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57

抑制剂 & 化合物

4

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T40222	FTO-IN-3	Others	Others
	FTO-IN-3 是一种 FTO 抑制剂，可以抑制胶质母细胞瘤干细胞自我更新。
T9089	FTO-IN-1 UUN44923	Others	Others
	UUN44923 是脂肪及肥胖相关酶(FTO) 抑制剂(IC50<1 μM)。其中FTO-IN-1 (UUN44923) 可用于研究癌症。
T40221	FTO-IN-2
	FTO-IN-2 is a FTO inhibitor that impairs self-renewal in glioblastoma stem cells.
T27393	FTO-IN-7d
	FTO-IN-7d is the first inhibitor of the RNA demethylase FTO with anticonvulsant activity.
T63740	FTO-IN-4
	FTO-IN-4 是有效的、选择性的脂肪量和肥胖相关蛋白（FTO）抑制剂。
T63843	FTO-IN-5
	FTO-IN-5 是一种有效且选择性的脂肪量和肥胖相关蛋白（FTO）抑制剂。
T82368	FTO-IN-10	Autophagy	Autophagy
	FTO-IN-10（化合物7）是一种针对人类去甲基酶FTO（脂肪量和肥胖相关蛋白）的有效抑制剂，其IC50值为4.5 μM。该化合物通过疏水作用和氢键相互作用与FTO的结构域II的结合口袋相结合。在A549细胞中，FTO-IN-10能够诱导DNA损伤和自噬性细胞死亡。
T60994	FTO-IN-6
	FTO-IN-6是脂肪量和肥胖相关蛋白（FTO）的选择性抑制剂。
T61152	FTO-IN-8
	FTO-IN-8, also known as FTO-43, is an inhibitor of N6-methyladenosine demethylase FTO (fat mass- and obesity-associated protein). It exhibits an IC50 value of 5.5 μM and displays anti-cancer cell proliferative activity [1].
T63447	FTO-IN-1 TFA
	FTO-IN-1 TFA 是脂肪和肥胖相关酶 (FTO) 抑制剂 (IC50<1 μM)。FTO-IN-1 TFA 能够用于研究癌症。
T8874	FB23	Others	Others
	FB23 是FTO 去甲基化酶选择性抑制剂(IC50:60 nM)。它能够直接与FTO 结合，选择性的抑制FTO 的 mRNA N6-甲基腺嘌呤脱甲基酶活性。
T2216	Entacapone OR-611,恩他卡朋	Transferase	Metabolism
	Entacapone (OR-611) 是可逆的、具有口服活性的、外周作用的儿茶酚-O-甲基转移酶抑制剂。它对大鼠脑、红细胞和肝脏 COMT 有抑制作用。它对 COMT 的选择性优于其他儿茶酚胺代谢酶。它抑制 FTO 去甲基化活性，可用于研究代谢紊乱。它可用于研究帕金森病。
T11990	Meclofenamic acid 甲氯芬那酸,Meclofenamate	Others; Gap Junction Protein	Cytoskeletal Signaling; Others
	Meclofenamic acid (Meclofenamate) 是一种非特异性 gap-junction 阻滞剂和特异性脂肪量和肥胖相关 (FTO) 酶抑制剂。 Meclofenamic acid 具有抗炎活性。
T30293	Bamocaftor VX-659	CFTR	Membrane transporter/Ion channel
	Bamocaftor是一种CFTR通道（DeltaF508-CFTR突变）矫正器，适用于 CF 跨膜传导调节器，被设计用于恢复 F508del-CFTR 蛋白功能。联合使用 tezacaftor 和 VX-561 治疗 F508del/MF 的囊性纤维化患者。
T6600	Naftopidil dihydrochloride KT-611,KT-611 2HCl,盐酸萘哌地尔,Naftopidil DiHCl	5-HT Receptor; Adrenergic Receptor	GPCR/G Protein; Neuroscience
	Naftopidil dihydrochloride (KT-611 2HCl) 是一种选择性的 alpha1-肾上腺素受体 (α1-adrenoceptor) 拮抗剂，对克隆的人类 α1a、α1b 和 α1d 亚型肾上腺素受体的亲和力Ki 分别为 3.7 nM、20 nM、1.2 nM。它具有抗增殖活性，可用于研究前列腺增生。
T39585	Ziftomenib KO-539	Histone Methyltransferase	Chromatin/Epigenetic
	Ziftomenib (KO-539) 是一种具有抗肿瘤活性的 menin-MLL 相互作用抑制剂，可以用于研究白血病。
TQ0077	Ceftobiprole Ro 63-9141,BAL 9141,头孢吡普	Antibacterial	Microbiology/Virology
	Ceftobiprole (Ro 63-9141) 是一种广谱头孢菌素，对甲氧西林耐受的金黄色葡萄球菌的MIC90值为 2 μg/mL。
T2588	Ivacaftor Ivacaftor (VX-770),VX-770,依伐卡托	CFTR; Autophagy	Autophagy; Membrane transporter/Ion channel
	Ivacaftor (VX-770) 是一种 CFTR 增强剂，靶向G551D-CFTR 和F508del-CFTR 的EC50分别为100 和 25 nM。
T2595	Lumacaftor 鲁玛卡托,VX-809,VRT 826809	CFTR; Autophagy	Autophagy; Membrane transporter/Ion channel
	Lumacaftor (VRT 826809) 是一种 CFTR 调节剂，可纠正 CFTR 蛋白的折叠和运输。它增强了 FRT 细胞中 F508del-CFTR 蛋白的成熟，EC50为100 nM。
T40475	Ceftobiprole medocaril BAL5788,头孢比普酯	Antibacterial	Microbiology/Virology
	Ceftobiprole medocaril (BAL5788) 是 Ceftobiprole 的前药。Ceftobiprole 是一种广谱的头孢菌素，对耐甲氧西林金黄色葡萄球菌具有活性。
T10483	Lisaftoclax Bcl-2/Bcl-xl inhibitor 1,APG-2575	BCL	Apoptosis
	Lisaftoclax (Bcl-2/Bcl-xl inhibitor 1) 是一种双重 Bcl-2 和 Bcl-xl 抑制剂(IC50：2 nM 和 5.9 nM)，具有抗肿瘤活性。
T14219	Aminaftone Aminaphthone	Endothelin Receptor	GPCR/G Protein
	Aminaftone 是 4-氨基苯甲酸的衍生物，可抑制内皮素-1 (ET-1) 的产生，可用于研究高血压和系统硬化症。
T9499	Icenticaftor QBW251	CFTR	Membrane transporter/Ion channel
	Icenticaftor (QBW251) 是一种具有口服活性CFTR 通道增强剂，可用于慢性阻塞性肺疾病 (COPD) 和囊性纤维化研究，对F508del 和G551D CFTR 的EC50分别为 79 和 497 nM。
T16681	Nesolicaftor PTI-428	CFTR; Autophagy	Autophagy; Membrane transporter/Ion channel
	Nesolicaftor (PTI-428) 特异性增强囊性纤维化跨膜电导调节蛋白合成。
T9220	Naftopidil hydrochloride 1-[4-(2-methoxyphenyl)piperazin-1-yl]-3-,萘哌地尔盐酸盐,KT-611 hydrochloride,BM-15275 hydrochloride	Adrenergic Receptor	GPCR/G Protein; Neuroscience
	Naftopidil hydrochloride (BM-15275 hydrochloride) 是一种选择性的 alpha1-肾上腺素受体 (α1-adrenoceptor) 拮抗剂，对克隆的人类 α1a、α1b 和 α1d 亚型肾上腺素受体的亲和力 Ki 分别为 3.7 nM、20 nM、1.2 nM。它具有抗增殖活性，可用于研究前列腺增生。
T2263	Tezacaftor VX661,1-(2,2-二氟-1,3-苯并二氧戊环-5-基)-N-[1-[(2R)-2,3-二羟基丙基]-6-氟-2-(2-羟基-1,1-二甲基乙基)-1H-吲哚-5-基]-环丙烷甲酰胺	CFTR; Autophagy	Autophagy; Membrane transporter/Ion channel
	Tezacaftor (VX661) 是一种小分子，可用作囊性纤维化跨膜电导调节器基因功能的校正剂。
T8877	Bonafton 1,2-萘醌,6-溴-,Bonaphthone	Antiviral	Immunology/Inflammation
	Bonafton (Bonaphthone) 是一种抗病毒剂。
T14935	Elexacaftor VX-445	CFTR; Autophagy	Autophagy; Membrane transporter/Ion channel
	Elexacaftor (VX-445) 是一种囊性纤维化跨膜电导调节因子 (CFTR) 校正剂。它促进CFTR 的加工和转运，增加细胞表面CFTR 的数量。
T30790	Ceftolozane sulfate FR 264205,FR264205,FR-264205
	Ceftolozane Sulfate may be used to treat urinary tract infections.
T75230	(Rac)-Tezacaftor
	(Rac)-Tezacaftor ((Rac)-VX-661) 是Tezacaftor 的外消旋体。Tezacaftor 是一种F508delCFTR 校正子。(Rac)-Tezacaftor 可以用于囊性纤维化的研究。
T78240	(R)-Elexacaftor (R)-VX-445	CFTR	Membrane transporter/Ion channel
	(R)-Elexacaftor，Elexacaftor (Compound 1) 的对映异构体，为囊性纤维化跨膜电导调节因子（CFTR）校正剂，其针对CFTR dF508突变体的EC50值为0.29 uM。
T13742L	Ivacaftor hydrate VX-770 hydrate	Others	Others
	Ivacaftor hydrate is an orally bioavailable CFTR potentiator. It also is used for cystic fibrosis treatment.
T39633	Navocaftor GLPG 3067,ABBV-3067
	Navocaftor, as a cystic fibrosis transmembrane regulator ( CFTR ), is a protein modulator (US 20200377491 Al, example 1).
TMIH-0568	Tezacaftor-d4 VX-661-d4
	Tezacaftor-d4 是 Tezacaftor 的氘代化合物。Tezacaftor 的 CAS 号为 1152311-62-0。VX-661 是一种小分子，可用作囊性纤维化跨膜电导调节器基因功能的校正剂。
T27098	Ivacaftor-D9 deutivacaftor,CTP-656
	CTP-656, a cystic fibrosis transmembrane conductance regulator (CFTR) channel activator, is used potentially for the treatment of cystic fibrosis.
T22252	Galicaftor	Others	Others
	ABBV-2222 is a CFTR corrector which is studied for the treatment of cystic fibrosis (CF).
T74417	Vanzacaftor
	Vanzacaftor 是一种囊性纤维化跨膜电导调节体（CFTR）的调节剂，用于研究囊性纤维化。
T72141	Ceftobiprole medocaril sodium 头孢比普酯钠盐,BAL5788 sodium
	Ceftobiprole medocaril (BAL5788) sodium 是 Ceftobiprole 的胃肠外前药。Ceftobiprole 是一种非肠道吡咯烷酮头孢菌素。Ceftobiprole 是一种广谱头孢菌素，对甲氧西林 (MRSA) 和耐万古霉素葡萄球菌 (VRSA) 和耐青霉素链球菌具有高水平的体外活性。Ceftobiprole 也抑制革兰氏阳性和革兰氏阴性病原体。
T74748	Zatonacaftor
	Zatonacaftor 是囊性纤维化跨膜调节剂(CFTR)蛋白的调节剂，主要应用于囊性纤维化的研究。
T29693	Aftobetin HCl ANCA11,NCE 11,NCE11,NCE-11
	Aftobetin, also known as ANCA11 and NCE-11, is a novel amyloid–binding compound applied topically in the form of an ophthalmic ointment. Aftobetin may be of useful as an aid in the diagnosis Alzheimer's disease.
T72860	(R)-Olacaftor (R)-VX-440
	(R)-Olacaftor ((R)-VX-440)，一种对囊性纤维化 (CF) 具有研究潜力的囊性纤维化跨膜调节因子 (CFTR) 调节剂。
T35925	(R)-Posenacaftor sodium
	(R)-Posenacaftor ((R)-PTI-801) sodium, the R enantiomer of Posenacaftor, is a cystic fibrosis transmembrane regulator (CFTR) protein modulator. It corrects the folding and trafficking of the CFTR protein, and is utilized in the research of cystic fibrosis (CF)[1].
T68866	Ceftolozane
	Ceftolozane, also known as FR-264,205 and CXA-101; is an antibiotic drug from the cephalosporin family, approved for the treatment of infections with gram-negative bacteria, or gram-positive bacteria. Ceftolozane is of great benefit due to its ability to target bacteria that have become resistant to conventional antibiotics. Ceftolozane is combined with the β-lactamase inhibitor tazobactam, as multi-drug resistant bacterial infections will generally show resistance to all β-lactam antibiotics un...
T25849	Naftoxate Naftoxatum,Naftoxato
	Naftoxate is an antimicotic. It is effective against both gram-positive and gram-negative bacteria as well as yeasts and other fungi in plant cell culture.
T0696	Naftopidil KT-611,萘哌地尔,BM-15275	Adrenergic Receptor	GPCR/G Protein; Neuroscience
	Naftopidil (KT-611) 是一种选择性的 alpha1-肾上腺素受体 (α1-adrenoceptor) 拮抗剂，对克隆的人类 α1a、α1b 和 α1d 亚型肾上腺素受体的亲和力Ki 分别为 3.7 nM、20 nM 、1.2 nM。它具有抗增殖活性，可用于研究前列腺增生。
T29693L	Aftobetin
	Aftobetin is a biochemical.
T39596	Dirocaftor PTI-808
	Dirocaftor (PTI-808) is a CFTR potentiator that augments CFTR protein function via the activation of chloride channels. Dirocaftor holds potential utility for research pertaining to cystic fibrosis (CF).
T25898	Olacaftor VX 440,VX-440,VX440
	Olacaftor, also known as VX-440, is a protein modulator of cystic fibrosis transmembrane regulator (CFTR).
T13742	Ivacaftor benzenesulfonate VX-770 benzenesulfonate	Others	Others
	Ivacaftor benzenesulfonate used for cystic fibrosis treatment. is an orally bioavailable CFTR potentiator.
T36519	Posenacaftor sodium
	Posenacaftor (PTI-801) sodium, a cystic fibrosis transmembrane regulator (CFTR) modulator, corrects CFTR protein folding and trafficking. It is utilized in researching cystic fibrosis (CF)[1].

化合物

Cat.No: T40222

Target: Others

Cat.No: T9089

Synonym: UUN44923

Target: Others

Cat.No: T40221

Cat.No: T27393

Cat.No: T63740

Cat.No: T63843

Cat.No: T82368

Target: Autophagy

Cat.No: T60994

Cat.No: T61152

Cat.No: T63447

Cat.No: T8874

Target: Others

Cat.No: T2216

Synonym: OR-611,恩他卡朋

Target: Transferase

Meclofenamic acid

Cat.No: T11990

Synonym: 甲氯芬那酸,Meclofenamate

Target: Others, Gap Junction Protein

Cat.No: T30293

Synonym: VX-659

Target: CFTR

Naftopidil dihydrochloride

Cat.No: T6600

Synonym: KT-611,KT-611 2HCl,盐酸萘哌地尔,Naftopidil DiHCl

Target: 5-HT Receptor, Adrenergic Receptor

Cat.No: T39585

Synonym: KO-539

Target: Histone Methyltransferase

Cat.No: TQ0077

Synonym: Ro 63-9141,BAL 9141,头孢吡普

Target: Antibacterial

Cat.No: T2588

Synonym: Ivacaftor (VX-770),VX-770,依伐卡托

Target: CFTR, Autophagy

Cat.No: T2595

Synonym: 鲁玛卡托,VX-809,VRT 826809

Target: CFTR, Autophagy

Ceftobiprole medocaril

Cat.No: T40475

Synonym: BAL5788,头孢比普酯

Target: Antibacterial

Cat.No: T10483

Synonym: Bcl-2/Bcl-xl inhibitor 1,APG-2575

Target: BCL

Cat.No: T14219

Synonym: Aminaphthone

Target: Endothelin Receptor

Cat.No: T9499

Synonym: QBW251

Target: CFTR

Cat.No: T16681

Synonym: PTI-428

Target: CFTR, Autophagy

Naftopidil hydrochloride

Cat.No: T9220

Synonym: 1-[4-(2-methoxyphenyl)piperazin-1-yl]-3-,萘哌地尔盐酸盐,KT-611 hydrochloride,BM-15275 hydrochloride

Target: Adrenergic Receptor

Cat.No: T2263

Synonym: VX661,1-(2,2-二氟-1,3-苯并二氧戊环-5-基)-N-[1-[(2R)-2,3-二羟基丙基]-6-氟-2-(2-羟基-1,1-二甲基乙基)-1H-吲哚-5-基]-环丙烷甲酰胺

Target: CFTR, Autophagy

Cat.No: T8877

Synonym: 1,2-萘醌,6-溴-,Bonaphthone

Target: Antiviral

Cat.No: T14935

Synonym: VX-445

Target: CFTR, Autophagy

Ceftolozane sulfate

Cat.No: T30790

Synonym: FR 264205,FR264205,FR-264205

(Rac)-Tezacaftor

Cat.No: T75230

(R)-Elexacaftor

Cat.No: T78240

Synonym: (R)-VX-445

Target: CFTR

Ivacaftor hydrate

Cat.No: T13742L

Synonym: VX-770 hydrate

Target: Others

Cat.No: T39633

Synonym: GLPG 3067,ABBV-3067

Cat.No: TMIH-0568

Synonym: VX-661-d4

Cat.No: T27098

Synonym: deutivacaftor,CTP-656

Cat.No: T22252

Target: Others

Cat.No: T74417

Ceftobiprole medocaril sodium

Cat.No: T72141

Synonym: 头孢比普酯钠盐,BAL5788 sodium

Cat.No: T74748

Cat.No: T29693

Synonym: ANCA11,NCE 11,NCE11,NCE-11

Cat.No: T72860

Synonym: (R)-VX-440

(R)-Posenacaftor sodium

Cat.No: T35925

Cat.No: T68866

Cat.No: T25849

Synonym: Naftoxatum,Naftoxato

Cat.No: T0696

Synonym: KT-611,萘哌地尔,BM-15275

Target: Adrenergic Receptor

Cat.No: T29693L

Cat.No: T39596

Synonym: PTI-808

Cat.No: T25898

Synonym: VX 440,VX-440,VX440

Ivacaftor benzenesulfonate

Cat.No: T13742

Synonym: VX-770 benzenesulfonate

Target: Others

Posenacaftor sodium

Cat.No: T36519

Cat. No.	Product Name	Target	Signaling Pathways
T3897	Isoschaftoside	Anti-infection; Antifungal	Microbiology/Virology
	Isoschaftosid 是从 Desmodium uncinatum 根部分泌物中提取的 c- 糖基黄酮类天然产物，有抗肿瘤、抗氧化和抗菌活性，它还对 M. incognita 具有很强的杀线虫活性。
T3898	Schaftoside 夏佛塔苷,APIGENIN-6-GLUCOSIDE-8-ARABINOSIDE,Shaftoside	Dynamin; Antioxidant; TLR; MyD88; Mitochondrial Metabolism; Autophagy	Autophagy; Cytoskeletal Signaling; Immunology/Inflammation; Metabolism; oxidation-reduction
	Schaftoside (APIGENIN-6-GLUCOSIDE-8-ARABINOSIDE) 是在多种中草药中发现的一种黄酮类天然产物。它抑制 TLR4 和 Myd88 表达，还降低 Drp1 表达和磷酸化，并减少线粒体分裂，具有抗氧化和抗癌活性。
TN6567	Neoschaftoside
	Neoschaftoside has antioxidant activity.
TN6779	Clausine E	Others	Others
	Clausine E 是脂肪量和肥胖相关蛋白 (FTO) 脱甲基酶活性的抑制剂。 Clausine E 与 FTO 的结合是由正熵和负焓变化驱动的。

天然产物

Cat.No: T3897

Target: Anti-infection, Antifungal

Cat.No: T3898

Synonym: 夏佛塔苷,APIGENIN-6-GLUCOSIDE-8-ARABINOSIDE,Shaftoside

Target: Dynamin, Antioxidant, TLR, MyD88, Mitochondrial Metabolism, Autophagy

Cat.No: TN6567

Cat.No: TN6779

Target: Others

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