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TGF-β / Smad Inhibitors

TGF-β / Smad Inhibitors

Inhibitory Selectivity

Catalog No.	Inhibitor Name	ALK1	ALK2	ALK3	ALK4	TGFβRI/ALK5	ALK6	ALK7	TGFβRII	TGF-β	Other
A10826	SB431542					**
A11205	LDN-193189		****	***
A11017	Galunisertib					**
A11133	LY2109761					***			*
A10827	SB525334					***
A11157	SB505124				**	**
A11083	GW788388					***
A13446	LY364947					**			*		RIPK2,CK1δ,MLK-7K
A11762	RepSox					****
A11478	LDN-193189 HCl		****	***
A14311	K02288	****	****	***	*	*	****
A16096	LDN-214117		***
A14066	SD-208					**
A14213	EW-7197				***	****
A14298	ML347	**	***	*			*
A12821	LDN-212854	****	****	**	*	*
A12820	DMH1		**
A16209	Pirfenidone
A10449	Hesperetin										Histamine receptor
A12358	A 83-01				***	**		****
A12924	ITD 1									*
A14436	A 77-01					***
A16065	SIS3
A16207	R-268712					****

Notes:
1.Hover mouse over " * " to view the IC50 value.(A few compounds have proven potency but without published IC50 data.)
2.For more details about the compound, click on the product name of your interest.
3.The higher the number of " * " is, the more potent the inhibitor or activator is.
4."" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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ML347

Catalog No. A14298
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BMP receptor 抑制剂

ML347是一种选择性BMP受体抑制剂。了解更多

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K02288

Catalog No. A14311
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BMP 抑制剂

K02288是一种有效的选择性I型BMP受体抑制剂，对ALK2，ALK1和ALK6的IC50为1.1、1.8、6.4 nM。了解更多

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A 77-01

Catalog No. A14436
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ALK5 抑制剂

A 77-01是有效的TGF-βI型受体超家族激活素样激酶ALK5抑制剂，IC50为25 nM。了解更多

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LY364947

Catalog No. A13446
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TGFβR-I 抑制剂

LY364947是一种二杂芳基取代的吡唑类化合物，用作TGF-βRI（TGF-β受体I激酶）的选择性ATP竞争性抑制剂。了解更多

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NG25

Catalog No. A15185
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TAK1/MAP4K2 抑制剂

NG25和TAK1抑制TLR7和TLR9激动剂激活IKK，并阻止Gen2.2细胞中这些配体诱导的1型IFN分泌。了解更多

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SB-505124 HCl

Catalog No. A15232
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TGF-β Receptors 抑制剂

SB-505124 Hydrochloride是激活素受体样激酶（ALKS）的抑制剂。了解更多

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SD-208

Catalog No. A14066
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TGF-βR 抑制剂

SD-208是一种有效的ATP竞争性转化生长因子-β受体1（TGF-βRI）抑制剂（IC50 = 49 nM）；与TGF-βRII和其他常见激酶相比，分别显示出> 100倍和> 17倍的选择性。了解更多

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(+)-ITD 1

Catalog No. A16073
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TGF-β 抑制剂

(+)-ITD 1 是ITD-1的拆分对映异构体，与外消旋ITD-1相比，其TGF-β抑制作用（?400 nM）增加了2倍以上，在心脏发生方面增加了1.3倍。了解更多

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LDN-214117

Catalog No. A16096
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ALK2 抑制剂

LDN-214117是一种选择性有效的ALK2抑制剂。LDN-214117对ALK2的抑制最大，生化IC50为24 nM。了解更多

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R-268712

Catalog No. A16207
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ALK5 抑制剂

R-268712是一种有效且选择性的ALK5抑制剂，IC50为2.5 nM。了解更多

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LY 3200882

Catalog No. A16816
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TGFβRI 抑制剂

LY 3200882是有效的、高选择性TGF-β receptor type 1 (TGFβRI)抑制剂，在体外肿瘤组织和免疫细胞以及体内皮下肿瘤中，有效地以浓度依赖方式抑制TGFβ介导的SMAD磷酸化。了解更多

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BIBF0775

Catalog No. A17230
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TGFβRI 抑制剂

BIBF0775 is an inhibitor of the transforming growth factor β receptor I (TGFβRI). 了解更多

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TGFβRI-IN-1

Catalog No. A18800
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TGFβRI kinase inhibitor

TGFβRI-IN-1 is an oral active and selective TGFβ receptor type I (TGFβRI) kinase inhibitor, with IC50 values of 2 nM and 7.6 μM for TGFβRI and TGFβRII, respectively. 了解更多

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F9995-0144

Catalog No. A14162
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TGF-βR 抑制剂

N/A 了解更多

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Kartogenin

Catalog No. A12926
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Smad 抑制剂

Kartogenin能有效诱导人骨髓间充质干细胞分化为软骨细胞。了解更多

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GW788388

Catalog No. A11083
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TGF-beta/Smad 抑制剂

GW788388是有效的，口服活性的，选择性的转化生长因子β受体I（TGF-βR1）（激活素受体样激酶5，ALK5）抑制剂,无细胞试验中IC50为18 nM，也抑制TGF-βII型受体和activin II型受体活性，但不抑制BMP II型受体。了解更多

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LDN-212854

Catalog No. A12821
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BMP receptor 抑制剂

LDN-212854是一种ALK2偏爱的BMP I型受体激酶抑制剂。了解更多

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SB-505124

Catalog No. A11157
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ALK5 抑制剂

SB-505124是转化生长因子-βI型受体（ALK5），ALK4和ALK7的选择性抑制剂（ALK5和ALK4的IC50值分别为47和129 nM）。了解更多

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A 83-01

Catalog No. A12358
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TGF-β/ALK5 抑制剂

A 83-01是转化生长因子βI型受体ALK5、淋巴结受体ALK4和淋巴结受体ALK7的选择性抑制剂。了解更多

Product Citations (17)

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- Dan Zhao, .et al. From crypts to enteroids: establishment and characterization of avian intestinal organoids, Poult Sci, 2022, Mar; 101(3): 101642 PMID: 35016046
- Anna Nakanishi, .et al. Effects of human induced pluripotent stem cell-derived intestinal organoids on colitis-model mice, Regen Ther, 2022, Sep 9;21:351-361 PMID: 36161099
- Amira Abugomaa, .et al. Establishment of a direct 2.5D organoid culture model using companion animal cancer tissues, Biomed Pharmacother, 2022, Oct;154:113597 PMID: 36030590
- Isamu Ogawa, .et al. Suspension culture of human induced pluripotent stem cell-derived intestinal organoids using natural polysaccharides, Biomaterials, 2022, Sep;288:121696 PMID: 36038421
- Mohamed Elbadawy, .et al. Anti-tumor effect of trametinib in bladder cancer organoid and the underlying mechanism, Authorea, 2020, October 20
- Daichi Onozato, .et al. Application of Human Induced Pluripotent Stem Cell-Derived Intestinal Organoids as a Model of Epithelial Damage and Fibrosis in Inflammatory Bowel Disease, Biol Pharm Bull, 2020, 43(7), 1088-1095
- Amira Abugomaa, .et al. Establishment of 2.5D Organoid Culture Model Using 3D Bladder Cancer Organoid Culture, Sci Rep, 2020, Jun 10;10(1):9393 PMID: 32523078
- Jing-Yu Lin, .et al. In vitro expansion of pancreatic islet clusters facilitated by hormones and chemicals, Cell Discov, 2020, 6: 20 PMID: 32284878
- Kondo S, .et al. Establishment of a novel culture method for maintaining intestinal stem cells derived from human induced pluripotent stem cells, Biol Open, 2020, Jan 9;9(1) PMID: 31919043
- Onozato D, .et al. Generation of Intestinal Organoids Suitable for Pharmacokinetic Studies from Human Induced Pluripotent Stem Cells, Drug Metab Dispos, 2018, Nov;46(11):1572-1580 PMID: 29615438
- Usui T, .et al. Preparation of Human Primary Colon Tissue-Derived Organoid Using Air Liquid Interface Culture, Curr Protoc Toxicol, 2018, Feb 21;75:22.6.1-22.6.7 PMID: 29512123
- Kondo S, .et al. Using human iPS cell-derived enterocytes as novel in vitro model for the evaluation of human intestinal mucosal damage, Inflamm Res, 2018, Dec;67(11-12):975-984 PMID: 30317465
- Onozato D, .et al. Efficient Generation of Cynomolgus Monkey Induced Pluripotent Stem Cell-Derived Intestinal Organoids with Pharmacokinetic Functions, Stem Cells Dev, 2018, Aug 1;27(15):1033-1045 PMID: 29742964
- Tatsuya Usui, .et al. Hedgehog Signals Mediate Anti-Cancer Drug Resistance in Three-Dimensional Primary Colorectal Cancer Organoid Culture, Int J Mol Sci, 2018, Apr; 19(4): 1098 PMID: 29642386
- Tatsuya Usui, .et al. Establishment of a dog primary prostate cancer organoid using the urine cancer stem cells, Cancer Sci, 2017, Dec; 108(12): 2383-2392 PMID: 29024204
- Tatsuya Usui, .et al. Establishment of a novel three-dimensional primary culture model for hippocampal neurogenesis, Physiol Rep, 2017, Jun; 5(12): e13318 PMID: 28642339
- Tatsuya Usui, .et al. Establishment of a Novel Model for Anticancer Drug Resistance in Three-Dimensional Primary Culture of Tumor Microenvironment, Stem Cells Int, 2016, 2016: 7053872 PMID: 28119740
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SB 525334

Catalog No. A10827
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ALK 抑制剂

SB525334是转化生长因子-β受体I（ALK5，TGF-βRI）的选择性抑制剂 (IC50 = 14.3 nM)。抑制TGF-β1诱导的smad2/3核定位和TGF-βRI诱导的肾细胞mRNA表达。了解更多

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Hesperetin

Catalog No. A10449
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PDE4 抑制剂

Hesperetin是一种选择性磷酸二酯酶(PDE)4抑制剂，存在于中药“陈皮”中。橙皮素是一种柑橘类黄酮，据报道可以降低血浆胆固醇。橙皮素降低Hep-G2细胞中ACAT-2 mRNA的转录，并以剂量依赖的方式降低ApoB蛋白的合成。它也是类癌的潜在疗法。了解更多

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LY2157299

Catalog No. A11017
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TGF-βR 抑制剂

LY2157299是一种口服活性转化生长因子β受体（TGF-βR）激酶抑制剂。了解更多

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- Satoshi Endo, .et al. Flavonol glycosides of Rosa multiflora regulates intestinal barrier function through inhibiting claudin expression in differentiated Caco-2 cells, Nutr Res, 2019, 4 November
- Oguri G, .et al. Effects of methylglyoxal on human cardiac fibroblast: roles of transient receptor potential ankyrin 1 (TRPA1) channels., Am J Physiol Heart Circ Physiol., 2014, 307(9):H1339-52 PMID: 25172898
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SB 431542

Catalog No. A10826
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TGF-beta/Smad 抑制剂

SB 431542是转化生长因子-β超家族I型激活素受体样激酶（ALK）受体ALK4，ALK5和ALK7的有效抑制剂。了解更多

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- Huong Pham, .et al. BMP11 Negatively Regulates Lipid Metabolism in C2C12 Muscle Cells, Biotechnol Bioprocess Eng, 2020, ID: 222137835
- Tamara Chamberlin, .et al. Obesity Reduces Mammary Epithelial Cell TGFβ1 Activity Through Macrophage-Mediated Extracellular Matrix Remodeling, FASEB J, 2020, Jun;34(6):8611-8624 PMID: 32359100
- Satoshi Endo, .et al. Flavonol glycosides of Rosa multiflora regulates intestinal barrier function through inhibiting claudin expression in differentiated Caco-2 cells, Nutr Res, 2019, 4 November
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LDN193189

Catalog No. A11205
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ALK 抑制剂

LDN193189是一种高效的小分子BMP抑制剂，可抑制BMP I型受体ALK2（IC50=5 nM），ALK3（IC50=30 nM）和ALK6（TGFβ1/BMP信号转导）以及随后的SMAD磷酸化。了解更多

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- Trang Thi Huyen Dang, .et al. BMP10 positively regulates myogenic differentiation in C2C12 myoblasts via the Smad 1/5/8 signaling pathway, Mol Cell Biochem, 2021, May;476(5):2085-2097 PMID: 33517521
- Shizu Aikawa, .et al. Autotaxin-lysophosphatidic acid-LPA 3 signaling at the embryo?\epithelial boundary controls decidualization pathways, EMBO J, 2017, Jul 14; 36(14): 2146-2160 PMID: 28588064
- HIROTAKA SOMEYA, .et al. Thymosin beta 4 is associated with RUNX2 expression through the Smad and Akt signaling pathways in mouse dental epithelial cells, Int J Mol Med, 2015, May; 35(5): 1169-1178 PMID: 25739055
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LY2109761

Catalog No. A11133
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TβRI/II kinase 抑制剂

LY2109761是一种新型的I型和II型转化生长因子β受体双重抑制剂，对Smad2的磷酸化产生负面影响，作为抑制胰腺癌转移的治疗方法。了解更多

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- Uto T, .et al. Critical role of plasmacytoid dendritic cells in induction of oral tolerance, J Allergy Clin Immunol, 2018, Jun;141(6):2156-2167.e9 PMID: 29477579
- Jared M. Fischer, .et al. Single cell lineage tracing reveals a role for TgfβR2 in intestinal stem cell dynamics and differentiation, Proc Natl Acad Sci U S A, 2016, Oct 25; 113(43): 12192-12197 PMID: 27791005
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SIS3

Catalog No. A16065
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Smad3 抑制剂

SIS3是Smad3的新型特异性抑制剂。它对转化生长因子-β1诱导的细胞外基质表达有影响。了解更多

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- Miao Deng, .et al. pH-Triggered Copper-Free Click Reaction-Mediated Micelle Aggregation for Enhanced Tumor Retention and Elevated Immuno-Chemotherapy against Melanoma, ACS Appl Mater Interfaces, 2021, Apr 21;13(15):18033-18046 PMID: 33834754
- Wei P, .et al. Transforming growth factor (TGF)-β1-induced miR-133a inhibits myofibroblast differentiation and pulmonary fibrosis, Cell Death Dis, 2019, Sep 11;10(9):670 PMID: 31511493
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DMH-1

Catalog No. A12820
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ALK2 抑制剂

DMH-1是骨形态发生蛋白（BMP）ALK2受体的选择性抑制剂（IC50 = 108 nM）。了解更多

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- Teresa Rayon, .et al. Species-specific pace of development is associated with differences in protein stability, Science, 2020, Sep 18;369(6510):eaba7667 PMID: 32943498
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ITD-1

Catalog No. A12924
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TGF-β 抑制剂

ITD-1是一种新型高选择性TGFβ途径抑制剂。ITD-1分子将干细胞转化为心脏细胞。了解更多

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- M. C. Wilkes, .et al. Diamond Blackfan anemia is mediated by hyperactive Nemo-like kinase, Nat Commun, 2020, 11: 3344 PMID: 32620751
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EW-7197 (Vactosertib)

Catalog No. A14213
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ALK4/ALK5 抑制剂

EW-7197是一种高效，选择性可生物利用的TGF-βI受体ALK4/ALK5抑制剂，IC50分别为13 nM和11 nM。了解更多

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- Bordignon P, .et al. Dualism of FGF and TGF-β Signaling in Heterogeneous Cancer-Associated Fibroblast Activation with ETV1 as a Critical Determinant, Cell Rep, 2019, Aug 27;28(9):2358-2372 PMID: 31461652
- Morita T, .et al. Tumor Progression Is Mediated by Thymosin-β4 through a TGFβ/MRTF Signaling Axis, Mol Cancer Res, 2018, May;16(5):880-893 PMID: 29330296