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抑制剂 & 化合物

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Cat. No. Product Name Target Signaling Pathways
T4283 SRI-011381

TGF-beta/Smad Stem Cells
SRI011381 是口服具有活力的 TGF-β信号通路的激活剂,具有神经保护活性。
T16886 Sinefungin

Adenosyl-Ornithine,西奈芬净,A-9145,Antibiotic 32232RP

Others; Histone Methyltransferase; Antibiotic; Antifungal Chromatin/Epigenetic; Microbiology/Virology; Others
Sinefungin (Adenosyl-Ornithine) 是病毒粒子mRNA (鸟嘌呤-7-)-甲基转移酶、 mRNA (核苷-2'-)-甲基转移酶和病毒增殖的有效抑制剂。它还抑制SET7/9,通过抑制H3K4甲基化来改善肾纤维化。
T5129 SRI-011381 hydrochloride

SRI-011381 hydrochloride [1629138-41-5(free base)]

TGF-beta/Smad Stem Cells
SRI-011381 hydrochloride 是口服具有活力的TGF-β信号通路的激活剂,具有神经保护活性。
T81149 SMA4

SMA4是一款选择性的PKG1α激活剂,其对PKG1α的EC50为29 μM。该化合物能够在细胞内促进PKG1底物——血管扩张刺激磷蛋白(VASP)的磷酸化,同时能够抑制人肺动脉平滑肌细胞(hPASMC)的增殖,适用于心血管疾病研究。
T61389 TGFβ1-IN-1

TGFβ1-IN-1(化合物42)是一种有效且可口服的TGF-β1抑制剂,能够抑制TGF-β1诱导的纤维化标志物(α-SMA和纤连蛋白)的上调,适用于肝纤维化疾病的研究。
T60266 (Rac)-Indoximod

(Rac)-Indoximod (1-Methyl-DL-tryptophan) is a potent inhibitor of indoleamine 2,3-dioxygenase (IDO). Combined treatment with IFN-γ and (Rac)-Indoximod significantly suppresses the activity of α-SMA-expressing human cardiac myofibroblasts (hCMs) and promotes apoptosis by up-regulating the genes IRF-1, Fas, and FasL. Moreover, this co-treatment effectively improves cardiac fibrosis[1].
T61586 TGFβ-IN-2

TGFβ-IN-2 (Compound 9d) effectively inhibits the accumulation of total collagen induced by TGF-β in NRK-49F cells, with an IC 50 value of 4.31 μM. It also suppresses the in vitro protein expression of COL1A1, α-SMA, and p-Smad3, which are induced by TGF-β. Additionally, TGFβ-IN-2 shows promise as a potential anti-fibrosis compound for in vivo applications through oral administration [1].
T63248 NTU281

NTU281 是转谷氨酰胺酶-2 (transglutaminase-2) 的有效抑制剂,能够减少糖尿病大鼠血清肌酐和蛋白尿的升高,并降低肾小球 I 型胶原积累、Hic-5 和α-SMA 表达,以及减少细胞凋亡 (apoptosis),能够用于糖尿病引起的肾小球硬化的研究。
T74996 FXR agonist 3

FXR agonist3 是一种抗 NASH 试剂,通过激活 FXR 起作用。FXR agonist3 抑制 COL1A1、TGF-β1、α-SMA 和 TIMP1的表达,具有抗纤维化活性。FXR agonist3 显著减轻肝脏脂肪变性和炎症,改善肝纤维化水平。
T64141 ATX inhibitor 11

ATX inhibitor 11 是 ATX (autotaxin) 的有效抑制剂 (IC50: 2.7 nM)。ATX inhibitor 11 能够缓解小鼠纤维化模型中纤维化组织的严重程度,有效减少纤维化生物标志物 α-SMA 的沉积。ATX inhibitor 11 能够用于研究肺纤维化。
T35807 C18 dihydro Ceramide (d18:0/18:0)

C18 dihydro Ceramide (d18:0/18:0),Cer(d18:0/18:0)

C18 dihydro Ceramide is a bioactive sphingolipid and precursor in the de novo synthesis of C18 ceramide that lacks the 4,5-trans double bond. [1] Increased C18 dihydroceramide lipid levels lead to increased triacylglycerol storage and autophagosome accumulation as well as upregulation of the fibrosis markers α-SMA and FGF2 in Chang and LX-2 liver cells. C18 dihydro Ceramide is elevated in the plasma of pre-diabetics up to 9 years prior to the onset of type 2 diabetes. [2] It is also elevated in...
T83770 Klotho-derived Peptide 1 (56-87) (human) TFA

KP1 (56-87)

Klotho衍生肽1(KP1)(56-87)是从人类Klotho蛋白质中衍生的肽,具有扰乱TGF-β信号传导的作用。它与TGF-β受体类型1(TGFBR2)和TGF-β受体类型2(TGFBR2;Kds分别为1.41和14.6µM)结合。KP1(10 µg/ml)的预孵育抑制TGF-β在NRK-49F大鼠成纤维细胞中诱导的纤维连接蛋白和α-平滑肌肌动蛋白(α-SMA)水平的增加。在体内,KP1(每天1 mg/kg)选择性地定位于受损的肾脏,并减少血清肌酐和血尿素氮水平,这些是肾功能的标志物,同时也减少了小鼠单侧输尿管阻塞(UUO)和单侧缺血-再灌注损伤诱导的肾脏纤维化模型中的肾纤维化。
T83682 Tat-Gap 19 TFA

Tat-Gap 19是一种针对连接蛋白43 (Cx43) 半通道的肽抑制剂,由HIV-1 Tat蛋白传导域与对应于Cx43第128-136残基的九氨基酸肽连接而成。Tat-Gap 19 (10 µM) 能够抑制初级大鼠肝细胞中由谷氨酸引发的ATP释放,这是Cx43半通道活性的标志。在通过中脑动脉堵塞(MCAO)诱导的小鼠脑缺血再灌注损伤模型中,以25 mg/kg的剂量进行给药,可减少梗死体积。腹腔内注射Tat-Gap 19 (1 mg/kg 每天) 能够减少硫代乙酰胺引起的小鼠肝损伤模型中的纤维化病灶面积及表达α-平滑肌肌动蛋白 (α-SMA) 的肝星状细胞(成纤维细胞的前体)面积,并提高同种小鼠分离的肝细胞中超氧化物歧化酶 (SOD) 活性。

化合物

SRI-011381
Cat.No: T4283
Synonym:
Target: TGF-beta/Smad
Sinefungin
Cat.No: T16886
Synonym: Adenosyl-Ornithine,西奈芬净,A-9145,Antibiotic 32232RP
Target: Others, Histone Methyltransferase, Antibiotic, Antifungal
SRI-011381 hydrochloride
Cat.No: T5129
Synonym: SRI-011381 hydrochloride [1629138-41-5(free base)]
Target: TGF-beta/Smad
SMA4
Cat.No: T81149
Synonym:
Target:
TGFβ1-IN-1
Cat.No: T61389
Synonym:
Target:
(Rac)-Indoximod
Cat.No: T60266
Synonym:
Target:
TGFβ-IN-2
Cat.No: T61586
Synonym:
Target:
NTU281
Cat.No: T63248
Synonym:
Target:
FXR agonist 3
Cat.No: T74996
Synonym:
Target:
ATX inhibitor 11
Cat.No: T64141
Synonym:
Target:
C18 dihydro Ceramide (d18:0/18:0)
Cat.No: T35807
Synonym: C18 dihydro Ceramide (d18:0/18:0),Cer(d18:0/18:0)
Target:
Klotho-derived Peptide 1 (56-87) (human) TFA
Cat.No: T83770
Synonym: KP1 (56-87)
Target:
Tat-Gap 19 TFA
Cat.No: T83682
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
T5S0896 Loureirin A

龙血素 A,龙血素A

Akt; PI3K Cytoskeletal Signaling; PI3K/Akt/mTOR signaling
Loureirin A 是一种黄酮类物质,从龙血树中分离得到,能够降低Akt 的磷酸化,具有抗血小板聚集作用。

天然产物

Loureirin A
Cat.No: T5S0896
Synonym: 龙血素 A,龙血素A
Target: Akt, PI3K
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