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TGF-β / Smad

TGF-β / Smad

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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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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

Product Citations (1)

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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

Product Citations (2)

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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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