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18

抑制剂 & 化合物

10

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T15130	Dilazep dihydrochloride	Others	Others
	Dilazep dihydrochloride 是一种腺苷摄取的抑制剂。它可抑制缺血性损伤，血小板聚集和核苷的膜转运。它能够增强腺苷的作用，进而具有脑和冠状血管舒张作用。
T8890	653-47 hydrochloride	Epigenetic Reader Domain	Chromatin/Epigenetic
	653-47 hydrochloride 是一种增强剂，能显著增强 666-15 的 cAMP 反应元件结合蛋白 (CREB) 抑制活性。它也是 CREB 抑制剂，IC50为 26.3 μM。
T9238	KI-7	Adenosine Receptor	GPCR/G Protein; Neuroscience
	KI-7 是一种A2B 腺苷受体阳性变构调节剂。它增强选择性 A2B 腺苷受体激动剂 BAY 60-6583 和腺苷诱导的 cAMP 积累，EC50分别为 2390 nM 和 2550 nM。它也增强非选择性 A2B 腺苷受体激动剂 NECA 诱导的 cAMP 积累，EC50为 445.8 nM。
T2608	CHIR-98014 CHIR 98014,CT98014,CHIR98014	FGFR; GSK-3; Src; S6 Kinase	Angiogenesis; MAPK; PI3K/Akt/mTOR signaling; Stem Cells; Tyrosine Kinase/Adaptors
	CHIR-98014 (CT98014) 是有效的，细胞通透的GSK-3抑制剂，可抑制 GSK-3α (IC50:0.65 nM) 和 GSK-3β (IC50:0.58 nM) 的活性，对 cdc2 和 erk2 的作用较弱。
T25672	Lesopitron	5-HT Receptor	GPCR/G Protein; Neuroscience
	Lesopitron 是一种具有突触前和突触后5-HT1A 激动剂活性的抗焦虑剂，在大鼠社会交往和狨猴焦虑模型中比5-HT1A 激动剂更有效。Lesopitron 能对抗苯二氮卓类药物戒断引起的啮齿动物的焦虑且急性毒性很低，不会增强酒精或巴比妥类药物的作用。
T21320	Methoxyamine HCl 甲氧基胺盐酸盐,TRC102,TRC 102,Methoxyamine,TRC-102	Others	Others
	Methoxyamine HCl (Methoxyamine) 与脱嘌呤/脱嘧啶 (AP) DNA 损伤位点共价结合并抑制碱基切除修复 (BER)，这可能导致 DNA 链断裂和细胞凋亡增加。 Methoxyamine 是一种具有潜在佐剂活性的口服生物可利用的小分子抑制剂。该药剂可增强烷化剂的抗肿瘤活性。
T17224	VER-246608	Dehydrogenase; PDK	Metabolism; PI3K/Akt/mTOR signaling
	VER-246608 是ATP 竞争性的丙酮酸脱氢酶激酶抑制剂，对PDK-1，PDK-3，PDK-2，和PDK-4的IC50分别为 35 nM，40 nM，84 nM 和 91 nM。
T25761	Lubeluzole R 87926,R87926,R-87926,Prosynap
	Lubeluzole, a well-known neuroprotective agent, is recently proved useful to potentiate the activity of anti-cancer drugs.
T70190	Tinostamustine HCl
	Tinostamustine, also known as EDO-S101, is an alkylatlng histone-deacetylase inhibitor (HDACi) fusion molecule. EDO-S101 is a functional pan-histone-deacetylase inhibitor and is assumed to potentiate the alkylating activity of the compound and/or may help to overcome resistance to other therapeutic agents.
T68952	NU1064
	NU1064 is a potent poly(ADP-ribose) polymerase (PARP) inhibitor, which can potentiate the cytotoxicity of a panel of mechanistically diverse anti-cancer agents in L1210 cells. NU1064 potentiated a sublethal concentration of a DNA methylating agent in a concentration-dependent manner.
T71908	NU1085
	NU1085 is a potent poly(ADP-ribose) polymerase (PARP) inhibitors have been developed that potentiate the cytotoxicity of ionizing radiation and anticancer drugs. The biological effects of NU1085 [Ki = 6 nM], in combination with temozolomide (TM) or topotecan (TP) have been studied in 12 human tumor cell lines (lung, colon, ovary, and breast cancer). Cells were treated with increasing concentrations of TM or TP +/- NU1085 (10 microM) for 72 h.
T70115	Pamiparib hydrate
	Pamiparib, also known as BGB-290, is a highly potent and selective PARP inhibitor with favorable drug metabolism and pharmacokinetic properties. BGB-290 selectively binds to PARP and prevents PARP-mediated repair of single-strand DNA breaks via the base-excision repair (BER) pathway. This enhances the accumulation of DNA strand breaks, promotes genomic instability, and eventually leads to apoptosis. BGB-290 may both potentiate the cytotoxicity of DNA-damaging agents and reverse tumor cell chemo...
T74829	AcrB-IN-4
	Efflux pump-IN-4是一种针对AcrB外排泵的抑制剂，能够增强抗生素效果。该化合物通过抑制尼罗红（AcrB的已知底物）的外排来发挥作用，同时不破坏细菌外膜，且在线虫模型中未显示出毒性。
T74827	AcrB-IN-2
	Efflux pump-IN-2 是一种 AcrB 外排泵抑制剂，能够增强抗生素的作用。Efflux pump-IN-2 抑制尼罗红 (AcrB 的一种已知底物) 外排。Efflux pump-IN-2 不破坏细菌外膜，也不会在线虫模型中显示毒性。
T80234	SFNGGP-NH2
	SFNGGP-NH2是一种具有生物活性的肽。PAR-3是一种与凝血酶高亲和力结合的受体，其mRNA在人类皮肤肥大细胞中得到表达。研究指出，蛋白酶激活受体（PAR）在瘙痒反应中的作用涉及组胺依赖性及独立途径。虽然PAR-3本身不直接诱发瘙痒，却可能与PAR-4共同促发此症状。它们的共同表达可增强凝血酶的效应，这表明PAR-3单独时不进行跨膜信号传导，而是作为激活PAR-4的协同因子。
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)....
T35742	IKD-8344
	IKD-8344 is a macrocyclic dilactone originally isolated from an actinomycete species and has diverse biological activities, including anticancer, antimicrobial, and anthelmintic properties.1,2,3 It is cytotoxic to L5178Y murine leukemia cells (IC50 = 0.54 ng/ml).1 IKD-8344 inhibits growth of the mycelial form of C. albicans (MIC = 6.25 μg/ml) and potentiates the activity of polymyxin B against the multidrug-resistant pathogenic bacterium B. cenocepacia.2,3 It is active against T. spiralis in vit...
T38145	Eltoprazine
	Eltoprazine(DU28853) is a serenic or antiaggressive agent which as an agonist at the 5-HT1A and 5-HT1B receptors and as an antagonist at the 5-HT2C receptor.IC50 value:Target: 5-HT1A/1B agonist; 5-HT2C antagonistin vitro: The binding of [3H]eltoprazine to whole tissue sections was saturable and revealed an apparent dissociation constant (Kd) of 11 nM. Specific [3H]eltoprazine binding was completely displaced by 5-HT; conversely, unlabelled eltoprazine reduced [3H]5-HT binding to the levels of no...

化合物

Dilazep dihydrochloride

Cat.No: T15130

Target: Others

653-47 hydrochloride

Cat.No: T8890

Target: Epigenetic Reader Domain

Cat.No: T9238

Target: Adenosine Receptor

Cat.No: T2608

Synonym: CHIR 98014,CT98014,CHIR98014

Target: FGFR, GSK-3, Src, S6 Kinase

Cat.No: T25672

Target: 5-HT Receptor

Methoxyamine HCl

Cat.No: T21320

Synonym: 甲氧基胺盐酸盐,TRC102,TRC 102,Methoxyamine,TRC-102

Target: Others

Cat.No: T17224

Target: Dehydrogenase, PDK

Cat.No: T25761

Synonym: R 87926,R87926,R-87926,Prosynap

Tinostamustine HCl

Cat.No: T70190

Cat.No: T68952

Cat.No: T71908

Pamiparib hydrate

Cat.No: T70115

Cat.No: T74829

Cat.No: T74827

Cat.No: T80234

Urocortin III (human) (trifluoroacetate salt)

Cat.No: T35814

Cat.No: T35742

Cat.No: T38145

Cat. No.	Product Name	Target	Signaling Pathways
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。
T4893	Spermidine N-(3-Aminopropyl)-1,4-diaminobutane,亚精胺,N-(4-Aminobutyl)-1,3-diaminopropane	Endogenous Metabolite	Metabolism
	Spermidine (N-(3-Aminopropyl)-1,4-diaminobutane) 能够维持细胞膜稳定性，提高抗氧化酶活性，改善光系统 II 以及相关基因表达。它结合并激活 NMDA，并已显示以浓度依赖性方式增强 NMDA 诱导的电流。
TCS2170	2,5-Dihydroxyacetophenone Quinacetophenone,2-Acetylhydroquinone,2-5-dihydroxyacetophenone,2 '，5'-二羟基苯乙酮,Acetylhydroquinone,2,5-二羟基苯乙酮,DHAP	ERK; NF-κB; Tyrosinase	MAPK; NF-κB; Proteases/Proteasome
	2,5-Dihydroxyacetophenone (Quinacetophenone) 是从熟地黄中分离出的一种天然产物，通过阻断 ERK1/2和 NF-κB 信号通路，抑制活化巨噬细胞中炎症介质的产生。
T4A2399	Cinobufotalin 华蟾毒它灵,华蟾素	IL Receptor; Akt; MRP; P-gp	Cytoskeletal Signaling; Immunology/Inflammation; Membrane transporter/Ion channel; Neuroscience; PI3K/Akt/mTOR signaling
	Cinobufotalin 是一种从蟾蜍的皮肤分泌物中提取的强心类固醇或丁二烯内酯。它已被用作强心药，利尿药和止血药，也是潜在的抗肺癌药物。
TN5879	Edgeworin
	Edgeworin is a DNA polymerase beta (pol beta) inhibitor, it inhibits both the lyase and polymerase activities of DNA polymerase beta; it can potentiate the inhibitory action of the anticancer drug bleomycin in cultured A549 cells via an inhibition of DNA
T78486	cis-Nerolidol
	cis-Nerolidol，一种倍半萜醇，广泛存在于众多植物中，具抗氧化与抗菌活性，并能增强抗生素效果。
T81013	tert-OMe-byakangelicin
	tert-OMe-byakangelicin 是一种香豆素，能够增强肾上腺素诱导的脂肪细胞中的脂肪溶解作用，同时抑制胰岛素在脂肪细胞中刺激的甘油三酯生成。
TN5880	Mesuol
	Mesuol has antioxidant activity, it shows very high scavenging activity against DPPH radical; it also has immunomodulatory activity, can potentiate percentage neutrophil adhesion in neutrophil adhesion test in rats and phagocytosis in carbon clearance assay. Mesuol can suppress HIV-1 replication in Jurkat T cells, it inhibits TNFα-induced HIV-1-LTR transcriptional activity by targeting the nuclear factor-κB (NF-κB) pathway.
TN5414	Wallichinine
	Wallichinine shows inhibitory activity on platelet aggregation caused by platelet activating factor (PAF). Wallichinine with ABCB1 presents valuable clues for the development of novel MDR reversal reagents from natural products, wallichinine can significa
TN5153	Torilin	MMP; ERK; IκB/IKK; p38 MAPK; NF-κB; Tyrosinase; Reductase; DNA/RNA Synthesis; JNK	Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Endocrinology/Hormones; MAPK; Metabolism; NF-κB; Proteases/Proteasome
	Torilin 是一种睾酮5α还原酶抑制剂，它（IC50=31.7+/-4.23μM）对5α还原酶的抑制作用强于α-亚麻酸（IC50=160.3+/-24.62μM），但弱于非那雄胺（IC50=0.38+/-0.06μM）。Torilin 具有免疫调节、肝脏保护和抗炎特性，它通过限制 TAK1介导的 MAP 激酶和 NF-βB 活化来抑制炎症，它可以减轻关节炎的严重程度，改变 dLN 或关节中的白细胞活化，并恢复血清和脾细胞细胞因子失衡。托利林抑制α-黑素细胞刺激激素激活的 B16黑色素瘤细胞中的黑色素生成，IC（50）值为25μM。Torilin 对枯草芽孢杆菌 ATCC 6633孢子和营养细胞表现出优异的抗菌活性。Torilin 在体内和体外都具有强大的抗血管生成活性，它可能通过抑制肿瘤侵袭来抑制肿瘤发生，逆转癌细胞的多药耐药性，它可以增强阿霉素、长春碱、紫杉醇和秋水仙碱对多药耐药 KB-V1和 MCF7/ADR 细胞的细胞毒性。

天然产物

Chrysosplenol D

Cat.No: TN1493

Synonym: 猫眼草酚D

Target: IL Receptor, NF-κB, JNK

Cat.No: T4893

Synonym: N-(3-Aminopropyl)-1,4-diaminobutane,亚精胺,N-(4-Aminobutyl)-1,3-diaminopropane

Target: Endogenous Metabolite

2,5-Dihydroxyacetophenone

Cat.No: TCS2170

Synonym: Quinacetophenone,2-Acetylhydroquinone,2-5-dihydroxyacetophenone,2 '，5'-二羟基苯乙酮,Acetylhydroquinone,2,5-二羟基苯乙酮,DHAP

Target: ERK, NF-κB, Tyrosinase

Cat.No: T4A2399

Synonym: 华蟾毒它灵,华蟾素

Target: IL Receptor, Akt, MRP, P-gp

Cat.No: TN5879

Cat.No: T78486

tert-OMe-byakangelicin

Cat.No: T81013

Cat.No: TN5880

Cat.No: TN5414

Cat.No: TN5153

Target: MMP, ERK, IκB/IKK, p38 MAPK, NF-κB, Tyrosinase, Reductase, DNA/RNA Synthesis, JNK

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