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抑制剂 & 化合物

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天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
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。
T1606	Fasudil HA-1077,AT877,法舒地尔	ROCK; Serine/threonin kinase; Calcium Channel; PKA; PKC; Autophagy	Autophagy; Cell Cycle/Checkpoint; Chromatin/Epigenetic; Cytoskeletal Signaling; Membrane transporter/Ion channel; Metabolism; Stem Cells; Tyrosine Kinase/Adaptors
	Fasudil (HA-1077) 是一种非特异性 RhoA/ROCK 抑制剂，也是 Ca2+通道拮抗剂和血管扩张剂。它对蛋白激酶有抑制作用，ROCK1 的 Ki 值为 0.33 μM，ROCK2 和 PKA、PKC、PKG 的 IC50值分别 0.158 μM 和 4.58 μM、12.30 μM、1.650 μM。
T3060	Fasudil hydrochloride Fasudil (HA-1077) HCl,盐酸法舒地尔,HA-1077,Fasudil HCl,HA-1077 hydrochloride,AT-877	ROCK; Serine/threonin kinase; Calcium Channel; HIV Protease; PKA; PKC; Autophagy	Autophagy; Cell Cycle/Checkpoint; Chromatin/Epigenetic; Cytoskeletal Signaling; Membrane transporter/Ion channel; Metabolism; Microbiology/Virology; Proteases/Proteasome; Stem Cells; Tyrosine Kinase/Adaptors
	Fasudil hydrochloride (HA-1077) 是一种非特异性RhoA/ROCK 抑制剂，也抑制蛋白激酶，对 ROCK1、PKA、PKC 和 MLCK 的 Ki 值分别为 0.33 μM、1.0 μM、9.3 μM 和 55 μM。
T3336	Rg3039 PF-06687859	Others	Others
	Rg3039 (PF-06687859) 是一种具有口服活性、能够透过血脑屏障的DcpS 抑制剂，其IC50=0.069 nM。
T73475	SMN-C2	DNA/RNA Synthesis	Cell Cycle/Checkpoint; DNA Damage/DNA Repair
	SMN-C2 是一种选择性的 SMN2 基因剪接调节剂，是risdiplam类似物，是调节前 mRNA 剪接的选择性 RNA 结合配体，通过结合 SMN2 pre-mRNA 来发挥作用。SMN-C2 具有研究脊髓性肌萎缩症 (SMA) 的潜力。
T31168	D153249 D 153249,D-153249
	D153249 is a promoter of spinal muscular atrophy (SMA).
T35594	Cuspin-1
	The Survival of Motor Neurons (SMN) protein participates in RNA splicing. Decreases in SMN, typically a consequence of defects in the smn1 gene, result in the death of motor neurons and lead to the neurodegenerative disease, spinal muscular atrophy (SMA). Cuspin-1 is a small molecule upregulator of SMN that has been shown in vitro to increase levels of SMN in SMA patient fibroblasts by 50% at 18 μM. Its mechanism of action is thought to involve increased phosphorylation of ERK to initiate Ras-Ra...
T34664	SMN2-Stablizer-27 SMN2-Stablizer 27,SMN2 Stablizer-27
	SMN2-Stablizer-27 is a stablizer of survival of motor neuron 2 (SMN2), and a post-translationally stablizing SMN protein for the treatment of spinal muscular atrophy (SMA).
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].
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].
T62381	Branaplam hydrochloride
	Branaplam (LMI070; NVS-SM1) hydrochloride 是一种选择性的、口服具有活力的 SMN2 拼接调节剂，能够作用于 SMN (EC50: 20 nM)。Branaplam hydrochloride 能够抑制 hERG (IC50: 6.3 μM)。在严重的脊髓性肌萎缩症 (SMA) 小鼠模型中，Branaplam hydrochloride 能够增加全长 SMN 蛋白并提高其生存期。
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。
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...
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。
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。

化合物

Cat.No: T16886

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

Target: Others, Histone Methyltransferase, Antibiotic, Antifungal

Cat.No: T1606

Synonym: HA-1077,AT877,法舒地尔

Target: ROCK, Serine/threonin kinase, Calcium Channel, PKA, PKC, Autophagy

Fasudil hydrochloride

Cat.No: T3060

Synonym: Fasudil (HA-1077) HCl,盐酸法舒地尔,HA-1077,Fasudil HCl,HA-1077 hydrochloride,AT-877

Target: ROCK, Serine/threonin kinase, Calcium Channel, HIV Protease, PKA, PKC, Autophagy

Cat.No: T3336

Synonym: PF-06687859

Target: Others

Cat.No: T73475

Target: DNA/RNA Synthesis

Cat.No: T31168

Synonym: D 153249,D-153249

Cat.No: T35594

SMN2-Stablizer-27

Cat.No: T34664

Synonym: SMN2-Stablizer 27,SMN2 Stablizer-27

Cat.No: T61586

(Rac)-Indoximod

Cat.No: T60266

Branaplam hydrochloride

Cat.No: T62381

Cat.No: T63248

ATX inhibitor 11

Cat.No: T64141

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

Cat.No: T35807

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

Cat.No: T83682

Klotho-derived Peptide 1 (56-87) (human) TFA

Cat.No: T83770

Synonym: KP1 (56-87)

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

Cat.No: T5S0896

Synonym: 龙血素 A,龙血素A

Target: Akt, PI3K

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