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42

抑制剂 & 化合物

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天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T13231L	Trovafloxacin mesylate	Others; DNA/RNA Synthesis; Topoisomerase; Antibacterial	Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Microbiology/Virology; Others
	Trovafloxacin是一种广谱氟喹诺酮类抗生素，可阻断 DNA 促旋酶 (DNA gyrase) 和拓扑异构酶 IV (topoisomerase IV) 的活性，也是一种有效的特异性 pannexin 1 通道抑制剂 (PANX1, IC50 = 4 μM)。
T4042	Talabostat mesylate Val-boroPro,PT100	Proteasome; DPP-4	Proteases/Proteasome; Ubiquitination
	Talabostat mesylate (PT100) 是一种具有口服活性和非选择性的二肽基肽酶 IV 抑制剂(IC50< 4 nM;Ki= 0.18 nM)。Talabostat mesylate 是成纤维细胞活化蛋白的第一个临床抑制剂(IC50= 560 nM)，抑制 DPP8/9 (IC50= 4/11 nM;Ki= 1.5/0.76 nM)，静息细胞脯氨酸二肽酶(IC50= 310 nM)、DPP2 和一些其他 DASH 家族酶。Talabostat mesylate 具有抗肿瘤和造血刺激活性。
T8550	NDMC101	Others; NF-κB; Proteasome	NF-κB; Others; Proteases/Proteasome; Ubiquitination
	NDMC101 是有效的破骨细胞形成抑制剂，通过下调 NFATc1 调控基因表达抑制破骨细胞分化。它与 DPP4底物相似，通过抑制DPP4抑制早期 T 细胞激活。它能够用于骨疾病的研究，如类风湿关节炎、滑膜炎等。
T1492	Gemifloxacin mesylate LB-20304a,甲磺酸吉米沙星,SB-265805S,Gemifloxacin mesylate	DNA gyrase; Topoisomerase; Antibacterial	DNA Damage/DNA Repair; Microbiology/Virology
	Gemifloxacin mesylate (Gemifloxacin mesylate) 是一种喹诺酮类口服广谱抗菌剂，可研究轻中度肺炎和慢性支气管炎的急性细菌性发作。
T7502	PF 05089771 tosylate	Sodium Channel	Membrane transporter/Ion channel
	PF 05089771 tosylate 是口服有效的、选择性的Nav1.7丙烯酰胺抑制剂。PF 05089771 tosylate 具有用于疼痛和糖尿病神经性疾病的研究。
T36466	Chlorin E6 Ce6,Chlorin e6,CE6	Parasite	Microbiology/Virology
	Chlorin E6 (CE6) 是一种第二代光敏剂，在与辐照结合使用时具有抗肿瘤活性。在植入性纤维肉瘤的小鼠模型中，Chlorin E6（2.5-10 毫克/千克，静脉注射，50-200 焦耳/平方厘米的辐照）在不同程度的辐照后会导致肿瘤完全消失。在一项针对支气管源性早期浅表鳞状细胞癌患者的 I 期临床研究中，对包括 Chlorin E6 在内的制剂进行了测试，结果良好（40 毫克/平方米，静脉注射，100 焦耳/平方厘米的激光辐照）。在一项针对早期肺癌患者的二期临床试验中，同样的给药模式使 82.9% 的患者获得了完全应答。Chlorin E6 已被研究为一种纳米技术给药工具。
T79911	O-Benzoylhydroxylamine
	O-Benzoyloxyamine 为一种DPP-IV 抑制剂，具备抗糖尿病功能。
T26242	SW IV-52 SW-IV-52,SW IV52,SW IV 52,SWIV52
	SW IV-52 is an XIAP-inhibitor that acts as a second mitochondria-derived activator of caspases (SMAC) mimetic.
T30923	CI-1018 UNII-05127JZ9KQ
	CI-1018 is a PDE IV inhibitor that is being developed as a drug to suppress inflammation.
T68424	Revamilast
	Revamilast, also known as GRC4039, is a phosphodiesterase IV inhibitor for potentially treating of asthma and rheumatoid arthritis
T68423	Revamilast sodium
	Revamilast, also known as GRC4039, is a phosphodiesterase IV inhibitor for potentially treating of asthma and rheumatoid arthritis
T68491	Melogliptin
	Melogliptin, also known as EMD-675992 and GRC-8200, is a potent and selective a dipeptidyl peptidase IV (DPP-IV) inhibitor potentially for treatment of type II diabetes. Melogliptin significantly reduced HbA1c from baseline as compared to placebo with a mean average reduction of 0.75 percent in patients receiving 50mg twice daily dose and 0.60 percent in patients receiving 100 mg once daily dose.
T61414	DPP-4 inhibitor 3
	DPP-4 inhibitor 3 (Compound 5a) 是一种有效的二肽基肽酶 IV (DPP-IV) 抑制剂，IC50为 0.75 nM。DPP-4 inhibitor 3 具有极好的抗氧化和胰岛素性活性。
T62019	Sheng Gelieting
	Sheng Gelieting (CGT-8012) 是二肽基肽酶-IV 酶(DP-IV)抑制剂，IC50值为 87 nM。Sheng Gelieting 可用于研究二肽基肽酶-IV 酶相关的疾病，如糖尿病，特别是 II 型糖尿病。
T74810	Anti-MRSA agent 7
	Anti-MRSA agent 7 (Compound 12)作为一种抗菌剂，具有针对S. aureus DNA gyrase、E. coli DNA gyrase、S. aureus topo IV和E. coli topo IV的显著抑制效果，其IC50值分别为0.185 μM、0.365 μM、0.341 μM和0.059 μM。
T74528	DPP-4/GPR119 modulator 1
	DPP-4/GPR119 modulator 1 (Compound 22) 是一种具有口服活性的二肽基肽酶 IV (DPP-IV) 抑制剂和 GPR119激动剂。DPP-4/GPR119 modulator 1 具有降血糖作用，抑制hERG 通道，IC50值为 4.9 µM。DPP-4/GPR119 modulator 1 可用于糖尿病的研究。
T78335	Inetetamab	EGFR	Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors
	Inetetamab是一种针对HER2受体结构域IV的单克隆抗体，无论是单药使用还是联合酪氨酸激酶抑制剂，均展现出抗肿瘤活性。
T68652	Carmegliptin dihydrochloride
	Carmegliptin dihydrochloride is the salt form of Camegliptin (free base), also known as RG-1579 and RO4876904, a dipeptidyl peptidase IV (DPP-4) inhibitor potentially for the treatment of type 2 diabetes.
T30169	ASP-8497 UNII-GC7THT248G,ASP8497,ASP 8497
	ASP8497 is a potent, long-acting DPP-IV inhibitor that improves glucose tolerance by elevating GLP-1 levels in a glucose-dependent insulin-stimulating manner. The compound is used as a therapeutic agent for impaired glucose tolerance and type 2 diabetes.
T26963	CBR-2092 TNP2092,CBR2092,TNP-2092,TNP 2092
	CBR-2092 is a DNA-directed RNA polymerase and DNA topoisomerase inhibitor. CBR-2092 exhibited rifampin-like potency as an inhibitor of RNA polymerase, was an equipotent (balanced) inhibitor of DNA gyrase and DNA topoisomerase IV, and retained activity against a prevalent quinolone-resistant variant. Studies of mutant strains that exhibited reduced susceptibility to CBR-2092 further substantiated RNA polymerase as the primary cellular target of CBR-2092, with DNA gyrase and DNA topoisomerase IV b...
T21370	Amiodarone Nexterone,胺碘酮,Amiodarona,Cordarone,Aratac,Amiodaronum
	Amiodarone is categorized as a class III antiarrhythmic agent and prolongs phase 3 of the cardiac action potential. It also has numerous other effects, including actions that are similar to those of antiarrhythmic classes Ia, II, and IV. Amiodarone chemic
T78632	Z-LLY-FMK Calpain Inhibitor IV	Proteasome	Proteases/Proteasome; Ubiquitination
	Z-LLY-FMK (Calpain Inhibitor IV) 为一种钙蛋白酶抑制剂，涉及调控多个细胞系统的凋亡过程。该化合物能够抑制胆总管结扎所引起的肠细胞凋亡(apoptosis)。
T75940	Norleual TFA
	Norleual TFA 是一种血管紧张素 (Ang) IV 类似物，是一种肝细胞生长因子(HGF)/c-Met 抑制剂，IC50为 3 pM。Norleual TFA 还是一种AT4拮抗剂，具有强大的抗血管生成活性。
T70932	L6H9
	L6H9 is a novel inhibitor of myeloid differentiation factor 2 (MD2), suppressing HG-induced expression of ACE and AT1 receptor and Angiotensin II (AngII) production in renal NRK‐52E cells, resulting in the decrease in fibrosis markers such as TGF-β and collagen IV.
T80189	Hainantoxin-IV HNTX-IV	Sodium Channel	Membrane transporter/Ion channel
	Hainantoxin-IV是针对河豚毒素敏感(TTX-S)电压门控钠通道的特异性拮抗剂。该化合物以His28和Lys32为主要残基与靶标结合，并采用了抑制剂胱氨酸结基序。
T11691	IV-23	Others	Others
	IV-23, a potent inhibitor of cell growth both in vitro and in vivo, effectively reduces colony formation, arrests the cell cycle at the M phase, and induces apoptosis in esophageal squamous cell carcinoma through Noxa-mediated pathways. This compound emerges as a promising anticancer agent with significant potential.
T74331	hCAII-IN-7
	hCAII-IN-7 (Compound R-13) 是一种有效的人碳酸酐酶(hCA)抑制剂，对 hCA I、II、IV 和 IX 的 Ki 分别为 60.7、320.7 和 2298 和 35.2 nM。
T34393	Rostaporfin SnET2,tin etiopurpurin dichloride,tin ethyl etiopurpurin dichloride,Purlytin,Sn(IV) etiopurpurin
	Rostaporfin (also known as REM-001, tin ethyl etiopurpurin, Sn(IV) etiopurpurin, Purlytin, SnET2), is a synthetic purpurin with photosensitizing activity. Rostaporfin preferentially accumulates in tumor cells due to an increased rate of metabolism. Upon e
T82230	HCoV-OC43-IN-1	SARS-CoV	Microbiology/Virology
	HCoV-OC43-IN-1 (Compound IV-16) 为一种针对冠状病毒HCoV-OC43的抑制剂，展现出显著的抗病毒活性 (EC50: 90 nM)，能有效抑制病毒核衣壳蛋白 (NP) 的 mRNA 水平及其表达。
TP1404	Hemorphin-7
	Hemorphin-7 binds to the angiotensin IV receptor, triggering multiple effects including cellular proliferation and memory enhancement. Hemorphins are endogenous peptides belonging to the family of atypical opioid peptides released from hydrolyzed hemoglob
T74848	DNA Gyrase-IN-6
	Antibacterial agent 138 是细菌 DNA 促旋酶和拓扑异构酶 IV 的苯并噻唑抑制剂。Antibacterial agent 138 表现出良好的溶解度和血浆蛋白结合。Antibacterial agent 138 对革兰氏阳性和革兰氏阴性菌株具有抗菌活性。Antibacterial agent 138 是一种双重 GyrB 和 ParE 抑制剂。
T11289	Finafloxacin	Others	Others
	Finafloxacin, a fluoroquinolone antimicrobial agent from a new 8-cyano subclass, is most effective in slightly acidic environments (pH 5.0-6.0), a condition where other fluoroquinolones typically reduce in activity. It selectively targets bacterial type II topoisomerases, such as DNA gyrase and DNA topoisomerase IV, making it suitable for treating serious bacterial infections particularly in acidic contexts, including urinary tract infections (UTIs) and Helicobacter pylori infections.
T37861	Talabostat
	Talabostat (PT100, Val-boroPro) is a potent, nonselective and orally available dipeptidyl peptidase IV (DPP-IV) inhibitor with a Ki of 0.18 nM. Talabostat is a nonselective DPP-IV inhibitor, inhibiting DPP8/9, FAP, DPP2 and some other DASH family enzymes essentially as potently as it inhibits DPP-IV[1]. Talabostat stimulates the immune system by triggering a proinflammatory form of cell death in monocytes and macrophages known as pyroptosis. The inhibition of two serine proteases, DPP8 and DPP9,...
T61054	Type II topoisomerase inhibitor 1
	Type II topoisomerase inhibitor 1 可用于抗菌领域。Type II topoisomerase inhibitor 1 是大肠杆菌DNA 旋转酶的选择性抑制剂，IC50值为 1.7 nM，并能与 Asp73 残基形成氢键。Type II topoisomerase inhibitor 1 抑制拓扑异构酶 IV 的活性，IC50值为 0.98 μM。
T78219	Obtustatin triacetate	Integrin	Cytoskeletal Signaling
	Obtustatin triacetate 是一种从 Vipera lebetina obtusa 毒液中提取、含有 41 个残基的非 RGD 型解整合素。它作为整合素α1β1与 IV 型胶原蛋白粘附的高效且选择性抑制剂，能够抑制血管生成，因此在癌症研究中有应用。
T21705	8-CPT-Cyclic AMP (sodium salt)
	8-CPT-Cyclic AMP (8-CPT-cAMP) sodium 是环 AMP 依赖性蛋白激酶的选择性激活剂。 8-CPT-Cyclic AMP sodium 也是有效的环 GMP 特异性磷酸二酯酶(PDE VA)抑制剂，IC50为 0.9 μM。 8-CPT-Cyclic AMP sodium 还抑制 PDE III 和 PDE IV，IC50分别为 24 和 25 μM。8-CPT-Cyclic AMP sodium 对 Epac 具有非常高的亲和力，是一种有效的Epac 活化剂。
T79618	M3/PDE4 modulator-1
	M3/PDE4 modulator-1 (10f) 为多功能化合物，具备M3mAChR拮抗和PDE4抑制作用。于OVA大鼠模型中，M3/PDE4 modulator-1 (10-1000 nM/kg；iv) 能降低半胱氨酸嗜酸性粒细胞内流。
T35760	Carnaubadiol
	Carnaubadiol is a triterpene that has been found in E. corollata and has antiprotozoal activities.1,2 It is active against L. infantum promastigotes and amastigotes, as well as T. cruzi trypomastigotes (IC50s = 46.2, 7.8, and 14.9 μM, respectively).2 \|1. Piatak, D.M., and Reimann, K.A. Plant investigations IV. Corollatadiol A new triterpene from euphorbia corollata. Tetrahedron Lett. 13(44), 4525-4528 (1972).\|2. de Almeida, B.C., Araújo, B.Q., Carvalho, A.A., et al. Antiprotozoal activity of ext...
T35876	Chlorthalidone Impurity G
	Chlorthalidone impurity G is a potential impurity found in commercial preparations of chlorthalidone that has moderate antihypertensive effects. Chlorthalidone is a thiazide-like diuretic that inhibits the Na+/Cl- cotransporter in the distal convoluted tubule of the kidney, which prevents reabsorption of sodium and chloride leading to a reduction in plasma volume and cardiac output. It also inhibits carbonic anhydrase (CA), including the isoforms CAVB, VII, IX, XII, and XIII (Kis = 2.8-23 nM) an...
T64672	Colivelin TFA
	Colivelin (sequence SALLRSIPAPAGASRLLLLTGEIDLP) is composed of activity-dependent neurotrophic factor (ADNF) C-terminally fused to AGA-(C8R)HNG17, a potent HN derivative. It works as a neuroprotective peptide and activator of STAT3. Colivelin-induced neuroprotection has been confirmed to occur via two neuroprotective pathways: one mediated by Ca2+/calmodulin-dependent protein kinase IV, triggered by ADNF, and one mediated by signal transducer and activator of transcription 3, triggered by HN. Co...
T10462L	Bavisant dihydrochloride hydrate JNJ31001074AAC	Others	Others
	Bavisant dihydrochloride hydrate (JNJ31001074AAC) is a highly selective, orally active antagonist of the human H3 receptor with a novel mechanism of action, involving wakefulness and cognition, with potential as a treatment for ADHD. in vivo: Mean change
T64553	GLP-1(7-37) TFA salt
	The truncated glucagon-like peptides GLP-1(7-37) is naturally occurring peptide product of the preproglucagon gene that are synthesized primarily in the intestine and acts as incretin that are released from the intestine into the bloodstream in response to food and stimulate insulin secretion. GLP-1(7-37) produced a dose-related enhancement of the glucose-stimulated increase in plasma insulin concentration and an increased rate of glucose infusion in Sprague-Dawley Rats at a dosing rang of 0.5, ...

化合物

Trovafloxacin mesylate

Cat.No: T13231L

Target: Others, DNA/RNA Synthesis, Topoisomerase, Antibacterial

Talabostat mesylate

Cat.No: T4042

Synonym: Val-boroPro,PT100

Target: Proteasome, DPP-4

Cat.No: T8550

Target: Others, NF-κB, Proteasome

Gemifloxacin mesylate

Cat.No: T1492

Synonym: LB-20304a,甲磺酸吉米沙星,SB-265805S,Gemifloxacin mesylate

Target: DNA gyrase, Topoisomerase, Antibacterial

PF 05089771 tosylate

Cat.No: T7502

Target: Sodium Channel

Cat.No: T36466

Synonym: Ce6,Chlorin e6,CE6

Target: Parasite

O-Benzoylhydroxylamine

Cat.No: T79911

Cat.No: T26242

Synonym: SW-IV-52,SW IV52,SW IV 52,SWIV52

Cat.No: T30923

Synonym: UNII-05127JZ9KQ

Cat.No: T68424

Revamilast sodium

Cat.No: T68423

Cat.No: T68491

DPP-4 inhibitor 3

Cat.No: T61414

Sheng Gelieting

Cat.No: T62019

Anti-MRSA agent 7

Cat.No: T74810

DPP-4/GPR119 modulator 1

Cat.No: T74528

Cat.No: T78335

Target: EGFR

Carmegliptin dihydrochloride

Cat.No: T68652

Cat.No: T30169

Synonym: UNII-GC7THT248G,ASP8497,ASP 8497

Cat.No: T26963

Synonym: TNP2092,CBR2092,TNP-2092,TNP 2092

Cat.No: T21370

Synonym: Nexterone,胺碘酮,Amiodarona,Cordarone,Aratac,Amiodaronum

Cat.No: T78632

Synonym: Calpain Inhibitor IV

Target: Proteasome

Cat.No: T75940

Cat.No: T70932

Cat.No: T80189

Synonym: HNTX-IV

Target: Sodium Channel

Cat.No: T11691

Target: Others

Cat.No: T74331

Cat.No: T34393

Synonym: SnET2,tin etiopurpurin dichloride,tin ethyl etiopurpurin dichloride,Purlytin,Sn(IV) etiopurpurin

Cat.No: T82230

Target: SARS-CoV

Cat.No: TP1404

DNA Gyrase-IN-6

Cat.No: T74848

Cat.No: T11289

Target: Others

Cat.No: T37861

Type II topoisomerase inhibitor 1

Cat.No: T61054

Obtustatin triacetate

Cat.No: T78219

Target: Integrin

8-CPT-Cyclic AMP (sodium salt)

Cat.No: T21705

M3/PDE4 modulator-1

Cat.No: T79618

Cat.No: T35760

Chlorthalidone Impurity G

Cat.No: T35876

Cat.No: T64672

Bavisant dihydrochloride hydrate

Cat.No: T10462L

Synonym: JNJ31001074AAC

Target: Others

GLP-1(7-37) TFA salt

Cat.No: T64553

Cat. No.	Product Name	Target	Signaling Pathways
T2973	Astragaloside IV AST-IV,黄芪甲苷IV,AS-IV,黄芪皂苷 IV	MMP; ERK; Estrogen/progestogen Receptor; JNK	Endocrinology/Hormones; MAPK; Proteases/Proteasome
	Astragaloside IV (AS-IV) 是从黄芪中分离得到的一种皂苷，抑制ERK1/2和JNK 激活，在乳腺癌细胞 MDA-MB-231 中，下调(MMP)-2和(MMP)-9的信号通路。
TN2444	Batatasin IV 山药素IV,山药	Others	Others
	Batatasin IV 从 Dioscorea opposita 中鉴定出来，Dioscorea opposita 是一种同源药用植物，通常用作日常生活中的食物。
T0480	Doxofylline Doxophylline,多索茶碱	PDE; Adenosine Receptor	GPCR/G Protein; Metabolism; Neuroscience
	Doxofylline (Doxophylline) 是腺苷 A1 受体拮抗剂，且能抑制磷酸二酯酶 IV，用于治疗哮喘。
T2S2215	Crebanine	Apoptosis; Others; Akt	Apoptosis; Cytoskeletal Signaling; Others; PI3K/Akt/mTOR signaling
	Crebanine 是来自于韦诺萨千金藤的一种生物碱，通过抑制 MAPKs 和 Akt 信号通路表现出抗炎活性，还具有抗心律失常的作用。它可诱导人类癌细胞的 G1阻滞和凋亡。
TN1938	Mogroside VI 罗汉果甜苷 VI,罗汉果甜苷VI	Antifection	Microbiology/Virology
	Lo Han Kuo extract is a high intensive sweetening agent with desirable health benefits, such as prevention of dental caries through specific antibacterial properties, no-calorie levels related to obesity, and a low glycemic index to help manage blood suga

天然产物

Astragaloside IV

Cat.No: T2973

Synonym: AST-IV,黄芪甲苷IV,AS-IV,黄芪皂苷 IV

Target: MMP, ERK, Estrogen/progestogen Receptor, JNK

Cat.No: TN2444

Synonym: 山药素IV,山药

Target: Others

Cat.No: T0480

Synonym: Doxophylline,多索茶碱

Target: PDE, Adenosine Receptor

Cat.No: T2S2215

Target: Apoptosis, Others, Akt

Cat.No: TN1938

Synonym: 罗汉果甜苷 VI,罗汉果甜苷VI

Target: Antifection

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