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8

抑制剂 & 化合物

2

天然产物

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Cat. No. Product Name Target Signaling Pathways
T2123 LY2109761

Autophagy; TGF-beta/Smad Autophagy; Stem Cells
LY2109761 是一种新型选择性 TGF-β 受体 I/II 型 (TβRI/II) 双重抑制剂,Ki 分别为 38 nM 和 300 nM。
T3636 (E)-SIS3

SIS3,SIS3 盐酸盐,SIS3 HCl

TGF-beta/Smad Stem Cells
(E)-SIS3 (SIS3) 是 Smad3 的选择性抑制剂,能够抑制 Smad3 磷酸化(IC50:3 μM)。它利用 TGF-β1 抑制成纤维细胞向肌成纤维细胞分化。
T80628 Myristoyl tetrapeptide-12

TGF-beta/Smad Stem Cells
Myristoyl tetrapeptide-12 直接激活SMAD2,并促使SMAD3与DNA结合。该化合物能有效促进毛发,特别是睫毛的生长。
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].
T77076 Luspatercept

Luspatercept (ACE-536) 是一种重组修饰的 ActRIIB 融合蛋白,与转化生长因子β超家族配体结合,通过与GDF11结合抑制Smad2/3信号通路,从而增加红细胞数量并促进红细胞前体成熟,用于贫血的研究。
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].
T26925 Butaprost

Butaprostum,TR-4979,(R)-Butaprost

Butaprost is a chemical compound that functions as a selective agonist for the prostaglandin E receptor (EP2). It exhibits an EC50 of 33 nM and a Ki of 2.4 μM when interacting with the murine EP2 receptor. However, Butaprost demonstrates lower activity against murine EP1, EP3, and EP4 receptors. Furthermore, it effectively attenuates fibrosis by inhibiting the TGF-β/Smad2 signaling pathway [1] [2] [3].
T61029 TP0427736 hydrochloride

TP0427736 hydrochloride 可用于雄激素性脱发 (AGA) 研究。TP0427736 hydrochloride 可抑制由 TGF-β1 诱导的 A549 细胞中 Smad2/3 的磷酸化,IC50值为 8.68 nM。它也是ALK5激酶的有效抑制剂,IC50值为 2.72 nM,比对 ALK3 836 nM 的抑制作用高 300 倍。

化合物

LY2109761
Cat.No: T2123
Synonym:
Target: Autophagy, TGF-beta/Smad
(E)-SIS3
Cat.No: T3636
Synonym: SIS3,SIS3 盐酸盐,SIS3 HCl
Target: TGF-beta/Smad
Myristoyl tetrapeptide-12
Cat.No: T80628
Synonym:
Target: TGF-beta/Smad
AZ12601011
Cat.No: T10426
Synonym:
Target: ALK
Luspatercept
Cat.No: T77076
Synonym:
Target:
ALK5-IN-8
Cat.No: T61203
Synonym:
Target:
Butaprost
Cat.No: T26925
Synonym: Butaprostum,TR-4979,(R)-Butaprost
Target:
TP0427736 hydrochloride
Cat.No: T61029
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
T5247 Trimethylamine N-oxide dihydrate

二水氧化三甲胺,TMANO Dihydrate

Others; Endogenous Metabolite Metabolism; Others
Trimethylamine N-oxide dihydrate (TMANO Dihydrate) 是内源性代谢产物的一种。
T3876 Loureirin B

龙血素B,龙血素 B

PAI-1; ERK; Potassium Channel; JNK MAPK; Membrane transporter/Ion channel; Metabolism
Loureirin B 是从剑叶龙血树中分离到的一种黄酮,是 PAI-1抑制剂,IC50值为 26.10 μM。它抑制 KATP,以及 ERK 和 JNK 的磷酸化,具有抗糖尿病的功效。

天然产物

Trimethylamine N-oxide dihydrate
Cat.No: T5247
Synonym: 二水氧化三甲胺,TMANO Dihydrate
Target: Others, Endogenous Metabolite
Loureirin B
Cat.No: T3876
Synonym: 龙血素B,龙血素 B
Target: PAI-1, ERK, Potassium Channel, JNK
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