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47

抑制剂 & 化合物

8

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T7317	CU-CPT-9a	TLR	Immunology/Inflammation
	CU-CPT-9a 是TLR8特异性拮抗剂，IC50值为 0.5 nM。
T27076	8-Cyclopentyl-1,3-dimethylxanthine CPT,A1受体拮抗剂,CPT	Adenosine Receptor	GPCR/G Protein; Neuroscience
	8-Cyclopentyl-1,3-dimethylxanthine (CPT) 是一种选择性的腺苷A1受体拮抗剂，对 A1 受体和 A2 受体的Ki 值分别为 10.9 和 1440 nM。
T22698	TLR3-IN-1 CU CPT 4a	TLR	Immunology/Inflammation
	TLR3-IN-1 (CU CPT 4a) 是一种选择性的TLR3信号抑制剂，在 RAW 264.7 细胞中 IC50 为 3.44 μM。它可以抑制 TLR3/dsRNA 复合物介导的下游信号通路，并抑制全细胞中 TNF-α 和 IL-1β 的产生。
T7347	CU-CPT-8m TLR8-specific antagonist	TLR	Immunology/Inflammation
	CU-CPT-8m (TLR8-specific antagonist) 是TLR8特异性拮抗剂，IC50值为 67 nM。
T7302	CU-CPT9b CU-CPT-9b,TLR8-specific antagonist 1	TLR	Immunology/Inflammation
	CU-CPT9b (TLR8-specific antagonist 1) 是 toll 样受体 8 (TLR8) 的拮抗剂，Kd 为 21 nM。它抑制由 TLR8 激动剂 R-848 在过表达 TLR8 的 HEK-Blue 细胞中诱导的 NF-ĸB 活化，IC50 值为 0.7 nM。
T24610	Pegamotecan Prothecan,PEG-camptothecin,PEG-beta-CPT	Topoisomerase	DNA Damage/DNA Repair
	Pegamotecan (PEG-camptothecin)是一种拓扑异构酶I(TOP1)抑制剂，具有抗癌活性，它可用于治疗食管癌、非小细胞肺癌和胰腺癌。
T41018	CPT-157633
	CPT-157633 is a difluoro-phosphonomethyl phenylalanine derivative that acts as a potent inhibitor of the enzyme PTP1B. It effectively prevents the development of glucose intolerance induced by binge drinking.
T38696	Rp-8-CPT-cAMPS
	Rp-8-CPT-cAMPS is a powerful and competitive antagonist of cAMP-induced activation of cAMP-dependent protein kinase (PKA) I and II. Acting as a potent cAMP analog, Rp-8-CPT-cAMPS exhibits a preference for site A of RI over site A of RII. Additionally, it favors site B of RII over site B of RI. This compound effectively inhibits cAMP-dependent PKA activation and demonstrates selectivity in binding to specific sites within the protein kinase.
T10899	CU-CPT17e	TLR	Immunology/Inflammation
	CU-CPT17e 是多Toll 样受体激动剂，可激活TLR3、TLR8和TLR9。
T15020	CU-CPT22	TLR	Immunology/Inflammation
	CU-CPT22 是 toll 样受体 1 和 2 蛋白复合物抑制剂，可阻断 Pam3CSK4诱导的 TLR1/2 激活，IC50值为 0.58 µM。它与 TLR1/2 结合的合成三酰脂蛋白竞争，Ki 值为 0.41 µM。
T38694	Sp-8-CPT-cAMPS
	Sp-8-CPT-cAMPS is a powerful and specific cAMP analog that activates cAMP-dependent protein kinase A (PKA I and PKA II) selectively and effectively. It exhibits a 153-fold preference for site A of RI over site A of RII, and a 59-fold preference for site B of RII over site B of RI.
T36678	Rp-8-CPT-cAMPS sodium
	Rp-8-CPT-cAMP is a structural combination of the lipophilic and non-hydrolyzable cAMP analogs, 8-CPT-cyclic AMP and Rp-cyclic AMPS .[1] It functions as a site-selective inhibitor of protein kinase A (PKA) type I and II, with preference towards site A of type I and site B of type II.2 By occupying cAMP binding sites at the regulatory subunit of PKA, Rp-8-CPT-cAMP prevents the kinase holoenzyme from dissociative activation.[2],[3]
T22014	8-CPT-2Me-cAMP, sodium salt
	8-CPT-2Me-cAMP sodium is a sodium salt compound that selectively activates exchange proteins activated by cAMP (Epac). These Epac proteins are cAMP-sensitive guanine nucleotide exchange factors (GEFs) responsible for activating small GTPases Rap1 and Rap2. 8-CPT-2Me-cAMP sodium specifically activates Epac1 with an EC50 value of 2.2 μM, while showing no activation of PKA with an EC50 value greater than 10 μM [1]. Additionally, 8-CPT-2Me-cAMP sodium stimulates the Epac-mediated release of calcium ...
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。
T73421	CPT-Se3	Topoisomerase	DNA Damage/DNA Repair
	CPT-Se3为含硒的喜树碱前体活性分子，其杀癌和抗肿瘤效力显著。它通过降低GSH/GSSG比率及总硫醇水平，增加Hep G2细胞中ROS含量，触发癌细胞凋亡。CPT-Se3对HeLa、Hep G2、A549及SMMC-7721细胞线具备显着细胞毒性，IC50值介于2.19-4.7 μM。
T73422	CPT-Se4	Topoisomerase	DNA Damage/DNA Repair
	CPT-Se4为含硒前体活性分子的喜树碱(CPT)衍生物，对癌细胞具有较高杀伤力和抑制肿瘤生长效果。在降低GSH/GSSG比率和总硫醇的同时，CPT-Se4能够增加Hep G2细胞中的ROS水平，触发癌细胞凋亡。此化合物对HeLa、Hep G2、A549和SMMC-7721细胞系显示出显著的细胞毒性，IC50值范围为2.54-6.4 μM。
T4535	Etomoxir sodium salt (R)-(+)-乙莫克舍钠盐,(R)-Etomoxir sodium salt,Na salt,Etomoxir	Apoptosis; Others	Apoptosis; Others
	Etomoxir sodium salt ((R)-Etomoxir sodium salt) 是一种肉碱棕榈酰转移酶 1a (CPT-1a) 抑制剂，可以阻断脂肪酸合成。Etomoxir sodium salt 具有抗肿瘤活性。
T78569	CPT2 Carnitine palmitoyltransferase 2	Apoptosis	Apoptosis
	CPT2 (Carnitine palmitoyltransferase 2) 是一种脂肪酸氧化过程中的酶，它在结直肠癌 (CRC) 预后评估中作为生物标志物。CPT2 通过过表达激活p-p53并增加p53蛋白水平，这有助于抑制肿瘤生长和促进细胞的凋亡。CPT2 缺乏是长链脂肪酸氧化障碍相关的常见遗传性疾病，并且CPT2 的表达降低与多种癌症的发展密切相关，因此，在癌症研究领域具有研究价值。
T8344	CPTH2	Apoptosis; Histone Acetyltransferase	Apoptosis; Chromatin/Epigenetic
	CPTH2 是一种组蛋白乙酰基转移酶抑制剂。它选择性地抑制Gcn5对组蛋白 H3 的乙酰化，通过抑制乙酰转移酶p300 (KAT3B)诱导凋亡并降低透明细胞肾癌细胞系的侵袭性。
T64643	Rh2(S-TCPTAD)4
	Rh2(S-TCPTAD)4 是一种有用的有机化合物，可用于生命科学领域的相关研究，其产品编号为 T64643。
T77873	NH2-bicyclo[1.1.1]pentane-7-MAD-MDCPT hydrochloride	Topoisomerase	DNA Damage/DNA Repair
	NH2-bicyclo[1.1.1]pentane-7-MAD-MDCPT（化合物I）盐酸盐是一种通过偶联抗体实现靶向细胞传递的拓扑异构酶I抑制剂，显示出优良的体内外ADC活性。
T22549	ACPT-I	Others	Others
	Agonist for group III mGlu receptors
T39941	MP-PEG4-Val-Lys-Gly-7-MAD-MDCPT MP-PEG4-Val-Lys-Gly-7-MAD-MDCPT
	MP-PEG4-Val-Lys-Gly-7-MAD-MDCPT is a Camptothecin-linker. MP-PEG4-Val-Lys-Gly-7-MAD-MDCPT is a drug-linker conjugate for antibody-drug conjugate (ADC).
T22550	ACPT-II	Others	Others
	metabotropic receptor antagonist
T22536	8-pCPT-2-O-Me-cAMP-AM	Others	Others
	Epac activator
T74750	NH2-bicyclo[1.1.1]pentane-7-MAD-MDCPT
	NH2-bicyclo[1.1.1]pentane-7-MAD-MDCPT(化合物I)作为一种拓扑异构酶I抑制剂，通过偶联抗体实现对细胞的靶向传递，展现出良好的体内外ADC活性。
T81752	MP-PEG8-Val-Lys-Gly-7-MAD-MDCPT
	MP-PEG8-Val-Lys-Gly-7-MAD-MDCPT为喜树碱-接头化合物，属于抗体偶联活性分子（drug-linker conjugate for ADC）部分。该化合物在癌症及自身免疫性疾病研究中显示出研究潜力。
T22693	CPTH2 (hydrochloride) (357649-93-5 free base) CPTH2 (hydrochloride)	Others	Others
	CPTH2 is an inhibitor of the HAT activity of Gcn5.
T72756	Gly-7-MAD-MDCPT
	Gly-7-MAD-MDCPT 是一种抗癌剂。Gly-7-MAD-MDCPT 是一种喜树碱 (Camptothecin) 化合物，对多种癌细胞有细胞毒性，IC50为 10-1000 nM。
T40879	7-MAD-MDCPT
	7-MAD-MDCPT, a Camptothecin analog, is a toxin payload in antibody drug conjugates (ADCs).
T74751	Br-Val-Ala-NH2-bicyclo[1.1.1]pentane-7-MAD-MDCPT
	Br-Val-Ala-NH2-bicyclo[1.1.1]pentane-7-MAD-MDCPT (Formula V)，作为抗体偶联药物(ADC)的药物连接体部分，该化合物通过linker与topoisomeraseI抑制剂相连。
T25409	FCPT
	FCPT is an ATP competitive kinesin-5 inhibitor.
T12408	Perhexiline maleate	Others; Mitochondrial Metabolism	Metabolism; Others
	Perhexiline maleate 是一种口服活性的 CPT1和 CPT2抑制剂，可降低脂肪酸的代谢。Perhexiline maleate 对大鼠心脏和肝脏CPT 1的IC50值分别为77 和 148 μM。
T4535L	Etomoxir (R)-(+)-Etomoxir	Antioxidant; CPT	Metabolism; oxidation-reduction
	Etomoxir 是肉碱棕榈酰转移酶 1a （CPT-1a）抑制剂，通过抑制 CPT-1a 来抑制脂肪酸氧化，且抑制人、大鼠和豚鼠中棕榈酸酯的氧化。Etomoxir 对腺嘌呤核苷酸转位酶有抑制作用，可通过破坏CoA稳态来抑制巨噬细胞极化。
T11978	McN3716 NSC359682,Methyl palmoxirate	Mitochondrial Metabolism; CPT	Metabolism
	McN3716 是一种肉碱棕榈酰转移酶 I (CPT-1) 抑制剂，可用于研究代谢疾病。
T9088	Topovale ARC111,ARC 111,ARC-111,Topoval	Topoisomerase	DNA Damage/DNA Repair
	Topovale (ARC111) 是一种有效的拓扑异构酶 I 抑制剂。Topovale 抑制缺氧介导的缺氧诱导因子 1alpha 的积累。 Topovale 对一组癌细胞表现出低 nM 细胞毒性。与 P388 细胞相比，在 CPT 抗性拓扑异构酶 I (TOP1) 缺陷的 P388/CPT45 细胞中，Topovale 细胞毒性和 Topovale 诱导的细胞凋亡减少了 > 100 倍。
T27831	Lifibrate
	Lifibrate is an inhibitor of cholinephosphotransferase (CPT), phosphatidyl-N,N-dimethylethanolamine N-methyltransferase (PDE-NMT), and phosphatidyl-N-methylethanolamine N-methyltransferase (PME-NMT).
T78069	RPR132595A hydrochloride NPC hydrochloride	Drug Metabolite	Metabolism
	RPR132595A (NPC) hydrochloride，CPT-11的活性代谢产物，由细胞色素P-450 3A4 (CYP3A4) 催化产生，经尿液排出体外。
T38474	CL2-MMT-SN38 CL2-MMT-SN38
	CL2-MMT-SN38 is a derivative of SN-38, which is a potent anticancer agent and the active metabolite of Irinotecan (CPT-11), a Topoisomerase I inhibitor.
T14454	Azido-PEG5-acid	Others	Others
	Azido-PEG5-acid is a non-cleavable 5 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs), such as the conjugate CPT-APO (CPT: Camptothecin.
T19553	RPR132595A NPC	Others	Others
	RPR132595A is an active CPT-11 metabolite, it is generated by cytochrome P-450 3A4 (CYP3A4).
T70380	ZBH-1205
	ZBH-1205 is a novel camptothecin derivative, revealing potent antitumor activities mainly through cell apoptosis pathway, being more effective than cpt-11 and sn38 at inhibiting topoismerase-1
T74494	Antitumor agent-63
	Antitumor agent-63（Compound 40），一种20 (S)-O-linked camptothecin (CPT) 糖复合物，作为抗肿瘤剂，对正常细胞展现出无毒性。该化合物表现出高稳定性和低topoisomeraseI (Topo I)直接抑制活性。
T68196	Aminocarnitine
	Aminocarnitine is an inhibitor of fatty acid oxidation that acts as a hypoglycemic and antiketogenic compound. It alters lipidic metabolism by inhibiting carnitine acetyltransferase (CAT) and carnitine palmitoyltransferase (CPT).
T73829	Malonyl CoA
	Malonyl CoA是脂肪酸生物合成的重要底物，同时也担任脂肪酸氧化过程中的抑制剂角色。此外，Malonyl CoA亦作为线粒体肉碱棕榈酰转移酶1（CPT1）的可逆性抑制剂。
T78711	A011	ATM/ATR	DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling
	A011，作为一种选择性的ataxia-telangiectasia mutated (ATM)抑制剂，其IC50为1.0 nM，能够在与CPT-11联合应用时，诱导Apoptosis及G2/M期细胞周期阻滞，显示出显著的抗肿瘤活性。
T77816	Deruxtecan analog 2
	Deruxtecananalog 2（示例9 P3）是一种含活性分子-linker的Deruxtecan类似物，由Camptothecin（一种对多种癌症如结直肠癌、乳腺癌、肺癌和卵巢癌具有抗肿瘤活性的Topo I抑制剂）和linker组成，主要用于开发针对EGFR2的抗体药物偶联物（ADC）活性分子。

化合物

Cat.No: T7317

Target: TLR

8-Cyclopentyl-1,3-dimethylxanthine

Cat.No: T27076

Synonym: CPT,A1受体拮抗剂,CPT

Target: Adenosine Receptor

Cat.No: T22698

Synonym: CU CPT 4a

Target: TLR

Cat.No: T7347

Synonym: TLR8-specific antagonist

Target: TLR

Cat.No: T7302

Synonym: CU-CPT-9b,TLR8-specific antagonist 1

Target: TLR

Cat.No: T24610

Synonym: Prothecan,PEG-camptothecin,PEG-beta-CPT

Target: Topoisomerase

Cat.No: T41018

Rp-8-CPT-cAMPS

Cat.No: T38696

Cat.No: T10899

Target: TLR

Cat.No: T15020

Target: TLR

Sp-8-CPT-cAMPS

Cat.No: T38694

Rp-8-CPT-cAMPS sodium

Cat.No: T36678

8-CPT-2Me-cAMP, sodium salt

Cat.No: T22014

8-CPT-Cyclic AMP (sodium salt)

Cat.No: T21705

Cat.No: T73421

Target: Topoisomerase

Cat.No: T73422

Target: Topoisomerase

Etomoxir sodium salt

Cat.No: T4535

Synonym: (R)-(+)-乙莫克舍钠盐,(R)-Etomoxir sodium salt,Na salt,Etomoxir

Target: Apoptosis, Others

Cat.No: T78569

Synonym: Carnitine palmitoyltransferase 2

Target: Apoptosis

Cat.No: T8344

Target: Apoptosis, Histone Acetyltransferase

Cat.No: T64643

NH2-bicyclo[1.1.1]pentane-7-MAD-MDCPT hydrochloride

Cat.No: T77873

Target: Topoisomerase

Cat.No: T22549

Target: Others

MP-PEG4-Val-Lys-Gly-7-MAD-MDCPT

Cat.No: T39941

Synonym: MP-PEG4-Val-Lys-Gly-7-MAD-MDCPT

Cat.No: T22550

Target: Others

8-pCPT-2-O-Me-cAMP-AM

Cat.No: T22536

Target: Others

NH2-bicyclo[1.1.1]pentane-7-MAD-MDCPT

Cat.No: T74750

MP-PEG8-Val-Lys-Gly-7-MAD-MDCPT

Cat.No: T81752

CPTH2 (hydrochloride) (357649-93-5 free base)

Cat.No: T22693

Synonym: CPTH2 (hydrochloride)

Target: Others

Gly-7-MAD-MDCPT

Cat.No: T72756

Cat.No: T40879

Br-Val-Ala-NH2-bicyclo[1.1.1]pentane-7-MAD-MDCPT

Cat.No: T74751

Cat.No: T25409

Perhexiline maleate

Cat.No: T12408

Target: Others, Mitochondrial Metabolism

Cat.No: T4535L

Synonym: (R)-(+)-Etomoxir

Target: Antioxidant, CPT

Cat.No: T11978

Synonym: NSC359682,Methyl palmoxirate

Target: Mitochondrial Metabolism, CPT

Cat.No: T9088

Synonym: ARC111,ARC 111,ARC-111,Topoval

Target: Topoisomerase

Cat.No: T27831

RPR132595A hydrochloride

Cat.No: T78069

Synonym: NPC hydrochloride

Target: Drug Metabolite

Cat.No: T38474

Synonym: CL2-MMT-SN38

Azido-PEG5-acid

Cat.No: T14454

Target: Others

Cat.No: T19553

Synonym: NPC

Target: Others

Cat.No: T70380

Antitumor agent-63

Cat.No: T74494

Cat.No: T68196

Cat.No: T73829

Cat.No: T78711

Target: ATM/ATR

Deruxtecan analog 2

Cat.No: T77816

Cat. No.	Product Name	Target	Signaling Pathways
T3S1957	9-amino-CPT 9-氨基喜树碱,Aminocamptothecin,9-amino-2(S)-camptothecin,9-Aminocamptothecin	Topoisomerase	DNA Damage/DNA Repair
	9-amino-CPT (Aminocamptothecin) 是一种拓扑异构酶I 的抑制剂，具有抗肿瘤活性。
T6228	Irinotecan CPT-11,Topotecin,伊立替康,(+)-Irinotecan	Topoisomerase; Autophagy	Autophagy; DNA Damage/DNA Repair
	Irinotecan (CPT-11) 是喜树碱的衍生物，是一种 DNA 拓扑异构酶 I (Topo I) 的抑制剂。Irinotecan 通过与 Topo I 复合物结合来阻止 DNA 链的重新连接，并导致双链 DNA 断裂和细胞死亡，具有抗肿瘤活性。
T1123	Camptothecin NSC-100880,Campathecin,喜树碱,(S)-(+)-Camptothecin,CPT	Apoptosis; Influenza Virus; Topoisomerase; Antibiotic; Antifungal	Apoptosis; DNA Damage/DNA Repair; Microbiology/Virology
	Camptothecin (CPT) 属于生物碱类天然产物，是一种 DNA 拓扑异构酶 I (Topo I) 的抑制剂 (IC50=679 nM)，具有特异性。Camptothecin 具有抗肿瘤活性，可以诱导细胞凋亡。
T0486L	Irinotecan Hydrochloride 盐酸伊立替康,伊立替康盐酸盐,Camptothecin 11 hydrochloride,CPT-11 hydrochloride	Topoisomerase; Autophagy	Autophagy; DNA Damage/DNA Repair
	Irinotecan Hydrochloride (CPT-11 hydrochloride) 是喜树碱半合成衍生物的盐酸盐，是一种拓扑异构酶 I 抑制剂，可研究结肠癌和直肠癌。
T0486	Irinotecan hydrochloride trihydrate Irinotecan HCl Trihydrate,CPT-11 HCl Trihydrate,盐酸伊立替康三水合物	Topoisomerase; Autophagy	Autophagy; DNA Damage/DNA Repair
	Irinotecan hydrochloride trihydrate (CPT-11 HCl Trihydrate) 通过抑制拓扑异构酶 1 来防止 DNA 展开，可研究结肠癌和直肠癌。
T4S1951	10-Methoxycamptothecin	Others	Others
	10-Methoxycamptothecin 是分离自喜树的喜树碱衍生物，具有高抗癌特性。通过对 2774 细胞系的抗肿瘤活性测定，发现它比 10-羟基喜树碱的细胞毒性更高。
T3S1955	7-Ethylcamptothecin	Others	Others
	7-Ethylcamptothecin 是一种喜树碱类似物。其中喜树碱是一种细胞毒性生物碱，从喜树中分离出得到，对 L1210 白血病和 Walker 256 癌肉瘤模型具有很强的抗肿瘤活性。
TN2460	12-Ethyl-9-hydroxycamptothecin 7-乙基-10-羟基喜树碱,7-Ethyl-10-Hydroxy-Camptothecin	Others	Others
	12-Ethyl-9-hydroxycamptothecin 是一种 Camptothecin 的衍生物。其中Camptothecin (CPT) 是一种生物碱，也是 DNA 拓扑异构酶I 抑制剂(IC50:679 nM)。

天然产物

Cat.No: T3S1957

Synonym: 9-氨基喜树碱,Aminocamptothecin,9-amino-2(S)-camptothecin,9-Aminocamptothecin

Target: Topoisomerase

Cat.No: T6228

Synonym: CPT-11,Topotecin,伊立替康,(+)-Irinotecan

Target: Topoisomerase, Autophagy

Cat.No: T1123

Synonym: NSC-100880,Campathecin,喜树碱,(S)-(+)-Camptothecin,CPT

Target: Apoptosis, Influenza Virus, Topoisomerase, Antibiotic, Antifungal

Irinotecan Hydrochloride

Cat.No: T0486L

Synonym: 盐酸伊立替康,伊立替康盐酸盐,Camptothecin 11 hydrochloride,CPT-11 hydrochloride

Target: Topoisomerase, Autophagy

Irinotecan hydrochloride trihydrate

Cat.No: T0486

Synonym: Irinotecan HCl Trihydrate,CPT-11 HCl Trihydrate,盐酸伊立替康三水合物

Target: Topoisomerase, Autophagy

10-Methoxycamptothecin

Cat.No: T4S1951

Target: Others

7-Ethylcamptothecin

Cat.No: T3S1955

Target: Others

12-Ethyl-9-hydroxycamptothecin

Cat.No: TN2460

Synonym: 7-乙基-10-羟基喜树碱,7-Ethyl-10-Hydroxy-Camptothecin

Target: Others

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