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27

抑制剂 & 化合物

6

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T14076	A 839977 A839977,A-839977	P2X Receptor; Calcium Channel	Membrane transporter/Ion channel; Metabolism; Neuroscience
	A 839977是一种选择性 P2X7 受体拮抗剂,具有抗炎和镇痛活性，可抑制 P2X7 受体的 BzATP 诱发的钙内流，可用于研究肾纤维化 .
T3525	PD150606	Cysteine Protease	Proteases/Proteasome
	PD150606 是一种具有选择性的非肽 calpain 抑制剂，具有神经保护活性，抑制 μ-calpains 和 m-calpains ，抑制红藻氨酸诱导的 Ca2+ 内流，干扰兴奋性毒性依赖性运动神经元死亡。
T12343	Benzquinamide BZQ,P2647,Benzoquinamide	Adrenergic Receptor	GPCR/G Protein; Neuroscience
	Benzquinamide (P2647) 是一种具有抗癌活性的止吐剂, 抑制p糖蛋白介导的药物外排，增强多重耐药细胞中抗癌药物的细胞毒性。Benzquinamide 对 α2A, α2B, 以及α2C 肾上腺素能受体（α2-AR）的 Ki值分别为 1,365, 691 和 545 nM。
T0939	Phenytoin 苯妥英,Diphenylhydantoin,5,5-Diphenylhydantoin	Virus Protease; Sodium Channel	Membrane transporter/Ion channel; Microbiology/Virology
	Phenytoin (5,5-Diphenylhydantoin) 是一种有效的电压门控钠离子通道阻滞剂，可减少小鼠乳腺肿瘤的生长和转移，具有抗癫痫活性。
T1433	Ritodrine hydrochloride DU21220,盐酸利托君,Ritodrine HCl,NSC 291565	Adrenergic Receptor	GPCR/G Protein; Neuroscience
	Ritodrine hydrochloride (NSC 291565) 是一种 β-2肾上腺素受体激动剂。
T10944	D13-9001	Others	Others
	The KD values of D13-9001 in Escherichia coli and Pseudomonas aeruginosa were 1.15μM and 3.57μM, respectively. D13-9001 has antibiotic activity. It is an effective AcrB (AcrAB-TolC efflux pump subunit) and MexB (MexAB-OprM efflux pump subunit) inhibitor.
T37296	GI-530159
	TREK1 and TREK2 channel activator (EC50 = 0.76 μM in Rb efflux assay in TREK1-expressing CHO cells). Exhibits selectivity for TREK1/2 over TRAAK, TASK3 and a range of other potassium channels. Hyperpolarizes membrane potential of dorsal root ganglion neurons and depresses neuronal activity in vitro. Loucif et al (2018) GI-530159, a novel, selective, mechanosensitive two-pore-domain potassium (K2P) channel opener, reduces rat dorsal root ganglion neuron excitability. Br.J.Pharmacol. 175 2272 PMID...
T69956	KR30031
	KR30031 is a novel P-glycoprotein inhibitor with potential anticancer activity. KR30031 is a verapamil analog with fewer cardiovascular effects. The ability of KR-30031 to reduce this efflux transport is equal to that of verapamil, a well-known P-glycoprotein inhibitor. The bioavailability of paclitaxel could be enhanced by coadministration of a P-glycoprotein inhibitor, KR-30031.
T69139	Thalicarpine
	Thalicarpine is a natural aporphine benzylisoquinoline vinca alkaloid with antineoplastic activity. Thalicarpine binds to and inhibits p-glycoprotein, the multidrug resistance efflux pump. Thalicarpine also induces single-strand breaks in DNA and arrests cancer cells at the G2/M and G1 phase of the cell cycle. Check for active clinical trials or closed clinical trials using this agent.
T69480	Sagopilone
	Sagopilone is a fully synthetic low-molecular-weight epothilone with potential antineoplastic activity. Sagopilone binds to tubulin and induces microtubule polymerization while stabilizing microtubules against depolymerization, which may result in the inhibition of cell division, the induction of G2/M arrest, and apoptosis. The agent is not a substrate for the P-glycoprotein (P-gp) efflux pump and so may exhibit activity in multidrug-resistant (MDR) tumors. The epothilone class of metabolites wa...
T60291	β-Nor-lapachone
	β-Nor-lapachone 是一种光滑念珠菌 (Candida glabrata)的抗生物膜剂。β-Nor-lapachone 能刺激ROS 的产生，抑制光念珠菌的外排活性、粘附、生物膜形成和成熟生物膜代谢。β-Nor-lapachone 具有抗真菌活性。
T28648	S39625 S-39625,S 39625
	S39625, an E-ring camptothecin keto analogue, is a stable, potent, and selective topoisomerase I inhibitor without being substrates of drug efflux transporters. Nanomolar concentrations of S39625 induces intense and persistent histone gamma-H2AX. The chem
T27211	DS-8587 DS 8587,DS8587,DS-8587 free
	DS-8587 is a DNA topoisomerase inhibitor. DS-8587 exhibits potent antibacterial activity against quinolone-resistant A. baumannii isolates that harbor mutations in quinolone resistance-determining regions. DS-8587 significantly reduces the number of viabl
T35568	BODIPY-aminoacetaldehyde diethyl acetal
	BODIPY-aminoacetaldehyde diethyl acetal (BAAA-DA) is a stable precursor to BODIPY-aminoacetaldehyde, a cell-permeable fluorescent substrate for aldehyde dehydrogenase (ALDH).1,2BODIPY-aminoacetaldehyde diethyl acetal is converted under acidic conditions to BODIPY-aminoacetaldehyde (BAAA).2BAAA is cell-permeant and is converted intracellularly by ALDH to BODIPY aminoacetate (BAA), which is retained by cells and can be used to identify cells with high ALDH activity.1BAA is a substrate for the effl...
T63982	Anticancer agent 50
	Anticancer agent 50 (compound 6) 是 ABCB1 外排泵的有效调节剂，具有细胞毒活性和抗增殖活性。Anticancer agent 50 能够减少细胞周期蛋白 D1 的表达，并诱导 p53 表达。Anticancer agent 50 对 T 淋巴瘤表现出研究潜力。
T71577	KOS-1584
	KOS-1584 is a second-generation epothilone with potential antineoplastic activity. Epothilone KOS-1584 binds to tubulin and induces microtubule polymerization and stabilizes microtubules against depolymerization, which may result in the inhibition of cell division, the induction of G2/M arrest, and apoptosis. Compared to first-generation epothilones, this agent exhibits greater safety and efficacy with an enhanced pharmaceutical profile, including enhanced water solubility and tumor penetration,...
T35902	Milbemycin A4 oxime
	Milbemycin A4 oxime is a derivative of milbemycin A4 and a component of milbemycin oxime , compounds that both have insecticidal and nematocidal activity. Milbemycin A4 oxime (0.05 mg/kg) reduces the number of microfilariae of the heartworm D. immitis in naturally infested dogs. It inhibits the growth of clinical isolates of C. glabrata with MIC80 values ranging from 16 to greater than 32 μg/ml. Milbemycin A4 oxime (2.5 μg/ml) blocks efflux of fluconazole from a clinical isolate of C. glabrata, ...
T71266	Omadacycline HCl
	Omadacycline, also known as PTK 0796 and Amadacyclin, is a novel first-in-class aminomethylcycline with potent activity against important skin and pneumonia pathogens, including community-acquired methicillin-resistant Staphylococcus aureus (MRSA), β-hemolytic streptococci, penicillin-resistant Streptococcus pneumoniae, Haemophilus influenzae, and Legionella. Omadacycline is active against strains expressing the two main forms of tetracycline resistance (efflux and ribosomal protection). The pri...
T79261	P-gp inhibitor 15
	P-gp inhibitor 15 (compound 7a) 是一种Pgp-非底物抑制剂，能够抑制Pgp-ATP酶的活性并干扰罗丹明123的Pgp介导外流。此外，P-gp inhibitor 15能增强紫杉醇的抗肿瘤效果，有效抑制裸鼠KBV异种移植肿瘤模型的肿瘤生长。
T70808	Cabazitaxel-d6
	Cabazitaxel-d6 is a deuterium labeled cabazitaxel. Cabazitaxel is a semi-synthetic derivative of the natural taxoid 10-deacetylbaccatin III with potential antineoplastic activity. Cabazitaxel binds to and stabilizes tubulin, resulting in the inhibition of microtubule depolymerization and cell division, cell cycle arrest in the G2/M phase, and the inhibition of tumor cell proliferation. Unlike other taxane compounds, this agent is a poor substrate for the membrane-associated, multidrug resistance...
T69305	Milataxel
	Milataxel is an orally bioavailable taxane with potential antineoplastic activity. Upon oral administration, milataxel and its major active metabolite M-10 bind to and stabilize tubulin, resulting in the inhibition of microtubule depolymerization and cell division, cell cycle arrest in the G2/M phase, and the inhibition of tumor cell proliferation. Unlike other taxane compounds, milataxel appears to be a poor substrate for the multidrug resistance (MDR) membrane-associated P-glycoprotein (P-gp) ...
T68480	4SC-207
	4SC-207 is a novel microtubule inhibitor , which shows strong anti-proliferative activity in a large panel of tumor cell lines with an average GI50 of 11 nM. In particular, 4SC-207 is active in multi-drug resistant cell lines, such as HCT-15 and ACHN, suggesting that it is a poor substrate for drug efflux pumps. 4SC-207 inhibits microtubule growth in vitro and in vivo and promotes, in a dose dependent manner, a mitotic delay/arrest, followed by apoptosis or aberrant divisions due to chromosome a...
T35633	Pinolenic Acid ethyl ester
	Pinolenic acid is a polyunsaturated fatty acid found in Korean pine (Pinus orientalis) and maritime pine (Pinus pinaster) seed oils. Both oils have been found to have lipid-lowering properties. A diet containing maritime pine seed oil (MPSO) lowered high-density lipoprotein and ApoA1 levels in transgenic mice expressing human ApoA1. MPSO was found to diminish cholesterol efflux in vitro. Korean pine seed oil supplements may help in obesity by reduction of appetite. People taking this oil had an ...
T36554	TMB 8 (hydrochloride)
	TMB 8 is a non-competitive antagonist of nicotinic acetylcholine receptors (nAChRs) with IC50 values of 390 and 350 nM, respectively, for human muscle-type and α3β4 subunit-containing ganglionic nAChRs expressed in TE671/RD or SH-SY5Y cells. It inhibits nicotine-induced dopamine release from rat brain synaptosomes (IC50 = 480 nM). TMB 8 also reduces calcium availability in smooth and skeletal muscle, blocking the contractile response in isolated rabbit aortic strip when used at a concentration o...
T35632	Pinolenic Acid
	Pinolenic acid is a polyunsaturated fatty acid found in Korean pine (Pinus orientalis) and maritime pine (Pinus pinaster) seed oils. Both oils have been found to have lipid-lowering properties. A diet containing maritime pine seed oil (MPSO) lowered HDL and ApoA1 levels in transgenic mice expressing human ApoA1. MPSO was found to diminish cholesterol efflux in vitro.[1] Korean pine seed oil supplements may help in obesity by reduction of appetite. People taking this oil had an increase in the sa...
T79384	Antifungal agent 72
	Antifungalagent 72（Compound B8）是一款高效抗真菌药物。该化合物通过抑制Pdr1-KIX相互作用（Ki：11.7μM）来干扰外排泵功能，并降低与耐药性相关的基因表达。Antifungalagent 72对抗氟康唑（Fluconazole）耐药的C. glabrata 0161菌株显示出显著的抗菌活性，其MIC值为63 ng/mL，并与氟康唑合用时表现出协同效果。此化合物可应用于C. glabrata感染的相关研究。
T36659	Boromycin
	Boromycin is a boron-containing macrolide antibiotic that has been found in Streptomyces. Boromycin inhibits growth of B. subtilis (MIC = 0.05 μg/ml) and induces efflux of potassium ions from B. subtilis without affecting Na+/K+-ATPase activity. It decreases the synthesis of protein, RNA, and DNA in B. subtilis when used at a concentration of 0.05 μg/ml. It inhibits the growth of B. halodurans (MIC = 10 ng/ml) and inhibits the futalosine pathway of menaquinone synthesis in B. halodurans. Boromyc...

化合物

Cat.No: T14076

Synonym: A839977,A-839977

Target: P2X Receptor, Calcium Channel

Cat.No: T3525

Target: Cysteine Protease

Cat.No: T12343

Synonym: BZQ,P2647,Benzoquinamide

Target: Adrenergic Receptor

Cat.No: T0939

Synonym: 苯妥英,Diphenylhydantoin,5,5-Diphenylhydantoin

Target: Virus Protease, Sodium Channel

Ritodrine hydrochloride

Cat.No: T1433

Synonym: DU21220,盐酸利托君,Ritodrine HCl,NSC 291565

Target: Adrenergic Receptor

Cat.No: T10944

Target: Others

Cat.No: T37296

Cat.No: T69956

Cat.No: T69139

Cat.No: T69480

β-Nor-lapachone

Cat.No: T60291

Cat.No: T28648

Synonym: S-39625,S 39625

Cat.No: T27211

Synonym: DS 8587,DS8587,DS-8587 free

BODIPY-aminoacetaldehyde diethyl acetal

Cat.No: T35568

Anticancer agent 50

Cat.No: T63982

Cat.No: T71577

Milbemycin A4 oxime

Cat.No: T35902

Omadacycline HCl

Cat.No: T71266

P-gp inhibitor 15

Cat.No: T79261

Cat.No: T70808

Cat.No: T69305

Cat.No: T68480

Pinolenic Acid ethyl ester

Cat.No: T35633

TMB 8 (hydrochloride)

Cat.No: T36554

Cat.No: T35632

Antifungal agent 72

Cat.No: T79384

Cat.No: T36659

Cat. No.	Product Name	Target	Signaling Pathways
T19768	γ-Tocotrienol gamma Tocotrienol,gammaTocotrienol,gamma-Tocotrienol,D-gamma-Tocotrienol,Plastochromanol,γ-生育三烯酚	Others	Others
	γ-Tocotrienol (Plastochromanol) 是一种维生素 E 的活性形式。
TN1493	Chrysosplenol D 猫眼草酚D	IL Receptor; NF-κB; JNK	Immunology/Inflammation; MAPK; NF-κB
	Chrysosplenol D 属于甲氧基黄酮类化合物，可诱导 ERK1/2 介导的三阴性人乳腺癌细胞凋亡。它还显示出抗炎和中等抗锥虫活性。
TN2160	Roemerine (-)-Roemerine	Antibiotic	Microbiology/Virology
	Roemerine ((-)-Roemerine) 是一种来自塞内加尔番荔枝的卟啉生物碱，具有抗真菌和抗癌活性，通过抑制 Bmr 来防止小檗碱外排。Roemerine 以浓度依赖性方式增加细胞膜通透性，可用于研究真菌感染和前列腺癌。
TN5466	Boeravinone B
	Boeravinone B, a novel efflux pump inhibitor, apart from inhibiting the MdeA mediated efflux, also significantly inhibit the biofilm formation of S. aureus, boeravinone B may be used in combination with mupirocin for further development. Boeravinone B exh
T80001	Majoranaquinone	Antibiotic	Microbiology/Virology
	Majoranaquinone对4种Staphylococcus菌株、1种Moraxella菌株和1种Enterococcus菌株显示出良好的抑菌作用。此外，Majoranaquinone在E.coli ATCC 25922菌株中表现出显著的外排泵抑制活性，并能有效抑制E.coli ATCC 25922和E.coli K-12 AG100的生物膜形成。
TN5474	Bonducellin
	Bonducellin has anti-inflammatory activities, it can significantly and dose-dependently inhibit the inflammatory mediators; nitric oxide (NO), and cytokines [tumor necrosis factor (TNF)-alpha and interleukin (IL)-12. Bonducellin shows weak antimalarial ac

天然产物

Cat.No: T19768

Synonym: gamma Tocotrienol,gammaTocotrienol,gamma-Tocotrienol,D-gamma-Tocotrienol,Plastochromanol,γ-生育三烯酚

Target: Others

Chrysosplenol D

Cat.No: TN1493

Synonym: 猫眼草酚D

Target: IL Receptor, NF-κB, JNK

Cat.No: TN2160

Synonym: (-)-Roemerine

Target: Antibiotic

Cat.No: TN5466

Majoranaquinone

Cat.No: T80001

Target: Antibiotic

Cat.No: TN5474

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