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24

抑制剂 & 化合物

4

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T25564	K-13 K-13 (Ace inhib)
	K-13 is used as an ACE inhibitor produced by Micromonospora halophytics subsp. exilisia K-13.
T32346	K 13-004 K 13004,K13004
	K 13-004 is a lipid-lowering agent.
T79685	PI3Kα-IN-13	PI3K	PI3K/Akt/mTOR signaling
	PI3Kα-IN-13（Compound 18a）是一款高效的PI3Kα抑制剂，具有2.5 nM的IC50值。此化合物能够诱发肿瘤细胞的凋亡，并显著抑制癌细胞的增殖，具体IC50值为MCF-7细胞系0.75 μM、HCT-116细胞系3.79 μM、MDA-MB-231细胞系13.71 μM和SW620细胞系9.85 μM。此外，PI3Kα-IN-13能有效阻止肿瘤细胞集落的形成、迁移以及侵袭。
T79627	PI3Kδ-IN-13	PI3K	PI3K/Akt/mTOR signaling
	PI3Kδ-IN-13（化合物89）是一种高效的PI3Kδ抑制剂，其IC50值为2.6 nM。该化合物主要用于研究癌症、感染、炎症以及自身免疫性病变等涉及细胞增殖的疾病。
T72380	PI3K/mTOR Inhibitor-13
	PI3K/mTOR Inhibitor-13 是一种具有口服活性的磷酸肌醇 3-激酶 (PI3K) 和mTOR 激酶双重抑制剂。PI3K/mTOR Inhibitor-13 在性疾病、实体瘤和特发性肺纤维化 (IPF) 中有潜在应用。
T6443	Chloroprocaine hydrochloride 盐酸氯普鲁卡因,Chloroprocaine HCl	ATPase; Others	Membrane transporter/Ion channel; Others
	Chloroprocaine hydrochloride (Chloroprocaine HCl) 是一种 Na/K-ATPase 活性抑制剂，IC50为 13 mM，可阻断外周神经。
T35610	2,5-dimethyl Celecoxib	Apoptosis; Wnt/beta-catenin; Prostaglandin Receptor	Apoptosis; Cytoskeletal Signaling; GPCR/G Protein; Immunology/Inflammation; Stem Cells
	2,5-dimethyl Celecoxib 是塞来昔布衍生物和微粒体前列腺素 E 合酶 1 (mPGES-1) 的靶向抑制剂，mPGES-1 是炎症介质 PGE2 合成途径中的关键酶。
T60469	Chloroprocaine
	Chloroprocaine (2-Chloroprocaine) 是一种有效的Na，K-ATPase 酶活性抑制剂（IC50 = 13 mM）。Chloroprocaine 是一种阻滞外周神经的局部麻醉剂。
T38807	[Lys8, Lys9]-Neurotensin (8-13) JMV438,[Lys8, Lys9]-Neurotensin (8-13)
	[Lys8, Lys9]-Neurotensin (8-13) (JMV438) is a Neurotensin analog that elicits analgesic effects by activating the G protein-coupled receptors NTS1 and NTS2. The compound has K i values of 0.33 nM and 0.95 nM for hNTS1 and hNTS2 receptors, respectively.
T80436	Hemitoxin	Potassium Channel	Membrane transporter/Ion channel
	Hemitoxin为一种蝎毒肽，作用于K+通道阻滞剂。其能够阻断表达于非洲爪蟾卵母细胞的大鼠Kv1.1、Kv1.2和Kv1.3通道，对应IC50值为13 nM、16 nM及2 nM。
T40537	Ibuprofen Impurity K
	Ibuprofen Impurity K is a compound that serves as an impurity in Ibuprofen. Ibuprofen itself is an anti-inflammatory inhibitor specifically designed to target COX-1 and COX-2. It exhibits inhibitory activity with IC50 values of 13 μM and 370 μM for COX-1 and COX-2, respectively.
T75906	Nociceptin (1-13), amide TFA
	Nociceptin (1-13), amide TFA 是一种有效的阿片受体 ORL1 (OP4)受体激动剂，对小鼠输精管 pEC50值为 7.9，与大鼠前脑膜结合的 Ki 值为 0.75 nM。
T61980	Carbonic anhydrase inhibitor 8
	Carbonic anhydrase inhibitor 8 (compound R-13) 是一种有效的人碳酸酐酶 (hCA) 抑制剂。Carbonic anhydrase inhibitor 8抑制 hCA I、hCA II、hCA IV 的Ki 值分别为 60.7 nM、320.7 nM、2298 nM。
T74330	hCAII-IN-6
	hCAII-IN-6 (Compound S-13) 是一种有效的人碳酸酐酶 II (hCA II) 抑制剂，Ki 为 4.4 nM。hCAII-IN-6 还抑制其他 hCA 同工型 I、IV 和 IX，Ki 值分别为 9.2 nM、480.2 nM 和 14.7 nM，并可用于青光眼的研究。
T61982	Human carbonic anhydrase II-IN-2
	Human carbonic anhydrase II-IN-24 (Compound R-13) 是一种有效的人碳酸酐酶(hCA)抑制剂。Human carbonic anhydrase II-IN-24抑制 hCA I、II、IV 和 IX 的 Ki 分别为 60.7、320.7 和 2298 和 35.2 nM。
T73637	Dot1L-IN-1 TFA
	Dot1L-IN-1 TFA 是一种高效选择性Dot1L抑制剂，具有2 pM的Ki值和小于0.1 nM的IC50值。在HeLa细胞中，它能有效抑制H3K79的二甲基化（IC50=3 nM），同时也能在Molm-13细胞中抑制HoxA9启动子的活性（IC50=17 nM）。
T78954	hNTS1R agonist-1	Neurotensin Receptor	GPCR/G Protein
	hNTS1R agonist-1 (Compound 10)为能穿透血脑屏障的hNTS1R全激动剂（Ki：6.9 nM）。它能提升帕金森病（PD）模型小鼠的运动能力及记忆。作为一种Neurotensin(8-13)类似物，hNTS1R agonist-1同时具有神经保护作用。
T38021	Obafluorin
	Obafluorin is a β-lactone antibiotic that has been found in P. fluorescens.1 It is active against S. aureus, S. faecalis, K. pneumoniae, and P. vulgaris (MIC = 125 μg/ml for all). \|1. Pu, Y., Lowe, C., Sailer, M., et al. Synthesis, stability, and antimicrobial activity of (+)-obafluorin and related β-lactone antibiotics. J. Org. Chem. 59(13), 3642-3655 (1994).
T79666	WLB-89462	Sigma receptor	GPCR/G Protein
	WLB-89462（Compound 20c）是一种高选择性σ2受体配体（Ki：13 nM），展示出神经保护活性，并能有效改善由Aβ肽引发的大鼠短期记忆障碍。该化合物拥有出色的ADMET特性，包含良好的溶解度、无CYP抑制作用、优异的代谢稳定性、高渗透性、脑部可渗透性以及在啮齿类动物中经口服途径高暴露量。
T37576	Callosobruchusic Acid
	Callosobruchusic acid is an insect pheromone and monoterpene that has been found as a component of the copulation release pheromone erectin in azuki bean weevils (C. chinensis).1It induces copulation release activity in male azuki bean weevils (EC50= 6.5 ng/insect). 1.Mori, K., Ito, T., Tanaka, K., et al.Synthesis and biological activity of optically active forms of (E)-3, 7-dimethyl-2-octene-1, 8-dioic acid (callosobruchusic acid): A component of the copulation release pheromone (erectin) of th...
T36999	7(S),17(S)-dihydroxy-8(E),10(Z),13(Z),15(E),19(Z)-Docosapentaenoic Acid
	Novel oxylipins, referred to as docosanoids, have been derived from C22polyunsaturated fatty acids 7(S),17(S)-dihydroxy-8(E),10(Z),13(Z),15(E),19(Z)-Docosapentaenoic acid (7(S),17(S)-hydroxy DPA) is a DPA-derived analog of the 17(S)-dihydroxy series of docosanoids known as protectins. Protectin D1, a DHA-derived dihydroxy fatty acid, exhibits potent anti-inflammatory activities.1,2,3Potentially, 7(S),17(S)-hydroxy DPA demonstrates similar properties; however, its biological activity has yet to b...
T35814	Urocortin III (human) (trifluoroacetate salt)
	Urocortin III is a neuropeptide hormone and member of the corticotropin-releasing factor (CRF) family which includes mammalian CRF , urocortin , urocortin II , frog sauvagine, and piscine urotensin I.1 Human urocortin III shares 90, 40, 37, and 21% identity to mouse urocortin III , mouse urocortin II , human urocortin , and mouse urocortin, respectively. Urocortin III selectively binds to type 2 CRF receptors (Kis = 21.7, 13.5, and >100 nM for rat CRF2α, rat CRF2β, and human CRF1, respectively)....
T35422	5'-pApA (sodium salt)
	5'-pApA is a linearized form of cyclic di-AMP, a bacterial second messenger that activates the host innate immune system through stimulator of interferon genes (STING).1,2,3,4It is a metabolite of cyclic di-AMP formedviahydrolysis by various phosphodiesterases (PDEs).55'-pApA is intended for use as a negative control for cyclic di-AMP signaling. 1.Burdette, D.L., Monroe, K.M., Sotelo-Troha, K., et al.STING is a direct innate immune sensor of cyclic-di-GMPNature478(7370)515-518(2011) 2.Parvatiyar...
T36490	AZT triphosphate TEA
	AZT triphosphate TFA (3'-Azido-3'-deoxythymidine-5'-triphosphate TFA) is a active triphosphate metabolite of Zidovudine (AZT). AZT triphosphate TFA exhibits antiretroviral activity and inhibits replication of HIV. AZT triphosphate TFA also inhibits the DNA polymerase of HBV. AZT triphosphate TFA activates the mitochondria-mediated apoptosis pathway[1][2][3]. Treatment with 100 μM Zidovudine (AZT) for 48h disrupts the mitochondrial tubular network via accumulation of AZT triphosphate (AZT-TP) in ...

化合物

Cat.No: T25564

Synonym: K-13 (Ace inhib)

Cat.No: T32346

Synonym: K 13004,K13004

Cat.No: T79685

Target: PI3K

Cat.No: T79627

Target: PI3K

PI3K/mTOR Inhibitor-13

Cat.No: T72380

Chloroprocaine hydrochloride

Cat.No: T6443

Synonym: 盐酸氯普鲁卡因,Chloroprocaine HCl

Target: ATPase, Others

2,5-dimethyl Celecoxib

Cat.No: T35610

Target: Apoptosis, Wnt/beta-catenin, Prostaglandin Receptor

Cat.No: T60469

[Lys8, Lys9]-Neurotensin (8-13)

Cat.No: T38807

Synonym: JMV438,[Lys8, Lys9]-Neurotensin (8-13)

Cat.No: T80436

Target: Potassium Channel

Ibuprofen Impurity K

Cat.No: T40537

Nociceptin (1-13), amide TFA

Cat.No: T75906

Carbonic anhydrase inhibitor 8

Cat.No: T61980

Cat.No: T74330

Human carbonic anhydrase II-IN-2

Cat.No: T61982

Cat.No: T73637

hNTS1R agonist-1

Cat.No: T78954

Target: Neurotensin Receptor

Cat.No: T38021

Cat.No: T79666

Target: Sigma receptor

Callosobruchusic Acid

Cat.No: T37576

7(S),17(S)-dihydroxy-8(E),10(Z),13(Z),15(E),19(Z)-Docosapentaenoic Acid

Cat.No: T36999

Urocortin III (human) (trifluoroacetate salt)

Cat.No: T35814

5'-pApA (sodium salt)

Cat.No: T35422

AZT triphosphate TEA

Cat.No: T36490

Cat. No.	Product Name	Target	Signaling Pathways
T38016	Hirsutide
	Hirsutide is a cyclotetrapeptide fungal metabolite produced by the entomopathogenic fungus Hirsutella. It has antibacterial activity against C. pyogenes, S. aureus, P. aeruginosa, and K. pneumonia (MICs = 25, 13, 6, and 21 μg/cm3, respectively). Hirsutide also has antifungal activity against C. albicans, M. audouinii, A. niger, and Ganoderma (MICs = 13, 6, 25, and 6 μg/cm3, respectively).
TN2918	3-Acetoxy-8(17),13E-labdadien-15-oic acid	cAMP; Potassium Channel; Calcium Channel	GPCR/G Protein; Membrane transporter/Ion channel; Metabolism
	ent-3-Acetoxy-labda-8(17),13-dien-15-oic acid have vasorelaxant and hypotensive actions, the mechanisms underlying the cardiovascular actions of the labdane involve the activation of the endothelial NO-cGMP pathway, the opening of K+ channels and the alteration on Ca2+ mobilization.
T37272	9(S),12(S),13(S)-TriHOME
	9(S),12(S),13(S)-TriHOME is a linoleic acid-derived oxylipin that has diverse biological activities.1,2,3,4It has been found in various plants and is produced in human eosinophils in a 15-lipoxygenase-dependent, soluble epoxide hydrolase-independent manner.1,59(S),12(S)13(S)-TriHOME inhibits antigen-induced β-hexosaminidase release from RBL-2H3 mast cells (IC50= 28.7 μg/ml).2It inhibits LPS-induced nitric oxide (NO) production in BV-2 microglia (IC50= 40.95 μM).3In vivo, 9(S),12(S),13(S)-TriHOME...
T35741	Gliovirin
	Gliovirin is a fungal metabolite that has been found inT. harzianumand has fungicidal, antimicrobial and anti-inflammatory activities.1It is active against the plant pathogenic fungusP. ultimum(MIC = 60 ng/ml) and the parasiteT. brucei brucei(IC50= 90 ng/ml), but has no effect on the plant pathogenic fungiR. solani,P. omnivorum,T. basicola,R. arrhizus, andV. dahliaeor the bacteriaB. thuringiensis,P. fluorescens, andX. malvacearumwhen used at concentrations up to 1,000 ng/ml.2,3Gliovirin decrease...

天然产物

Cat.No: T38016

3-Acetoxy-8(17),13E-labdadien-15-oic acid

Cat.No: TN2918

Target: cAMP, Potassium Channel, Calcium Channel

9(S),12(S),13(S)-TriHOME

Cat.No: T37272

Cat.No: T35741

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