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70

抑制剂 & 化合物

4

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T19033	Nile Red Phenoxazone 9,尼罗红,Nile Blue A oxazone	Others	Others
	Nile Red (Nile Blue A oxazone) 是一种选择性疏水性荧光染料，针对细胞内脂质小滴和中性脂质。它在所有有机溶剂中均具有强烈的荧光性，其荧光颜色范围从金黄色到深红色。
T3146	BMS-202 PD1-PDL1 inhibitor 2,PD-1/PD-L1 inhibitor 2	Apoptosis; PD-1/PD-L1	Apoptosis; Cell Cycle/Checkpoint; Immunology/Inflammation
	BMS-202 (PD1-PDL1 inhibitor 2) 是一种非肽类 PD-1/PD-L 复合物抑制剂，其 IC50为 18 nM，KD 为 8 μM。它与 PD-L1 直接结合并阻断人类 PD-1/PD-L 的相互作用，具有抗肿瘤活性。
T19507	Perfluamine FTPA,Tris(perfluoropropyl)amine,Perfluorotripropylamine	Others	Others
	Perfluamine (FTPA) 是一种疏水性载液，可用作血液替代品。
T19068	TMA-DPH	Others	Others
	TMA-DPH 是疏水性荧光膜探针 (Ex=355 nm; Em=430 nm)。
T66152	NDSB-211	Others	Others
	NDSB-211 是一种具有较小的疏水端并能温和地溶解蛋白质的表面活性剂，可用于蛋白提取和分析。
T72075	HyT36
	HyT36 是一种小分子疏水标签，可选择性的破坏稳定，促进融合蛋白和假激酶 Her3 的降解。HyT36可治疗表达 erht 的细胞诱导急性。
T37482	Diclofenac methyl ester	Others	Others
	Diclofenac methyl ester 是双氯芬酸(diclofenac)的疏水性前药形式，它是一种非甾体抗炎药 (NSAID)。它比双氯芬酸更易溶于肉豆蔻酸异丙酯，但毒性更高。
T4949	1,2-Didecanoyl-sn-glycero-3-phosphocholi 1,2-Didecanoyl Phosphatidylcholine,1,2-Didecanoyl PC,L-A-癸酰磷脂酰胆碱	Others	Others
	1,2-Didecanoyl-sn-glycero-3-phosphocholi (1,2-Didecanoyl PC) 是一种合成的、疏水性较低的磷脂，已被发现可用于增强肽类药物和激素(如胰岛素)的吸收。
T4072	Methyl-β-cyclodextrin Methyl-beta-cyclodextrin,甲基-β-环糊精,甲基倍他环糊精,beta-Cyclodextrin methyl ethers	Others	Others
	Methyl-β-cyclodextrin (Methyl-beta-cyclodextrin) 是一种大环化合物，可以作为疏水性化合物的增溶剂用于生物实验中。Methyl-β-cyclodextrin 也是一种脂筏抑制剂，具有降胆固醇活性，还具有潜在抗肿瘤活性。
T12492	Pivagabine CXB-722,匹伐加宾	GABA Receptor	Membrane transporter/Ion channel; Neuroscience
	Pivagabine (CXB-722) 是疏水性 4-氨基丁酸的衍生物，具有神经调节活性。它可穿透大鼠的血脑屏障，拮抗足部休克对大鼠脑中 GABAA 受体功能和促肾上腺皮质激素释放因子 (CRF) 浓度的影响。
T8782	MitoBloCK-11 (MB-11)	Others	Others
	MitoBloCK-11 (MB-11) 是线粒体蛋白输入的小分子抑制剂，可能通过转运蛋白 Seo1 起作用，但不通过 Tom70 或 Tom20；抑制含有疏水片段的前体蛋白，以特定方式在缺乏尿嘧啶的培养基中促进生长，并影响斑马鱼的发育。
T9103	BVDV-IN-1	DNA/RNA Synthesis	Cell Cycle/Checkpoint; DNA Damage/DNA Repair
	BVDV-IN-1 是一种牛病毒性腹泻病毒 (BVDV) 的非核苷抑制剂 (NNI)，EC50 为 1.8 μM。它直接与 BVDV RdRp 的疏水口袋结合，对耐 NNI 氨基硫脲 (TSC) 的 BVDV 具有抗病毒活性。
T8873	Bractoppin	Others; DNA/RNA Synthesis	Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Others
	Bractoppin 是一种BRCA1 (t)BRCT domain 识别磷酸肽的选择性抑制剂，IC50为 74 nM。它优先抑制 BRCA1 -tBRCT 依赖的 DNA 损伤。它减少 BRCA1 对 DNA 断裂片段的招募，进而抑制损伤诱导的 G2 期阻滞和重组酶 RAD51 的组装。
T73499	NG-497 NG497	Lipase	Metabolism
	NG-497 是一种具有选择性的小分子人类的脂肪甘油三酯脂肪酶 (ATGL) 抑制剂，可以靶向人类 ATGL 的酶促活性 patatin 样结构域。NG-497在活性位点附近的疏水腔内结合ATGL。NG-497以剂量依赖性和可逆的方式消除人脂肪细胞中的脂肪分解。NG-497 可用于研究癌症。
T35841	5-Benzyloxygramine	Dopamine Receptor; 5-HT Receptor	GPCR/G Protein; Neuroscience
	5-Benzyloxygramine 是一种 N 蛋白、蛋白互作的原位稳定剂，具有抗病毒和稳定 N-NTD 蛋白的作用。它能够阻断多巴胺受体，可拮抗 5-HT 对大鼠子宫和兔耳的作用。
T34253	Rad 242 Rad242,Rad-242
	Rad 242 is a hydrophobic lidocaine derivative.
T27529	HC-3 HC 3
	HC-3 inhibits ChoK by binding at the conserved hydrophobic groove on the C-terminal lobe.
T19730	12-Crown-4 12 C 4,12-Crown-4 ether,12C4,12-C-4
	12-Crown-4 disrupts Aβ40 fibrils. 12-Crown-4 can enter into the hydrophobic core region and form competitive, hydrophobic interactions with key hydrophobic residues.
T26087	Rilopirox
	Rilopirox is a synthetic fungicidal antimycotic with hydrophobic characteristics.
T12149	N-Me-L-Ala-maytansinol	Others	Others
	N-Me-L-Ala-maytansinol used for making antibody-drug conjugate (ADC),is a hydrophobic, cell permeable payload.
T21141	Decylene glycol Decane-1,2-diol,AI3-16595,1,2-Decanediol
	Decylene glycol is used as an antimicrobial agent in cosmetics. It also suppresses the fluidity of the hydrophobic and hydrophilic groups in the phospholipid membrane of liposomes.
T19055	RT-NH2 Real Thiol-NH2	Others	Others
	RT-NH2 is fairly hydrophobic and cannot distribute in the nucleus. It is a RealThiol prototype without the carboxylic acid groups.
TP2460	Lys-phe-phe-phe-ile-ile-trp-och3
	Lys-phe-phe-phe-ile-ile-trp-och3 is a hydrophobic peptide which reacts with lipid vesicles.
T39676	CM121 CM121
	CM121 is a reversible inhibitor of ALDH1A2 that acts specifically on the active site, exhibiting an IC50 of 0.54 μM and a Kd of 1.1 μM. It exerts its inhibitory effect through multiple hydrophobic interactions.
T31530	Disoxaril BRN 3626820,WIN51711,WIN-51711,BRN-3626820,WIN 51711,WIN-51,711
	Disoxaril (BRN 3626820, WIN 51711) is an anti-picornavirus agent that inhibits enterovirus replication by binding to a hydrophobic bag within the VP1 coat protein, thereby stabilizing virions and preventing their uncoating. When used in combination with A
TD0084	DiI triflate [1,1‘-Dioctadecyl-3,3,3’,3‘-tetramethylindocarbocyanine triflate]
	DiI, DiO, DiD and DiR dyes are a family of lipophilic fluorescent stains for labeling membranes and other hydrophobic structures. The fluorescence of these environment-sensitive dyes is greatly enhanced when incorporated into membranes or bound to lipophi
T81699	NBD-amine
	NBD-amine是荧光性质变化的胺类化合物，其在水介质中的荧光较弱，而在有机溶剂、膜结构以及疏水条件下则显著增强。
T77266	C13-112-tri-tail
	C13-112-tri-tail 是一种阳离子类脂化合物，可用于配制脂质纳米颗粒。
T77269	C13-113-tetra-tail
	C13-113-tetra-tail 是一种阳离子类脂化合物，可用于配制脂质纳米颗粒。
T80630	H-Arg-OtBu dihydrochloride	Antibiotic	Microbiology/Virology
	H-Arg-OtBu (dihydrochloride) 是一膜靶向抗菌剂，依靠电静力与疏水作用相结合，针对负电荷细菌膜。本化合物适用于细菌感染病研究之用。
T35887	MBD
	MBD, a novel fluorescent probe (7-(p-Methoxybenzylamino)-4-nitrobenz-2,1,3-oxadiazole), is utilized to study the conformation of protein and nucleoprotein. Its application is extended to bacterial ribosomes, as well as bovine trypsinogen and trypsin. MBD exhibits significant fluorescence when it binds to the hydrophobic region of macromolecules [1][2].
TD0083	DiIiodide1,1‘-Dioctadecyl-3,3,3’,3‘-tetramethylindocarbocyanine iodide] DiI碘化物
	DiI, DiO, DiD and DiR dyes are a family of lipophilic fluorescent stains for labeling membranes and other hydrophobic structures. The fluorescence of these environment-sensitive dyes is greatly enhanced when incorporated into membranes or bound to lipophilic biomolecules such as proteins although they are weakly fluorescent in water.
T76009	Thermolysin
	Thermolysin 是由革兰氏阳性菌 Bacillus thermoproteolyticus 分泌的耐热的中性金属蛋白酶。Thermolysin 可催化含有疏水残基的肽键水解。
T20937	Dodecenylsuccinic anhydride 2-十二烯基-丁二酸酐,Rikacid DDSA,Dodecenylsuccinic acid anhydride,DDSA	Others	Others
	Dodecenylsuccinic anhydride (DDSA) 可与胶原水凝胶接枝，作为疏水性伤口敷料掺入辛伐他汀后，在治疗溃疡和预防伤口感染方面具有潜在应用。
TP1341	Polymyxin B nonapeptide
	Polymyxin B nonapeptide, a cationic cyclic peptide derived by enzymatic processing from the naturally occurring peptide polymyxin B, is able to increase the permeability of the outer membrane of Gram-negative bacteria toward hydrophobic antibiotics probab
T77268	C13-112-tetra-tail
	C13-112-tetra-tail 是一种阳离子类脂化合物，可用于配制脂质纳米颗粒。
T37147	5'-O-DMT-N4-Ac-dC 5'-O-DMT-N4-Ac-dC
	5'-O-DMT-N4-Ac-dC (N4-Acetyl-2'-deoxy-5'-O-DMT-cytidine, compound 7) is a deoxynucleoside utilized in the synthesis of dodecyl phosphoramidite. Dodecyl phosphoramidite serves as a crucial precursor for dod-DNA production, which is amphiphilic DNA comprising dodecyl phosphotriester linkages and featuring an internal hydrophobic region[1][2].
T22233	Aliskiren
	Aliskiren(CGP 60536)是口服有效的肾素抑制剂，IC50为1.5 nM。
T77267	C13-113-tri-tail
	C13-113-tri tail 是一种阳离子类脂化合物，可用于配制脂质纳米颗粒。
T60775	BB 0305179
	BB 0305179 (化合物 59) 抑制疏水结构域缺失的特定 PrP 突变体的毒性，是有效的抗朊病毒剂 (IC50 = 4.7 μM)。
T63285	Antifungal agent 40
	Antifungal agent 40 是抗真菌剂，能够延伸到 C.alb.CYP51 的狭窄疏水口袋 II 中，可抑制 lanosterol 14α-demethylase (CYP51) 的活性，对生物膜的形成具有抑制作用。
T70646	Deltarasin HCl
	Deltarasin is a high affinity PDEδ-KRAS interaction inhibitor. Deltarasin can inhibit KRAS-PDEδ interactions by binding to a hydrophobic pocket on PDEδ, resulting in the impairment of cell growth, KRAS activity, and RAS/RAF signaling in human pancreatic ductal adenocarcinoma cell lines. The anti-cancer cell activity of deltarasin can be enhanced by simultaneously blocking tumor protective" autophagy
T80118	α-Synuclein (61-95) (human)
	α-Synuclein(61-95) (human) 是 α-Synuclein 的疏水核心区段，具有诱导神经元死亡的能力。该肽段在神经退行性疾病的研究中有应用，涉及阿尔茨海默病 (AD) 与帕金森病 (PD)。
T75878	Catestatin TFA
	Catestatin TFA，一个含有21个氨基酸残基、阳离子性疏水性肽，作为内源性肽，调节心脏功能及血压。它通过烟碱型乙酰胆碱受体(nAChRs)以非竞争性方式抑制儿茶酚胺释放，功能为烟碱类拮抗剂。
T83936	LL-K9-3
	LL-K9-3是一种基于选择性疏水标记技术（HyT）的CDK9-cyclin T1复合物降解剂（DC50值分别为cyclin T1的589 nM和CDK9的662 nM）。它由CDK9抑制剂SNS 032和一个糖基连接器连接到疏水标记组成。LL-K9-3不会降解其他CDKs（CDK1、2、4、5、6和7）。在22RV1细胞中，LL-K9-3通过诱导CDK9和cyclin T1的选择性和同步降解，降低雄激素受体（AR）和cMyc的表达。
T69911	CU-6PMN
	CU-6PM is a new fluorescent RXR agonist. CU-6PMN was designed based on the fact that umbelliferone emits strong fluorescence in a hydrophilic environment, but the fluorescence intensity decreases in hydrophobic environments such as the interior of proteins. The developed assay CU-6PMN enabled screening of rexinoids to be performed easily within a few hours by monitoring changes of fluorescence intensity with widely available fluorescence microplate readers, without the need for processes such a...
T78387	5-Dodecanoylaminofluorescein
	5-Dodecanoylaminofluorescein为亲脂性荧光探针，属于游离脂肪酸的荧光素衍生物。该探针应用于膜流动性分析与洗涤剂临界胶束浓度测定，并可用于制备药物递送用的疏水性纳米球。
T64037	CYP3A4-IN-2
	CYP3A4-IN-2 是细胞色素 P450 3A4 (CYP3A4) (cytochrome P450 3A4 (CYP3A4)) 的特异性抑制剂 (IC50: 0.055 μM)。CYP3A4-IN-2 是利托那韦类似物，与利托那韦相比，其 R2 侧基的疏水性更高，抑制作用更强。CYP3A4-IN-2 能够作为免疫抑制剂及抗病毒剂。
T77284	DSPE-NHS
	DSPE-NHS 是一种具有两个疏水性脂质尾巴的生物共轭磷脂分子。DSPE-NHS 是一种在水溶液中形成脂质双分子层的自组装试剂。DSPE-NHS 可用于制备脂质体作为活性分子纳米载体。
T78740	α-Glucosidase-IN-28	Glucosidase	Metabolism
	α-Glucosidase-IN-28（Compound 18）是一种有效的α-Glucosidase抑制剂，具有IC50为0.62 μM和Ki为3.93μM。该化合物通过与α-Glucosidase的OBS区域结合以及与周围氨基酸建立多重疏水作用力，展现抑制活性。它主要用于研究糖尿病及其相关疾病。

化合物

Cat.No: T19033

Synonym: Phenoxazone 9,尼罗红,Nile Blue A oxazone

Target: Others

Cat.No: T3146

Synonym: PD1-PDL1 inhibitor 2,PD-1/PD-L1 inhibitor 2

Target: Apoptosis, PD-1/PD-L1

Cat.No: T19507

Synonym: FTPA,Tris(perfluoropropyl)amine,Perfluorotripropylamine

Target: Others

Cat.No: T19068

Target: Others

Cat.No: T66152

Target: Others

Cat.No: T72075

Diclofenac methyl ester

Cat.No: T37482

Target: Others

1,2-Didecanoyl-sn-glycero-3-phosphocholi

Cat.No: T4949

Synonym: 1,2-Didecanoyl Phosphatidylcholine,1,2-Didecanoyl PC,L-A-癸酰磷脂酰胆碱

Target: Others

Methyl-β-cyclodextrin

Cat.No: T4072

Synonym: Methyl-beta-cyclodextrin,甲基-β-环糊精,甲基倍他环糊精,beta-Cyclodextrin methyl ethers

Target: Others

Cat.No: T12492

Synonym: CXB-722,匹伐加宾

Target: GABA Receptor

MitoBloCK-11 (MB-11)

Cat.No: T8782

Target: Others

Cat.No: T9103

Target: DNA/RNA Synthesis

Cat.No: T8873

Target: Others, DNA/RNA Synthesis

Cat.No: T73499

Synonym: NG497

Target: Lipase

5-Benzyloxygramine

Cat.No: T35841

Target: Dopamine Receptor, 5-HT Receptor

Cat.No: T34253

Synonym: Rad242,Rad-242

Cat.No: T27529

Synonym: HC 3

Cat.No: T19730

Synonym: 12 C 4,12-Crown-4 ether,12C4,12-C-4

Cat.No: T26087

N-Me-L-Ala-maytansinol

Cat.No: T12149

Target: Others

Decylene glycol

Cat.No: T21141

Synonym: Decane-1,2-diol,AI3-16595,1,2-Decanediol

Cat.No: T19055

Synonym: Real Thiol-NH2

Target: Others

Lys-phe-phe-phe-ile-ile-trp-och3

Cat.No: TP2460

Cat.No: T39676

Synonym: CM121

Cat.No: T31530

Synonym: BRN 3626820,WIN51711,WIN-51711,BRN-3626820,WIN 51711,WIN-51,711

DiI triflate [1,1‘-Dioctadecyl-3,3,3’,3‘-tetramethylindocarbocyanine triflate]

Cat.No: TD0084

Cat.No: T81699

C13-112-tri-tail

Cat.No: T77266

C13-113-tetra-tail

Cat.No: T77269

H-Arg-OtBu dihydrochloride

Cat.No: T80630

Target: Antibiotic

Cat.No: T35887

DiIiodide1,1‘-Dioctadecyl-3,3,3’,3‘-tetramethylindocarbocyanine iodide]

Cat.No: TD0083

Synonym: DiI碘化物

Cat.No: T76009

Dodecenylsuccinic anhydride

Cat.No: T20937

Synonym: 2-十二烯基-丁二酸酐,Rikacid DDSA,Dodecenylsuccinic acid anhydride,DDSA

Target: Others

Polymyxin B nonapeptide

Cat.No: TP1341

C13-112-tetra-tail

Cat.No: T77268

5'-O-DMT-N4-Ac-dC

Cat.No: T37147

Synonym: 5'-O-DMT-N4-Ac-dC

Cat.No: T22233

C13-113-tri-tail

Cat.No: T77267

Cat.No: T60775

Antifungal agent 40

Cat.No: T63285

Cat.No: T70646

α-Synuclein (61-95) (human)

Cat.No: T80118

Cat.No: T75878

Cat.No: T83936

Cat.No: T69911

5-Dodecanoylaminofluorescein

Cat.No: T78387

Cat.No: T64037

Cat.No: T77284

α-Glucosidase-IN-28

Cat.No: T78740

Target: Glucosidase

Cat. No.	Product Name	Target	Signaling Pathways
T8032	4-Pentenoic acid	Others; Endogenous Metabolite	Metabolism; Others
	4-Pentenoic acid 是内源性代谢产物的一种。
T4889	2,6-Diaminoheptanedioic acid	Others; Endogenous Metabolite	Metabolism; Others
	2,6-Diaminoheptanedioic acid 是内源性代谢产物的一种。
T8098	γ-Hexalactone γ-caprolactone,gamma-己内酯,γ-己内酯	Others	Others
	γ-Hexalactone (γ-caprolactone) 是一种存在成熟水果中的 gamma 内酯。它会导致 DNA 损伤，可用作对氧磷酶 1 的底物 (PON1)。
T36439	Gramicidin A	Antibacterial; HIF; Parasite	Angiogenesis; Chromatin/Epigenetic; Microbiology/Virology
	Gramicidin A 是一种从从 B. brevis 分离出来的多肽类抗生素。Gramicidin A 是一种高度疏水的通道形成离子载体，在人工膜中形成一价阳离子可渗透的通道。Gramicidin A 诱导缺氧诱导因子 1α (HIF-1α) 的降解，并能降低人肾细胞癌小鼠异种移植模型的生长。Gramicidin A 具有抗菌、抗疟活性以及溶血活性。

天然产物

4-Pentenoic acid

Cat.No: T8032

Target: Others, Endogenous Metabolite

2,6-Diaminoheptanedioic acid

Cat.No: T4889

Target: Others, Endogenous Metabolite

Cat.No: T8098

Synonym: γ-caprolactone,gamma-己内酯,γ-己内酯

Target: Others

Cat.No: T36439

Target: Antibacterial, HIF, Parasite

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