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12

抑制剂 & 化合物

5

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
TQ0003	740 Y-P 740YPDGFR,PDGFR 740Y-P	PI3K; Autophagy	Autophagy; PI3K/Akt/mTOR signaling
	740 Y-P (740YPDGFR) 是一个细胞渗透性PI3K 激活剂。它能结合含有 p85 的 N- 和 C- 末端 SH2 结构域的 GST 融合蛋白。
T1912	Dinaciclib SCH 727965,PS-095760	Apoptosis; CDK	Apoptosis; Cell Cycle/Checkpoint
	Dinaciclib (SCH 727965) 是一种 CDK 抑制剂，抑制 CDK1、CDK2、CDK5 和 CDK9 (IC50分=3/1/1/4 nM)，具有选择性。Dinaciclib 具有潜在的抗肿瘤活性，可以抑制胸甘 (dThd) DNA 的整合。
T2503	PAC-1 Procaspase activating compound 1	Apoptosis; Caspase; Autophagy	Apoptosis; Autophagy; Proteases/Proteasome
	PAC-1 (Procaspase activating compound 1) 是一种 procaspase-3激活剂，诱导癌细胞凋亡，EC50为 2.08 μM，可用于研究淋巴瘤、黑色素瘤、实体瘤、乳腺癌和胸癌等治疗的试验。
TP2106L	Urantide acetate(669089-53-6 free base)	Neurotensin Receptor	GPCR/G Protein
	Urantide acetate(669089-53-6 free base) 是一种选择性和竞争性的 urotensin-II (UT) 受体拮抗剂 (pKB = 8.3)。体外阻断 hU-II 诱导的胸主动脉收缩。对去甲肾上腺素或内皮素 1 诱导的收缩或乙酰胆碱诱导的松弛没有影响。在钙动员测定（在表达 hUT 受体的 CHO 细胞中）中表现为部分激动剂。
T20692	Schistoflrfamide Pdvdhvflrfamide
	Schistoflrfamide is a locust myosuppressin, it is isolated from the thoracic nervous system of the locust Schistocerca gregaria.
TP2106	Urantide
	Selective and competitive urotensin-II (UT) receptor antagonist (pKB = 8.3). Blocks hU-II induced contractions in thoracic aorta ex vivo. Exhibits no effect on noradrenaline or endothelin 1-induced contraction or on acetylcholine-induced relaxation. Behav
T81782	mLR12
	mLR12为Trem1抑制肽，能显著降低BAPN诱导的胸主动脉瘤及夹层(TAAD)小鼠模型中的主动脉破裂率。
T35985	CAY10487
	The early stage of atherosclerosis is characterized by the aggregation of foam cells, so called a fatty streak, in the inner arterial wall. CAY10487 inhibits formation of fatty streak lesions of the thoracic aorta in high cholesterol-fed rabbits without affecting plasma lipid profiles or significantly inhibiting ACAT-1 or ACAT-2 activity. The percent area occupied by the atherosclerotic lesion in rabbits supplemented with 0.05% CAY10487 in the diet was 16.1% compared to 53.5% in control rabbits....
T76712	Satralizumab
	Satralizumab为一种人源化单克隆抗体，有效抑制白细胞介素-6(IL-6)。此抗体能防止dTAA在褐家鼠中的形成与发展，并可应用于视神经脊髓炎(NMOSD)及降胸主动脉动脉瘤(dTAA)的研究。
T38187	6-Aminophenanthridine
	6-Aminophenanthridine is an antiprion agent. It inhibits prion formation in yeast- and mammalian-based screening assays when used alone and, to a greater extent, when used in combination with the α2-adrenergic receptor agonist guanabenz . 6-Aminophenanthridine (300 μM) inhibits protein folding activity of the ribosome (PFAR) by directly competing with protein substrates for the active site and decreases the yield of refolded protein without affecting the refolding rate. It prevents progressive w...
T36166	8-iso-15-keto Prostaglandin F2α 8-iso-15-keto Prostaglandin F2α
	8-iso-15-keto Prostaglandin F2α (8-iso-15-keto PGF2α) is a metabolite of the isoprostane 8-iso PGF2α in rabbits, monkeys, and humans. 8-isoprostane (8-iso PGF2α) is a prostaglandin-like product of non-specific lipid peroxidation. In both humans and monkeys, exogenously infused 8-iso PGF2α is converted primarily to metabolites having 2 or 4 carbon atoms removed from the top side chain by β-oxidation. A similar pattern is observed when tritiated 8-iso PGF2α is infused into rabbits. Early in the in...
T83910	S1PL-IN-31 Sphingosine-1-Phosphate Lyase Inhibitor 31,S1PL Inhibitor 31,S1P Lyase Inhibitor 31
	S1PL-IN-31是一种鞘氨醇-1-磷酸(S1P)裂解酶的抑制剂(IC50 = 210 nM)，同时也是Smoothened(Smo)受体的对抗剂(IC50 = 440 nM)。在体内，S1PL-IN-31 (每天2 mg/kg)能够防止实验性自身免疫性脑炎(EAE)模型大鼠中，由髓鞘少突胶质细胞糖蛋白(MOG)肽段MOG29-152诱发的颈部及胸部淋巴细胞渗透和神经肌肉虚弱。该化合物降低了大鼠的淋巴细胞总数及CD4+ T细胞、CD8+ T细胞和B细胞的水平。S1PL-IN-31 (每天3及10 mg/kg剂量)在雄性和雌性大鼠心脏和淋巴结中增加了S1P水平，并且在雌性大鼠中降低了心率。

化合物

Cat.No: TQ0003

Synonym: 740YPDGFR,PDGFR 740Y-P

Target: PI3K, Autophagy

Cat.No: T1912

Synonym: SCH 727965,PS-095760

Target: Apoptosis, CDK

Cat.No: T2503

Synonym: Procaspase activating compound 1

Target: Apoptosis, Caspase, Autophagy

Urantide acetate(669089-53-6 free base)

Cat.No: TP2106L

Target: Neurotensin Receptor

Schistoflrfamide

Cat.No: T20692

Synonym: Pdvdhvflrfamide

Cat.No: TP2106

Cat.No: T81782

Cat.No: T35985

Cat.No: T76712

6-Aminophenanthridine

Cat.No: T38187

8-iso-15-keto Prostaglandin F2α

Cat.No: T36166

Synonym: 8-iso-15-keto Prostaglandin F2α

Cat.No: T83910

Synonym: Sphingosine-1-Phosphate Lyase Inhibitor 31,S1PL Inhibitor 31,S1P Lyase Inhibitor 31

Cat. No.	Product Name	Target	Signaling Pathways
T13475	β-Aminopropionitrile 3-氨基丙腈,3-Aminopropionitrile,BAPN	Others; Endogenous Metabolite	Metabolism; Others
	β-Aminopropionitrile (3-Aminopropionitrile) 是赖氨酰氧化酶的特异性抑制剂。
T5S1889	Yunaconitine Guayewuanine B,滇乌头碱	Others	Others
	Yunaconitine (Guayewuanine B) 是一种乌头类生物碱，具有剧毒。
TN1724	Harmalol hydrochloride Harmidol hydrochloride	P450; Antioxidant	Metabolism; oxidation-reduction
	Harmalol hydrochloride (Harmidol hydrochloride) 是一种可从Peganum harmala L.的种子中提取出来的β-咔啉生物碱。Harmalol hydrochloride 是Harmaline 的主要代谢产物，在转录和翻译后水平上显著抑制二恶英介导的 CYP1A1 诱导。Harmalol hydrochloride 在去氧肾上腺素或KCl 预先收缩的分离大鼠胸主动脉制剂中显示出血管松弛活性。 Harmalol hydrochloride 具有抗氧化活性.
T83596	(+)-Osbeckic acid
	(+)-Osbeckic acid，一种Tartary Buckwheat中提取的血管松弛剂，对Sprague-Dawley大鼠胸主动脉环展现出显著的血管舒张效应，其半数有效浓度(EC50)为887 μM。
TN1246	3-Deoxysappanone B	Others	Others
	3-Deoxysappanone B has vasorelaxation effects, it can mediate endothelium- independent vasodilator action in rat thoracic aortic rings.

天然产物

β-Aminopropionitrile

Cat.No: T13475

Synonym: 3-氨基丙腈,3-Aminopropionitrile,BAPN

Target: Others, Endogenous Metabolite

Cat.No: T5S1889

Synonym: Guayewuanine B,滇乌头碱

Target: Others

Harmalol hydrochloride

Cat.No: TN1724

Synonym: Harmidol hydrochloride

Target: P450, Antioxidant

(+)-Osbeckic acid

Cat.No: T83596

3-Deoxysappanone B

Cat.No: TN1246

Target: Others

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