Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T9523 |
TGFβRI-IN-3
|
TGF-beta/Smad | Stem Cells |
TGFβRI-IN-3 抑制TGFβR1,IC50为 0.79 nM,是对 MAP4K4 的选择性2000 倍。TGFβRI-IN-3 是一种高选择性的 TGFβR1 抑制剂,在免疫肿瘤中具有潜在的应用。 | |||
T13137 | TGFβRI-IN-1 | TGF-beta/Smad | Stem Cells |
TGFβRI-IN-1 is an oral active and selective inhibitor of TGFβ receptor type I (TGFβRI) kinase(IC50 values of 2 nM and 7.6 μM for TGFβRI and TGFβRII, respectively ). | |||
T72976 |
TGFβRI-IN-6
|
||
TGFβRI-IN-6 是一种有效的TGFβRI 抑制剂,IC50值为 0.55 nM。TGFβRI-IN-6 具有增强抗肿瘤免疫力的潜力。 | |||
T62559 | TGFβRI-IN-4 | ||
TGFβRI-IN-4 是一种高效的、口服具有活力的 TGFβ 受体 I 型激酶 (TGFβRI) 抑制剂,能够作用于 ALK5 (IC50: 44 nM) 和 NIH3T3 (IC50: 42.5 nM)。TGFβRI-IN-4 在异种移植瘤模型中,能够抑制肿瘤生长和肿瘤重量。 | |||
T60931 |
TGFβRI-IN-5
|
||
TGFβRI-IN-5 (Compound 4b) 是 TGFβRI 的有效抑制剂,IC50值为 0.08 μM。TGFβRI-IN-5 对所有测试细胞系的均显示出显著的抗癌活性,可增强细胞凋亡并抑制细胞周期的 G2/M 期。 | |||
T13139 |
TP-008
TGFβRI-IN-2 |
Others | Others |
TGFβRI-IN-2 is a selective, potent and orally active inhibitor of (Activin-Like Kinase 5) ALK 5(pIC50 and pEC50 values of 7.6 and 6.63, respectively). | |||
T5125 |
LY3200882
|
TGF-beta/Smad | Stem Cells |
LY3200882 是一种高度选择性的、口服活性的、具有 ATP 竞争性的 TGF-β 受体 1 型 (ALK5) 抑制剂(IC50:38.2 nM)。它能够抑制多种促肿瘤活性,可用作免疫调节剂。 | |||
T12433 |
PF-06952229
PF06952229 |
TGF-beta/Smad | Stem Cells |
PF-06952229 是 TGFβRI 的选择性抑制剂。 PF-06952229 可用于治疗实体瘤,特别是转移性乳腺癌的研究。 | |||
T2510 |
Galunisertib
LY2157299 |
TGF-beta/Smad | Stem Cells |
Galunisertib (LY2157299) 是一种TGF-β 受体 I 型 (TGF-βRI) 激酶的选择性抑制剂,其IC50=56 nM。 | |||
T9837 |
N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-bromoaniline
|
ALK | Angiogenesis; Tyrosine Kinase/Adaptors |
N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-bromoaniline 是一种有效的 ALK5 抑制剂,IC50 为 7nM。 | |||
T6337 |
RepSox
ALK5 Inhibitor II,SJN 2511,E-616452 |
ALK; TGF-beta/Smad | Angiogenesis; Stem Cells; Tyrosine Kinase/Adaptors |
RepSox (ALK5 Inhibitor II) 是一种 TGFβR-1/ALK5 的抑制剂,可以抑制 ATP 与 ALK5 结合 以及 ALK5 自磷酸化 (IC50=23/4 nM),具有选择性。RepSox 可以诱导 MEFs 细胞的脂肪生成。 | |||
T2109 |
SD-208
ALK5 Inhibitor V,SD208 |
TGF-beta/Smad | Stem Cells |
SD-208 (ALK5 Inhibitor V) 是 TGF-βRI (ALK5) 的选择性抑制剂(IC50:48 nM),对其选择性是对 TGF-βRII 的 100 多倍。 | |||
T61203 |
ALK5-IN-8
|
||
ALK5-IN-8 is a highly effective inhibitor of TGFβRI (ALK5). It hinders the phosphorylation of ALK5 on downstream signaling proteins (Smad2 or Smad3) by obstructing the interaction between TGFβRI and ligands. Consequently, it disrupts or prevents TGF-β signaling. ALK5-IN-8 shows promise in the study of diverse diseases associated with ALK5-mediated pathways[1]. | |||
T64051 | ALK5-IN-9 | ||
ALK5-IN-9 是一种有效的、口服具有活力的 TGFβRI (ALK5) 抑制剂。ALK5-IN-9 能够抑制 ALK5 自磷酸化 (IC50: 25 nM) 并抑制 NIH3T3 细胞活性 (IC50: 74.6 nM)。ALK5-IN-9 具有良好的药代动力学特征,能够改善 hERG 抑制。ALK5-IN-9 对癌症疾病表现出研究潜能。 | |||
T2048 |
LY-364947
LY 364947,HTS466284 |
MLK; Casein Kinase; TGF-beta/Smad; RIP kinase | Apoptosis; MAPK; Metabolism; NF-κB; Stem Cells |
LY-364947 (HTS466284) 是有效的、ATP 竞争性的TGFβR-I 抑制剂(IC50:59 nM),是对 TGFβR-II 选择性的 7 倍。 | |||
T35896 |
AZ 12799734
AZ12799734 |
ALK | Angiogenesis; Tyrosine Kinase/Adaptors |
AZ 12799734 是一种具有口服活性、选择性和有效性的 TGFBR1和 ALK5 双重抑制剂,对 BMP 和 TGFβ 有抑制作用,可用于研究肿瘤。 | |||
T10426 | AZ12601011 | ALK | Angiogenesis; Tyrosine Kinase/Adaptors |
AZ12601011 is a highly potent and selective inhibitor of the TGFBR1 kinase, administered orally. It displays an IC50 of 18 nM and a Kd of 2.9 nM. By selectively targeting ALK4, TGFBR1, and ALK7, AZ12601011 effectively inhibits the phosphorylation of SMAD2. Additionally, it has been shown to hinder the growth and metastasis of mammary tumors [1]. | |||
T1744 |
BIX02188
|
Apoptosis; MEK | Apoptosis; MAPK |
BIX02188 是一种具有选择性和有效性的 MEK5 抑制剂,抑制 MEK5 诱导表达致癌突变体FLT3-ITD的细胞凋亡。 | |||
T21295 |
BIX02189
BIX 02189 |
ERK; MEK | MAPK |
BIX02189 是一种有效的选择性 MEK5 和 ERK5 抑制剂,IC50分别为 1.5 和 59 nM。 |