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TGF-β / Smad

TGF-β / Smad

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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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RepSox (SJN 2511)

Catalog No. A11762
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RepSox (SJN 2511)是TGF-βI型受体ALK5的选择性抑制剂（ALK5自磷酸化和ALK5结合的IC50值分别为0.004和0.023μM）。了解更多

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- Wojciech J Szlachcic, .et al. SARS-CoV-2 infects an in vitro model of the human developing pancreas through endocytosis, iScience, 2022, Jul 15;25(7) PMID: 35756892
- Xu H, .et al. Androgen receptor reverses the oncometabolite R-2-hydroxyglutarate-induced prostate cancer cell invasion via suppressing the circRNA-51217/miRNA-646/TGFβ1/p-Smad2/3 signaling, Cancer Lett, 2020, Mar 1;472:151-164 PMID: 31846689
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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
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LDN193189 HCl

Catalog No. A11478
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LDN193189 HCl是ldn193189的盐酸盐。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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- Brandon J.Peiffer, .et al. Activation of BMP Signaling by FKBP12 Ligands Synergizes with Inhibition of CXCR4 to Accelerate Wound Healing, Cell Chem Biol, 2019, 26, 1-10
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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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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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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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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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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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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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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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F9995-0144

Catalog No. A14162
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TGF-βR 抑制剂

N/A 了解更多

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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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Alantolactone

Catalog No. A14810
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Alantolactone是一种天然的桉烷类倍半萜内酯，能诱导activin/SMAD3信号、干扰Cripto-1/activin受体ⅡA型受体的相互作用。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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Chebulinic acid

Catalog No. A16208
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Chebulinic acid是结核分枝杆菌DNA促旋酶的有效天然抑制剂，也可以抑制SMAD-3磷酸化，抑制H+K+-ATPase活性。了解更多

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Pirfenidone

Catalog No. A16209
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Pirfenidone是一种用于治疗特发性肺纤维化（IPF）的抗纤维化药物。它通过下调生长因子和前胶原I和II的产生来减少肺纤维化。了解更多

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SRI-011381 hydrochloride

Catalog No. A16210
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TGF-beta 激动剂

SRI-011381 hydrochloride是一种TGF-β信号传导激动剂。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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PKC 412 (Midostaurin)

Catalog No. A12650
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PKC 抑制剂

PKC 412 (Midostaurin)是一种广谱蛋白激酶抑制剂。抑制常规PKC亚型α/β/γ，PDFRβ，VEGFR2，Syk，Flk-1，Flt3，Cdk1/B，PKA，c-Kit，c-Fgr，c-Src，VEGFR1和EGFR。显示有效的抗肿瘤活性。了解更多

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GO6983

Catalog No. A13790
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PKC 抑制剂

GO6983是有效的蛋白激酶C（PKC）抑制剂。它减少了心肌缺血/再灌注损伤后多形核白细胞的粘附和浸润。了解更多

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- Kouki Kawakami, .et al. Heterotrimeric Gq proteins act as a switch for GRK5/6 selectivity underlying β-arrestin transducer bias, Nat Commun, 2022, 13: 487 PMID: 35078997
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Ro 31-8220 mesylate

Catalog No. A13514
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PKC 抑制剂

Ro 31-8220 mesylate是一种PKC抑制剂，可抑制PKC激活剂佛波肉豆蔻酸酯乙酸酯（PMA，IC50 = 1.35 x 10（-6）M）或二酰基甘油（OAG，diC8）诱导的人PMN的刺激性液体胞吞作用了解更多

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- Dao-Lai Zhang, .et al. Gq activity- and β-arrestin-1 scaffolding-mediated ADGRG2/CFTR coupling are required for male fertility, eLife, 2018, 7: e33432 PMID: 29393851
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12-O-tetradecanoyl phorbol-13-acetate

Catalog No. A14616
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PKC activator

12-O-tetradecanoyl phorbol-13-acetate是佛波醇的二酯，是从巴豆油中提取的促肿瘤化合物。它是在体内和体外以nM浓度可逆的高效蛋白激酶C（PKC）激活剂。了解更多

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- 孙哲 ,etc. 右美托咪定对痛觉过敏大鼠脊髓 PKCγ, CaMKⅡα 及 pCaMKⅡα 表达的影响. 天津医药, 2016, 44(6), 700-703.
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PKC (19-36)

Catalog No. A14871
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PKC 抑制剂

PKC (19-36)蛋白激酶C的假底物肽抑制剂（IC50 = 0.18 uM）。了解更多

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(-)-Indolactam V

Catalog No. A13043
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PKC activator

(-)-Indolactam V是一种蛋白激酶C激活剂，可将人ES细胞衍生的定形内胚层强有力地引导至胰腺内胚层中。了解更多

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- Manuel Mendoza, .et al. The total synthesis of (-)-indolactam I, Tetrahedron, 2019, May
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PKC-IN-1

Catalog No. A16212
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PKC 抑制剂

PKC-IN-1是一种有效的PKC beta II抑制剂，Ki为14.9 nM。专利WO 2008096260 A1的化合物实例H6。了解更多

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NSC305787

Catalog No. A16213
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PKC 抑制剂

NSC305787是PKC的小分子抑制剂，IC50为8.3 uM，9.4 uM，55 uM，用于重组ezrin，moesin和radixin的PKC磷酸化。了解更多

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Ruboxistaurin (LY333531 HCl)

Catalog No. A16604
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PKCβ1 and PKCβ2 抑制剂

LY333531是一种特异性β-蛋白激酶C的抑制剂。竞争性和可逆性抑制PKCβ1和PKCβ2，IC50值分别为4.7和5.9 nM。了解更多

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BJE6-106

Catalog No. A18627
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PKCδ inhibitor

BJE6-106 (B106) is a potent, selective 3rd generation PKCδ inhibitor with an IC50 of 0.05 μM and targets selectivity over classical PKC isozyme PKCα (IC50=50 μM). 了解更多

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LXS196

Catalog No. A19419
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PKC inhibitor

LXS196 is a potent, selective and orally active protein kinase C (PKC) inhibitor, with IC50 values of 1.9 nM, 0.4 nM and 3.1 μM for PKCα, PKCθ and GSK3β, respectively. It can be used for the treatment of uveal melanoma. 了解更多

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PKC-theta inhibitor 1

Catalog No. A18966
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PKCθ inhibitor

PKC-theta inhibitor 1 is the PKCθ inhibitor with an Ki value of 6 nM, inhibits IL-2 production in vivo with an IC50 of 0.19 μM. 了解更多

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Roy-Bz

Catalog No. A13348
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PKCδ activator

Roy-Bz is a selecive PKCδ activator. Roy-Bz potently inhibits the proliferation of colon cancer cells by inducing a PKCδ-dependent mitochondrial apoptotic pathway involving caspase-3 activation. 了解更多

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Delcasertib

Catalog No. A12829
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δ-protein kinase C (δPKC) inhibitor

Delcasertib (KAI-9803) is a potent and selective δ-protein kinase C (δPKC) inhibitor. 了解更多

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DCPLA-ME

Catalog No. A21368
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PKCε activator

DCPLA-ME, the methyl ester form of DCPLA, is a potent PKCε activator for use in the treatment of neurodegenerative diseases. 了解更多

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