL
S1576	Sulfasalazine (NSC 667219)	<1 mg/mL	80 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
S7692	A-83-01	˂1 mg/mL	23 mg/mL	˂1 mg/mL
S0752	AUDA	<1 mg/mL	78 mg/mL	6 mg/mL
S8700	TP0427736 HCl	<1 mg/mL	67 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
S2234	BIBF-0775	<1 mg/mL	14 mg/mL	2 mg/mL
S8772	LY 3200882	<1 mg/mL	87 mg/mL	<1 mg/mL
S3552	SIS3	<1 mg/mL	91 mg/mL	91 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
S8144	Halofuginone	<1 mg/mL	20 mg/mL	'<1 mg/mL
S6713	ITD-1	<1 mg/mL	83 mg/mL	<1 mg/mL
S7840	Dorsomorphin (Compound C)	<1 mg/mL	1 mg/mL	'''''2 mg/mL
S6807	TA-02	<1 mg/mL	67 mg/mL	3 mg/mL
S5183	PD 169316	<1 mg/mL	14 mg/mL	'<1 mg/mL
S3223	L-Quebrachitol	-1 mg/mL	100 mg/mL	-1 mg/mL
S7914	Isoxazole 9 (ISX-9)	<1 mg/mL	46 mg/mL	13 mg/mL
S7658	Kartogenin	<1 mg/mL	63 mg/mL	'5 mg/mL
S0153	SJ000291942	<1 mg/mL	64 mg/mL	12 mg/mL
S0523	SB 4	˂1 mg/mL	64 mg/mL	'''21 mg/mL
S6654	SRI-011381	<1 mg/mL	66 mg/mL	66 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 (41) TGF-beta/Smad阻害剤(33) TGF-beta/Smad活性剤(4) TGF-beta/Smad作動薬(2) TGF-beta/Smadモジュレータ(2)

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, 2022, 605(7909):325-331 Adv Mater, 2022, e2106829 Adv Sci (Weinh), 2022, e2103939	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 (DM3189) is a selective BMP signaling inhibitor, inhibits the ALK1, ALK2, ALK3 and ALK6 with IC50s of 0.8 nM, 0.8 nM, 5.3 nM and 16.7 nM in the kinase assay, respectively. LDN-193189 inhibits the transcriptional activity of the BMP type I receptors ALK2 and ALK3 with IC50s of 5 nM and 30 nM in C2C12 cells, respectively, exhibits 200-fold selectivity for BMP versus TGF-β. For animal testing, the water-soluble S7507 LDN-193189 2HCl is recommended.	Adv Mater, 2022, e2106829 Adv Sci (Weinh), 2022, e2106075 Stem Cell Res Ther, 2022, 13(1):120	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.	Cancer Cell, 2022, S1535-6108(21)00662-0 Int J Biol Sci, 2022, 18(5):1912-1932 Arch Toxicol, 2022, 10.1007/s00204-022-03265-7	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. LY2109761 blocks autophagy and induces apoptosis.	Nat Immunol, 2022, 23(2):237-250 Nat Commun, 2022, 13(1):1017 Cell Mol Life Sci, 2022, 79(3):153	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.	Sci Immunol, 2022, 7(71):eabl6543 Cancer Res, 2022, canres.3910.2021 Glia, 2022, 10.1002/glia.24218	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.
S7710^新	R-268712 R-268712 is a potent and selective inhibitor of ALK5 with an IC50 of 2.5 nM.
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.	Blood Cancer J, 2022, 12(3):39 Sci Rep, 2022, 12(1):7 Biomaterials, 2021, 274:120856	(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.
S7306	Dorsomorphin (Compound C) 2HCl Dorsomorphin 2HCl (BML-275, Compound C) is a potent, reversible, selective AMPK inhibitor with K_i of 109 nM in cell-free assays, exhibiting no significant inhibition of several structurally related kinases including ZAPK, SYK, PKCθ, PKA, and JAK3. Also inhibits type Ⅰ BMP receptor activity. Dorsomorphin induces autophagy in cancer cell line.	Signal Transduct Target Ther, 2022, 7(1):66 Redox Biol, 2022, 52:102288 Brain Behav Immun, 2022, S0889-1591(22)00041-1	AMPK inhibition by compound C(Dorsomorphin) inhibited autophagy activation and neuroprotection induced by IPC in PC12 cells. (A) Compound C (Comp C) abolished IPC induced neuroprotection in PC12 cells. Cells were incubated with compound C 5 μM 60 min before the onset of IPC. Twelve hours after IPC, the cells were subjected to OGD for 10 h and cell viability was examined with CCK-8 kit. (B) Compound C reduced LC3II/LC3I ratio. The cells were incubated with compound C 5 μM 60 min before the onset of IPC. Then the cells were harvested 12 h after IPC and subjected to Western blot analysis. Bar represents mean ± SD, n = 3. P < 0.05, **P < 0.001 compared with the control group; $$$ P < 0.001 compared with the OGD group; %%% P < 0.001 compared with the IPC + OGD group; # P < 0.05 compared with the IPC group.
S2907	Pirfenidone (S-7701) Pirfenidone (S-7701, AMR-69) 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. Pirfenidone attenuates chemokine (CC motif) ligand-2 (CCL2) and CCL12 production with anti-fibrotic activity. Phase 3.	Cancer Biol Ther, 2022, 23(1):150-162 Sci Rep, 2022, 12(1):7 Integr Biol (Camb), 2022, 14(1):1-12	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.	Sci Rep, 2022, 12(1):7 EMBO Mol Med, 2021, 13(6):e13270 iScience, 2021, 24(10):103193	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 (HTS 466284) 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.	Cell Rep, 2022, 38(5):110329 Front Immunol, 2022, 13:853894 Aging Dis, 2022, 13(1):313-328	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 (E-616452) RepSox (E-616452, SJN 2511, ALK5 Inhibitor II) 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.	Sci Adv, 2022, 8(8):eabj6621 Int J Mol Sci, 2022, 23(8)4213 Biomater Sci, 2022, 10.1039/d1bm01287h	(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 2HCl LDN-193189 (DM3189) 2HCl is a selective BMP signaling inhibitor, inhibits the ALK1, ALK2, ALK3 and ALK6 with IC50s of 0.8 nM, 0.8 nM, 5.3 nM and 16.7 nM in the kinase assay, respectively. LDN-193189 inhibits the transcriptional activity of the BMP type I receptors ALK2 and ALK3 with IC50s of 5 nM and 30 nM in C2C12 cells, respectively, exhibits 200-fold selectivity for BMP versus TGF-β.	Adv Mater, 2022, e2106829 Adv Sci (Weinh), 2022, e2106075 Redox Biol, 2022, 50:102248	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.
S1576	Sulfasalazine (NSC 667219) Sulfasalazine (NSC 667219, Azulfidine, Salazopyrin, Sulphasalazine) is a sulfa derivative of mesalazine, used as an anti-inflammatory agent to treat bowel disease and rheumatoid arthritis. Sulfasalazine is a potent and specific inhibitor of nuclear factor kappa B (NF-κB), TGF-β and COX-2. Sulfasalazine induces ferroptosis, apoptosis and autophagy.	Cell Mol Life Sci, 2022, 79(5):228 Front Bioeng Biotechnol, 2022, 10:855755 Cell Metab, 2021, S1550-4131(21)00233-3
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.	Sci Rep, 2022, 12(1):7 Nat Commun, 2021, 12(1):6177 Mol Oncol, 2021, 10.1002/1878-0261.12963	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.	Acta Biomater, 2022, S1742-7061(22)00004-6 Cardiovasc Res, 2021, cvab205 J Clin Invest, 2020, 130(3):1377-1391
S7692	A-83-01 A-83-01 is a potent inhibitor of TGF-β type I receptor (ALK5-TD) with IC50 of 12 nM. A-83-01 also inhibits the transcription induced by activin/nodal type I receptor (ALK4-TD) and nodal type I receptor (ALK7-TD) with IC50 of 45 nM and 7.5 nM, respectively.Solutions of Acetylcysteine are best fresh-prepared.	Sci Adv, 2021, 7(51):eabh0562 Sci Adv, 2021, 7(33)eabf4416 Biomaterials, 2021, 280:121266
S0752	AUDA AUDA (compound 43) is a potent inhibitor of soluble epoxide hydrolase (sEH) with IC50 of 18 nM and 69 nM for the mouse sEH and human sEH, respectively. AUDA has anti-inflammatory activity that reduces the protein expression of MMP-9, IL-1β, TNF-α and TGF-β. AUDA downregulates Smad3 and p38 signaling pathways.
S8700	TP0427736 HCl TP0427736 is a potent inhibitor of ALK5 kinase activity with an IC50 of 2.72 nM and this effect is 300-fold higher than the inhibitory effect on ALK3 (IC50 = 836 nM for ALK3). It also inhibits Smad2/3 phosphorylation in A549 cells induced by TGF-β1 with an IC50 value of 8.68 nM.	Commun Biol, 2021, 4(1):318 Stem Cell Res Ther, 2020, 11(1):365 Mol Med Rep, 2019, 10.3892/mmr.2019.10655
S7627	LDN-214117 LDN-214117 is a potent and selective BMP type I receptor kinase ALK2 inhibitor with IC50 of 24 nM.	FASEB J, 2021, 35(3):e21263 Stem Cells Int, 2019, 2019:5026793
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.	Nat Immunol, 2022, 23(2):237-250 J Biol Chem, 2022, 298(4):101748 Biol Trace Elem Res, 2022, 10.1007/s12011-022-03169-8	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.
S2234	BIBF-0775 BIBF-0775 is a selective inhibitor of transforming growth factor β Receptor I (TGFβRI,Alk5) with an IC50 of 34 nM.
S8772	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.	J Inflamm Res, 2021, 14:2897-2911 Pediatr Rheumatol Online J, 2021, 19(1):72 Br J Cancer, 2020, 10.1038/s41416-020-01040-y
S3552	SIS3 SIS3 is a cell-permeable inhibitor of Smad3 that selectively inhibits TGF-β1-dependent Smad3 phosphorylation and Smad3-mediated cellular signaling. SIS3 reduces TGF-β1-induced type 1 procollagen expression and myofibroblast differentiation in normal dermal fibroblasts as well as scleroderma fibroblasts.	Mol Cancer, 2022, 21(1):77 Biol Trace Elem Res, 2022, 10.1007/s12011-022-03169-8 Front Cell Dev Biol, 2021, 9:632372
S7530	Vactosertib (TEW-7197) Vactosertib (TEW-7197, EW-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.	Cancer Cell, 2021, S1535-6108(21)00492-X Cell Rep, 2021, 34(12):108882 Biomater Sci, 2021, 10.1039/d1bm01699g	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. DMH1 inhibits autophagy.	Atherosclerosis, 2022, 351:9-17 Nat Commun, 2021, 12(1):6374 Proc Natl Acad Sci U S A, 2021, 118(29)e2101783118	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 ofthe 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 (BMP Inhibitor III) 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.	Nat Commun, 2021, 12(1):6177 Mol Oncol, 2021, 10.1002/1878-0261.12963 Mol Med Rep, 2020, 21(1):61-68
S7148	ML347 ML347 (LDN-193719) 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.	Biomolecules, 2020, 10(4)E519 Biomolecules, 2020, 29;10(4) pii: E519 eNeuro, 2020, 7(5):ENEURO.0104-20.2020
S8144	Halofuginone Halofuginone (RU-19110) is the competitively inhibitor of prolyl-tRNA synthetase with Ki of 18.3 nM.It could also down-regulate Smad3 and blocked TGF-β signaling at 10 ng/ml in mammal.	Gastric Cancer, 2021, 10.1007/s10120-021-01259-5 Research Square, 2021, 10.21203/rs.3.rs-738132/v1 Sci Rep, 2020, 10(1):19723
S6713	ITD-1 ITD-1 is a potent TGF-β inhibitor. It does not block the kinase activity of either type I (TGFBR1) or type II (TGFBR2) TGFβ receptors but potently blocks phosphorylation of the effector SMAD2/3 proteins induced by TGFβ2, and only minimally in response to Activin A.	Nat Commun, 2022, 13(1):438 Cell Death Dis, 2022, 13(4):339 J Exp Clin Cancer Res, 2021, 40(1):62
S7840	Dorsomorphin (Compound C) Dorsomorphin (Compound C, BML-275) is a potent, reversible, selective AMPK inhibitor with K_i of 109 nM in cell-free assays, exhibiting no significant inhibition of several structurally related kinases including ZAPK, SYK, PKCθ, PKA, and JAK3. Dorsomorphin selectively inhibits the BMP type I receptors ALK2, ALK3 and ALK6. Dorsomorphin is used in promoting specific cell differentiation and inducing cancer cell line autophagy. For animal testing, the water-soluble S7306 Dorsomorphin (Compound C) 2HCl is recommended.	Signal Transduct Target Ther, 2022, 7(1):66 Adv Sci (Weinh), 2022, e2105208 Brain Behav Immun, 2022, S0889-1591(22)00041-1	FGF21 activates myogenic and aerobic myofiber-associated genes expression via AMPK pathway. The activator (acadesine) or inhibitor (dorsomorphin) of AMPK pathway were used to treat the pcDNA3.1-21 or control transfected C2C12 myoblasts. For this experiment, four groups were set up: FGF21-ACA (pcDNA3.1-21‡acadesine), Control-ACA (control‡acadesine), FGF21-DOR (pcDNA3.1-21‡dorsomorphin), and Control-DOR(control‡dorsomorphin). The qRT-PCR was performed to detect the genes expression of FGF21 (A), AMPK (B), Sirt 1, Myoglobin(C), Desmin (D), MEF2c (E), a-actin (F). (G) The C2C12 myoblasts were transiently transfected with pCDNA3.1-21 or pCDNA3.1, Western blot showed FGF21 activated AMPK signal via FGF21-Sirt1-AMPK. For the phosphorylated AMPK (right), the intensity of band was normalized total AMPK, and then normalized by control. (H and I) FGF21, as well as AMPK activator acadesine (ACA), increased phosphorylation of AMPM, and myogenic genes expression, especially MyHC I, which was activated by ACA (FGF21‡ACA) and suppressed by AMPK inhibitor DOR(FGF21‡DOR). The data are presented as mean±SD (P<0.05, *P<0.01, and P<0.001), n=ˆ3.
S6807	TA-02 TA-02 is a p38 MAPK inhibitor with IC50 of 20 nM. TA-02 especially inhibits TGFBR-2.
S5183	PD 169316 PD 169316 is a potent, selective and cell-permeable p38 MAP kinase inhibitor with IC50 of 89 nM. PD169316 abrogates signaling initiated by both TGFbeta and Activin A. PD169316 shows antiviral activity against Enterovirus71.	PLoS One, 2021, 16(5):e0252541
S3223	L-Quebrachitol L-Quebrachitol (L-QCT), a natural product isolated from many plants, promotes proliferation and cell DNA synthesis. L-Quebrachitol upregulates bone morphogenetic protein-2 (BMP-2) and runt-related transcription factor-2 (Runx2) and regulatory genes associated with mitogen-activated protein kinase (MAPK) and Wnt/β-catenin signaling pathway, while down-regulating the receptor activator of the nuclear factor-κB(NF-κB) ligand (RANKL) mRNA level.
S7914	Isoxazole 9 (ISX-9) Isoxazole 9 (Isx-9) is a synthetic promotor of adult neurogenesis by triggering neuronal differentiation of adult neural stem/precursor cells (NSPCs). Isoxazole 9 (Isx-9) activates multiple pathways including TGF-β induced epithelial–mesenchymal transition (EMT) signaling, canonical and non-canonical Wnt signaling at different stages of cardiac differentiation.	Front Cell Dev Biol, 2021, 9:728352
S7658	Kartogenin Kartogenin (KGN) is an activator of the smad4/smad5 pathway, and promotes the selective differentiation of multipotent mesenchymal stem cells into chondrocytes.	Acta Biomater, 2021, S1742-7061(21)00015-5 Anticancer Res, 2021, 41(10):4753-4759 Front Chem, 2019, 7:677
S0153	SJ000291942 SJ000291942 is a canonical bone morphogenetic proteins (BMP) signaling pathway activator.
S0523	SB 4 SB 4 is a potent and selective agonist of bone morphogenetic protein 4 (BMP4) signaling with EC50 of 74 nM. SB 4 enhances canonical BMP signaling and activates SMAD-1/5/9 phosphorylation.
S6654	SRI-011381 SRI-011381 is a novel agonist of the TGF-beta signaling pathway for treatment of Alzheimer's disease.	Dis Model Mech, 2022, dmm.046979 Front Cell Dev Biol, 2021, 9:648201 Eur J Pharmacol, 2021, 912:174587
S2308	Hesperetin Hesperetin is a bioflavonoid and, to be more specific, a flavanone.	Sci Rep, 2022, 12(1):7 Front Pharmacol, 2021, 12:735087 Carcinogenesis, 2020, 41(7):993-1004
S8318	Alantolactone Alantolactone (helenin, helenine, Eupatal), a naturally occurring eudesmane-type sesquiterpene lactone (SL), could induce activin/SMAD3 signaling and disrupt Cripto-1/activin receptor type II A interaction.	Nat Commun, 2022, 13(1):107 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, 2022, 605(7909):325-331 Adv Mater, 2022, e2106829 Adv Sci (Weinh), 2022, e2103939	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 (DM3189) is a selective BMP signaling inhibitor, inhibits the ALK1, ALK2, ALK3 and ALK6 with IC50s of 0.8 nM, 0.8 nM, 5.3 nM and 16.7 nM in the kinase assay, respectively. LDN-193189 inhibits the transcriptional activity of the BMP type I receptors ALK2 and ALK3 with IC50s of 5 nM and 30 nM in C2C12 cells, respectively, exhibits 200-fold selectivity for BMP versus TGF-β. For animal testing, the water-soluble S7507 LDN-193189 2HCl is recommended.	Adv Mater, 2022, e2106829 Adv Sci (Weinh), 2022, e2106075 Stem Cell Res Ther, 2022, 13(1):120	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.	Cancer Cell, 2022, S1535-6108(21)00662-0 Int J Biol Sci, 2022, 18(5):1912-1932 Arch Toxicol, 2022, 10.1007/s00204-022-03265-7	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. LY2109761 blocks autophagy and induces apoptosis.	Nat Immunol, 2022, 23(2):237-250 Nat Commun, 2022, 13(1):1017 Cell Mol Life Sci, 2022, 79(3):153	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.	Sci Immunol, 2022, 7(71):eabl6543 Cancer Res, 2022, canres.3910.2021 Glia, 2022, 10.1002/glia.24218	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.
S7710^新	R-268712 R-268712 is a potent and selective inhibitor of ALK5 with an IC50 of 2.5 nM.
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.	Blood Cancer J, 2022, 12(3):39 Sci Rep, 2022, 12(1):7 Biomaterials, 2021, 274:120856	(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.
S7306	Dorsomorphin (Compound C) 2HCl Dorsomorphin 2HCl (BML-275, Compound C) is a potent, reversible, selective AMPK inhibitor with K_i of 109 nM in cell-free assays, exhibiting no significant inhibition of several structurally related kinases including ZAPK, SYK, PKCθ, PKA, and JAK3. Also inhibits type Ⅰ BMP receptor activity. Dorsomorphin induces autophagy in cancer cell line.	Signal Transduct Target Ther, 2022, 7(1):66 Redox Biol, 2022, 52:102288 Brain Behav Immun, 2022, S0889-1591(22)00041-1	AMPK inhibition by compound C(Dorsomorphin) inhibited autophagy activation and neuroprotection induced by IPC in PC12 cells. (A) Compound C (Comp C) abolished IPC induced neuroprotection in PC12 cells. Cells were incubated with compound C 5 μM 60 min before the onset of IPC. Twelve hours after IPC, the cells were subjected to OGD for 10 h and cell viability was examined with CCK-8 kit. (B) Compound C reduced LC3II/LC3I ratio. The cells were incubated with compound C 5 μM 60 min before the onset of IPC. Then the cells were harvested 12 h after IPC and subjected to Western blot analysis. Bar represents mean ± SD, n = 3. P < 0.05, **P < 0.001 compared with the control group; $$$ P < 0.001 compared with the OGD group; %%% P < 0.001 compared with the IPC + OGD group; # P < 0.05 compared with the IPC group.
S2907	Pirfenidone (S-7701) Pirfenidone (S-7701, AMR-69) 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. Pirfenidone attenuates chemokine (CC motif) ligand-2 (CCL2) and CCL12 production with anti-fibrotic activity. Phase 3.	Cancer Biol Ther, 2022, 23(1):150-162 Sci Rep, 2022, 12(1):7 Integr Biol (Camb), 2022, 14(1):1-12	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.	Sci Rep, 2022, 12(1):7 EMBO Mol Med, 2021, 13(6):e13270 iScience, 2021, 24(10):103193	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 (HTS 466284) 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.	Cell Rep, 2022, 38(5):110329 Front Immunol, 2022, 13:853894 Aging Dis, 2022, 13(1):313-328	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 (E-616452) RepSox (E-616452, SJN 2511, ALK5 Inhibitor II) 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.	Sci Adv, 2022, 8(8):eabj6621 Int J Mol Sci, 2022, 23(8)4213 Biomater Sci, 2022, 10.1039/d1bm01287h	(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 2HCl LDN-193189 (DM3189) 2HCl is a selective BMP signaling inhibitor, inhibits the ALK1, ALK2, ALK3 and ALK6 with IC50s of 0.8 nM, 0.8 nM, 5.3 nM and 16.7 nM in the kinase assay, respectively. LDN-193189 inhibits the transcriptional activity of the BMP type I receptors ALK2 and ALK3 with IC50s of 5 nM and 30 nM in C2C12 cells, respectively, exhibits 200-fold selectivity for BMP versus TGF-β.	Adv Mater, 2022, e2106829 Adv Sci (Weinh), 2022, e2106075 Redox Biol, 2022, 50:102248	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.
S1576	Sulfasalazine (NSC 667219) Sulfasalazine (NSC 667219, Azulfidine, Salazopyrin, Sulphasalazine) is a sulfa derivative of mesalazine, used as an anti-inflammatory agent to treat bowel disease and rheumatoid arthritis. Sulfasalazine is a potent and specific inhibitor of nuclear factor kappa B (NF-κB), TGF-β and COX-2. Sulfasalazine induces ferroptosis, apoptosis and autophagy.	Cell Mol Life Sci, 2022, 79(5):228 Front Bioeng Biotechnol, 2022, 10:855755 Cell Metab, 2021, S1550-4131(21)00233-3
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.	Sci Rep, 2022, 12(1):7 Nat Commun, 2021, 12(1):6177 Mol Oncol, 2021, 10.1002/1878-0261.12963	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.	Acta Biomater, 2022, S1742-7061(22)00004-6 Cardiovasc Res, 2021, cvab205 J Clin Invest, 2020, 130(3):1377-1391
S7692	A-83-01 A-83-01 is a potent inhibitor of TGF-β type I receptor (ALK5-TD) with IC50 of 12 nM. A-83-01 also inhibits the transcription induced by activin/nodal type I receptor (ALK4-TD) and nodal type I receptor (ALK7-TD) with IC50 of 45 nM and 7.5 nM, respectively.Solutions of Acetylcysteine are best fresh-prepared.	Sci Adv, 2021, 7(51):eabh0562 Sci Adv, 2021, 7(33)eabf4416 Biomaterials, 2021, 280:121266
S0752	AUDA AUDA (compound 43) is a potent inhibitor of soluble epoxide hydrolase (sEH) with IC50 of 18 nM and 69 nM for the mouse sEH and human sEH, respectively. AUDA has anti-inflammatory activity that reduces the protein expression of MMP-9, IL-1β, TNF-α and TGF-β. AUDA downregulates Smad3 and p38 signaling pathways.
S8700	TP0427736 HCl TP0427736 is a potent inhibitor of ALK5 kinase activity with an IC50 of 2.72 nM and this effect is 300-fold higher than the inhibitory effect on ALK3 (IC50 = 836 nM for ALK3). It also inhibits Smad2/3 phosphorylation in A549 cells induced by TGF-β1 with an IC50 value of 8.68 nM.	Commun Biol, 2021, 4(1):318 Stem Cell Res Ther, 2020, 11(1):365 Mol Med Rep, 2019, 10.3892/mmr.2019.10655
S7627	LDN-214117 LDN-214117 is a potent and selective BMP type I receptor kinase ALK2 inhibitor with IC50 of 24 nM.	FASEB J, 2021, 35(3):e21263 Stem Cells Int, 2019, 2019:5026793
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.	Nat Immunol, 2022, 23(2):237-250 J Biol Chem, 2022, 298(4):101748 Biol Trace Elem Res, 2022, 10.1007/s12011-022-03169-8	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.
S2234	BIBF-0775 BIBF-0775 is a selective inhibitor of transforming growth factor β Receptor I (TGFβRI,Alk5) with an IC50 of 34 nM.
S8772	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.	J Inflamm Res, 2021, 14:2897-2911 Pediatr Rheumatol Online J, 2021, 19(1):72 Br J Cancer, 2020, 10.1038/s41416-020-01040-y
S3552	SIS3 SIS3 is a cell-permeable inhibitor of Smad3 that selectively inhibits TGF-β1-dependent Smad3 phosphorylation and Smad3-mediated cellular signaling. SIS3 reduces TGF-β1-induced type 1 procollagen expression and myofibroblast differentiation in normal dermal fibroblasts as well as scleroderma fibroblasts.	Mol Cancer, 2022, 21(1):77 Biol Trace Elem Res, 2022, 10.1007/s12011-022-03169-8 Front Cell Dev Biol, 2021, 9:632372
S7530	Vactosertib (TEW-7197) Vactosertib (TEW-7197, EW-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.	Cancer Cell, 2021, S1535-6108(21)00492-X Cell Rep, 2021, 34(12):108882 Biomater Sci, 2021, 10.1039/d1bm01699g	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. DMH1 inhibits autophagy.	Atherosclerosis, 2022, 351:9-17 Nat Commun, 2021, 12(1):6374 Proc Natl Acad Sci U S A, 2021, 118(29)e2101783118	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 ofthe 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 (BMP Inhibitor III) 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.	Nat Commun, 2021, 12(1):6177 Mol Oncol, 2021, 10.1002/1878-0261.12963 Mol Med Rep, 2020, 21(1):61-68
S7148	ML347 ML347 (LDN-193719) 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.	Biomolecules, 2020, 10(4)E519 Biomolecules, 2020, 29;10(4) pii: E519 eNeuro, 2020, 7(5):ENEURO.0104-20.2020
S8144	Halofuginone Halofuginone (RU-19110) is the competitively inhibitor of prolyl-tRNA synthetase with Ki of 18.3 nM.It could also down-regulate Smad3 and blocked TGF-β signaling at 10 ng/ml in mammal.	Gastric Cancer, 2021, 10.1007/s10120-021-01259-5 Research Square, 2021, 10.21203/rs.3.rs-738132/v1 Sci Rep, 2020, 10(1):19723
S6713	ITD-1 ITD-1 is a potent TGF-β inhibitor. It does not block the kinase activity of either type I (TGFBR1) or type II (TGFBR2) TGFβ receptors but potently blocks phosphorylation of the effector SMAD2/3 proteins induced by TGFβ2, and only minimally in response to Activin A.	Nat Commun, 2022, 13(1):438 Cell Death Dis, 2022, 13(4):339 J Exp Clin Cancer Res, 2021, 40(1):62
S7840	Dorsomorphin (Compound C) Dorsomorphin (Compound C, BML-275) is a potent, reversible, selective AMPK inhibitor with K_i of 109 nM in cell-free assays, exhibiting no significant inhibition of several structurally related kinases including ZAPK, SYK, PKCθ, PKA, and JAK3. Dorsomorphin selectively inhibits the BMP type I receptors ALK2, ALK3 and ALK6. Dorsomorphin is used in promoting specific cell differentiation and inducing cancer cell line autophagy. For animal testing, the water-soluble S7306 Dorsomorphin (Compound C) 2HCl is recommended.	Signal Transduct Target Ther, 2022, 7(1):66 Adv Sci (Weinh), 2022, e2105208 Brain Behav Immun, 2022, S0889-1591(22)00041-1	FGF21 activates myogenic and aerobic myofiber-associated genes expression via AMPK pathway. The activator (acadesine) or inhibitor (dorsomorphin) of AMPK pathway were used to treat the pcDNA3.1-21 or control transfected C2C12 myoblasts. For this experiment, four groups were set up: FGF21-ACA (pcDNA3.1-21‡acadesine), Control-ACA (control‡acadesine), FGF21-DOR (pcDNA3.1-21‡dorsomorphin), and Control-DOR(control‡dorsomorphin). The qRT-PCR was performed to detect the genes expression of FGF21 (A), AMPK (B), Sirt 1, Myoglobin(C), Desmin (D), MEF2c (E), a-actin (F). (G) The C2C12 myoblasts were transiently transfected with pCDNA3.1-21 or pCDNA3.1, Western blot showed FGF21 activated AMPK signal via FGF21-Sirt1-AMPK. For the phosphorylated AMPK (right), the intensity of band was normalized total AMPK, and then normalized by control. (H and I) FGF21, as well as AMPK activator acadesine (ACA), increased phosphorylation of AMPM, and myogenic genes expression, especially MyHC I, which was activated by ACA (FGF21‡ACA) and suppressed by AMPK inhibitor DOR(FGF21‡DOR). The data are presented as mean±SD (P<0.05, *P<0.01, and P<0.001), n=ˆ3.
S6807	TA-02 TA-02 is a p38 MAPK inhibitor with IC50 of 20 nM. TA-02 especially inhibits TGFBR-2.
S5183	PD 169316 PD 169316 is a potent, selective and cell-permeable p38 MAP kinase inhibitor with IC50 of 89 nM. PD169316 abrogates signaling initiated by both TGFbeta and Activin A. PD169316 shows antiviral activity against Enterovirus71.	PLoS One, 2021, 16(5):e0252541

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S3223	L-Quebrachitol L-Quebrachitol (L-QCT), a natural product isolated from many plants, promotes proliferation and cell DNA synthesis. L-Quebrachitol upregulates bone morphogenetic protein-2 (BMP-2) and runt-related transcription factor-2 (Runx2) and regulatory genes associated with mitogen-activated protein kinase (MAPK) and Wnt/β-catenin signaling pathway, while down-regulating the receptor activator of the nuclear factor-κB(NF-κB) ligand (RANKL) mRNA level.
S7914	Isoxazole 9 (ISX-9) Isoxazole 9 (Isx-9) is a synthetic promotor of adult neurogenesis by triggering neuronal differentiation of adult neural stem/precursor cells (NSPCs). Isoxazole 9 (Isx-9) activates multiple pathways including TGF-β induced epithelial–mesenchymal transition (EMT) signaling, canonical and non-canonical Wnt signaling at different stages of cardiac differentiation.	Front Cell Dev Biol, 2021, 9:728352
S7658	Kartogenin Kartogenin (KGN) is an activator of the smad4/smad5 pathway, and promotes the selective differentiation of multipotent mesenchymal stem cells into chondrocytes.	Acta Biomater, 2021, S1742-7061(21)00015-5 Anticancer Res, 2021, 41(10):4753-4759 Front Chem, 2019, 7:677
S0153	SJ000291942 SJ000291942 is a canonical bone morphogenetic proteins (BMP) signaling pathway activator.

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S0523	SB 4 SB 4 is a potent and selective agonist of bone morphogenetic protein 4 (BMP4) signaling with EC50 of 74 nM. SB 4 enhances canonical BMP signaling and activates SMAD-1/5/9 phosphorylation.
S6654	SRI-011381 SRI-011381 is a novel agonist of the TGF-beta signaling pathway for treatment of Alzheimer's disease.	Dis Model Mech, 2022, dmm.046979 Front Cell Dev Biol, 2021, 9:648201 Eur J Pharmacol, 2021, 912:174587

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S0523

SB 4

SB 4 is a potent and selective agonist of bone morphogenetic protein 4 (BMP4) signaling with EC50 of 74 nM. SB 4 enhances canonical BMP signaling and activates SMAD-1/5/9 phosphorylation.

S6654

SRI-011381

SRI-011381 is a novel agonist of the TGF-beta signaling pathway for treatment of Alzheimer's disease.

Dis Model Mech, 2022, dmm.046979

Front Cell Dev Biol, 2021, 9:648201

Eur J Pharmacol, 2021, 912:174587

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S2308	Hesperetin Hesperetin is a bioflavonoid and, to be more specific, a flavanone.	Sci Rep, 2022, 12(1):7 Front Pharmacol, 2021, 12:735087 Carcinogenesis, 2020, 41(7):993-1004
S8318	Alantolactone Alantolactone (helenin, helenine, Eupatal), a naturally occurring eudesmane-type sesquiterpene lactone (SL), could induce activin/SMAD3 signaling and disrupt Cripto-1/activin receptor type II A interaction.	Nat Commun, 2022, 13(1):107 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.

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S2308

Hesperetin

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

Sci Rep, 2022, 12(1):7

Front Pharmacol, 2021, 12:735087

Carcinogenesis, 2020, 41(7):993-1004

S8318

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

Nat Commun, 2022, 13(1):107

Onco Targets Ther, 2017, 10:1767-1776