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35

抑制剂 & 化合物

7

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T8796	CAN508	CDK	Cell Cycle/Checkpoint
	CAN508 是一种有效的 ATP 竞争性 CDK9/cyclin T1 抑制剂，IC50 为 0.35 μM。它还是 Cdk2-cyclin E 对 ATP 的竞争性抑制剂，Ki 和 IC50 值分别为 13.3 和 20 µM。它对 CDK9/cyclin T 的选择性是其他 CDK/cyclin 复合物的 38 倍，有抗肿瘤活性。
T15771	Lobaplatin D-19466,络铂	DNA Alkylation	DNA Damage/DNA Repair
	Lobaplatin (D-19466) 是一种铂 (II) 复合物的非对映混合物，是一种有前途的抗肿瘤化疗药物，在多种肿瘤类型的患者中具有活性。
T2455	PFK-015 PFK15,PFK 015	Glucokinase; Autophagy	Autophagy; Metabolism
	PFK-015 (PFK15) 是一种有效的 PFKFB3 抑制剂，对重组PFKFB3的IC50为110 nM。它能抑制 Y 细胞中的 PFKFB3 活性，IC50为20 nM。
T7322	Theliatinib 席栗替尼,西利替尼	EGFR	Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors
	Theliatinib 是一种ATP 竞争性、口服活性和高度选择性的EGFR 抑制剂，Ki 为 0.05 nM，IC50为 3 nM。它具有抗肿瘤活性，对EGFR T790M/L858R 突变体的IC50值为 22 nM。它对EGFR 的选择性是其他激酶的 50 倍以上。
T0992	Carbenoxolone disodium Biogastrone,Duogastrone,甘珀酸钠,Bioral	Gap Junction Protein	Cytoskeletal Signaling
	Carbenoxolone disodium (Duogastrone) 是甘草酸的活性代谢物和人11β-HSD 和细菌3α, 20β-HSD 的抑制剂。它是一种缝隙连接的解耦剂，可抑制牛痘病毒生长，用于消化性、食道和口腔溃疡和炎症的相关研究。
T0866	Propafenone Rythmol,普罗帕酮,Propafenonum	Potassium Channel; MRP; Sodium Channel	Immunology/Inflammation; Membrane transporter/Ion channel
	Propafenone (Propafenonum) 是钠通道阻滞剂，它对 β 受体具有高亲和力 (IC50=32 nM)。它能够阻断瞬时外向钾电流 (Ito) (IC50: 4.9 nM) 和持续延迟整流器K+电流 (Isus) (IC50: 8.6 nM) ，具有抗心律失常的作用。它能够诱导线粒体功能障碍及诱导细胞凋亡，从而抑制食管癌增殖。
T11918	Lysipressin Lysine vasopressin,[Lys8]-Vasopressin,赖氨加压素	Others	Others
	Lysipressin ([Lys8]-Vasopressin) 是一种抗利尿激素，从猪身上发现，能够诱发兔膀胱平滑肌的收缩，激活腺苷酸环化酶。
T8341	QX 314 QX-314	Others	Others
	QX 314 (Lidocaine N-ethyl bromide) 是一种非膜渗透性阻滞剂，可抑制酸诱导的食管伤害性 C 纤维神经元活化。
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。
T39640	JAB-3068 SHP2-IN-6	Phosphatase	Metabolism
	JAB-3068 (SHP2-IN-6) 是一种高效的 SHP2 抑制剂，具有抗癌抗肿瘤活性，可用于研究乳腺癌肺癌和食道癌。
T38387	Compound C108	GTPase	GPCR/G Protein
	Compound C108 是 GTPase 激活蛋白 SH3 结构域结合蛋白 2 (G3BP2) 的抑制剂。 Compound C108可用于乳腺肿瘤和食管鳞状细胞癌的研究。
T76717	Serplulimab HLX 10	COX	Immunology/Inflammation; Neuroscience
	Serplulimab (HLX 10) 是人源化 PD-1 单克隆抗抗体。Serplulimab 具有抗肿瘤活性，可用于小细胞肺癌和食管鳞状细胞癌。
T35394	Sintilimab (anti-PD-1) IBI308,Sintilimab (anti-PD-1)	PD-1/PD-L1	Apoptosis; Cell Cycle/Checkpoint; Immunology/Inflammation
	Sintilimab (IBI308) 是一种人源化的 IgG4 单克隆抗体，具有显著的抗肿瘤活性，通过与 PD-1 结合从而阻断 PD-1 与其配体 (PD-L1 和 PL-L2) 的相互作用，进而恢复内源性抗肿瘤 T 细胞反应。Sintilimab 联合其他化合物来治疗经典霍奇金淋巴瘤、非小细胞肺癌和食管癌。
T0044	Oxethazaine 奥昔卡因,Oxetacaine	HBV; Sodium Channel	Membrane transporter/Ion channel; Microbiology/Virology
	Oxethazaine (Oxetacaine) 是一种具有耐酸性和口服活性试剂，是芬特明的酸性前体，有潜力缓解消化性溃疡疾病或食管炎引起的疼痛。
T1291	Cisapride 西沙必利,西沙比利,Prepulsid,R 51619,Pridesia,Kaudalit,(±)-Cisaprid,Kinestase	Potassium Channel; 5-HT Receptor; HER	Angiogenesis; GPCR/G Protein; JAK/STAT signaling; Membrane transporter/Ion channel; Neuroscience; Tyrosine Kinase/Adaptors
	Cisapride (R 51619) 是一种5-HT4受体激动剂，还是 hERG 抑制剂。它可作用于肠道中的血清素受体，促进肠道蠕动，增加胃排空并减少食管反流。
T61699	Osunprotafib AC 484,Osunprotafib,AC484,ABBV-CLS-484	Phosphatase	Metabolism
	ABBV-CLS-484 (Osunprotafib) 是一种具有亚纳摩尔活性的有效的PTPN2抑制剂，具有抗肿瘤活性，可增强T细胞抗肿瘤免疫力。ABBV-CLS-484可用于治疗肿瘤、食管癌和消化系统疾病。
T6136	Canertinib PD-183805,CI-1033,卡纽替尼	EGFR	Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors
	Canertinib (CI-1033) 是有效地，不可逆的EGFR 抑制剂；抑制细胞EGFR 和ErbB2自身磷酸化的IC50值分别为7.4和9 nM。
T9636	Dalpiciclib SHR-6390	CDK	Cell Cycle/Checkpoint
	Dalpiciclib (SHR-6390) 是一种高选择性、口服生物利用度和相当效力的 CDK4 和 CKD6 抑制剂，IC50 分别为 12.4 nM 和 9.9 nM。它通过抑制磷酸化 Rb 蛋白和诱导 G1 细胞周期阻滞在食管鳞状细胞癌中发挥有效的抗肿瘤活性。
T71399	Plogosertib CYC140
	Plogosertib (CYC140) 是一种选择性的、有效的、具有口服活性的 ATP 竞争性的 PLK1抑制剂 (IC50: 3 nM)。Plogosertib 是一种有抗增殖活性的抗癌剂，可用于多种肿瘤的研究，包括食管癌、胃癌、白血病、非小细胞肺癌、卵巢癌和鳞状细胞癌。
T7057	Methylstat	Histone Demethylase; Others	Chromatin/Epigenetic; Others
	Methylstat 是一种含有 Jumonji C 结构域的组蛋白去甲基化酶 (JMJD) 抑制剂的甲酯前药，具有良好的细胞渗透性。在体外试验中，methylstat 的游离酸可抑制 JMJD2A、JMJD2C、JMJD2E、PHF8 和 JMJD3，IC50 值分别约为 4.3、3.4、5.9、10 和 43 µM。 Methylstat 抑制 JMJD2C 敏感的食管癌细胞系 KYSE150 的生长，GI50 为 5.1 µM，而 methylstat 的游离酸在高达 100 µM 时不抑制细胞生长。 Methylstat 以浓度依赖性方式在多个位点诱导组蛋白高甲基化（KYSE150 细胞中 H3K4me3 和 H3K9me3 的 EC50 = 10.3 和 8.6 µM，MCF-7 细胞中的 EC50 分别为 6.7 和 6.3 µM）。
T33471	Monoethanolamine Oleate FO-611,Ethamolin,brand name: Ethamolin,FO 611,FO611
	Monoethanolamine Oleate (Etamolin, FO-611) is a hardening agent used in the treatment of varicose and esophageal veins.
T1552L	Itopride free base HSR803,HSR-803,Itopride hydrochloride,HSR 803
	Itopride HCl is an AChE inhibitor and dopamine D2 receptor antagonist. It inhibits lower esophageal sphincter relaxation. It also used to treat functional dyspepsia and gastroesophageal reflux disease
T80599	Dectrekumab QAX576
	Dectrekumab (QAX576) 是针对IL-13的人源化单克隆抗体。它能显著降低嗜酸性粒细胞性食管炎 (EoE) 患者上皮内的嗜酸性粒细胞数量，并改善食管疾病相关的转录失调情况，适用于免疫炎症研究。
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.
T36709	N’-Nitrosonornicotine
	N’-Nitrosonornicotine is a tobacco-specific N-nitrosamine and carcinogen that has been found in unburned tobacco and cigarette smoke.1It induces the formation of DNA adducts in isolated rat nasal mucosa and esophagus. N’-Nitrosonornicotine induces tumor formation in rat esophagus and nasal cavity, mouse lung, forestomach, and trachea, and hamster trachea and forebrain. Urinary levels of N’-nitrosonornicotine are positively correlated with the risk of esophageal cancer in smokers.2 1.Hecht, S....
T35822	CAY10722
	CAY10722 is an inhibitor of sirtuin 3 (SIRT3), a class III HDAC (71% inhibition at 200 μM). SIRT3 is involved in modulating metabolic homeostasis as a NAD+-dependent protein deacetylase in the mitochondria. SIRT3 functions as either an oncogene or tumor suppressor, depending on cancer cell type. High SIRT3 expression in patient-derived esophageal cancer tissues is associated with shorter survival and, in mice, downregulation leads to a lower tumor load. In contrast, low SIRT3 expression in patie...
T74997	ERK-IN-6
	ERK-IN-6 (compound 6g) 是有效的食管鳞状细胞癌 (ESCC) 的抗增殖剂。ERK-IN-6 通过ERK 通路诱导细胞凋亡。ERK-IN-6 可用于食管鳞状细胞癌的研究。
T63199	Dalpiciclib hydrochloride
	Dalpiciclib (SHR-6390) hydrochloride 是高度选择性的、口服具有活力的CDK4/6抑制剂，他们的IC50值分别为 12.4 nM 和 9.9 nM，能够作用于乳腺癌和食道鳞状细胞癌，具有出抗肿瘤作用。
T40572	Lesogaberan napadisylate AZD-3355 napadisylate
	Lesogaberan (AZD-3355) napadisylate is a potent and selective agonist of GABA B receptors, with an EC 50 of 8.6 nM for human recombinant GABA B receptors. It demonstrates an affinity (Ki) of 5.1 nM for rat GABA B receptors and 1.4 μM for GABA A receptors, as determined by its displacement of [3H]GABA binding in brain membranes. Notably, Lesogaberan napadisylate exerts a peripheral mode of action, inhibiting transient lower esophageal sphincter relaxation.
T76997	Socazolimab
	Socazolimab (ZKAB001) 是一种针对PD-L1的单克隆抗体，在治疗复发或转移性宫颈癌方面展现了持久的安全性和有效性。此外，Socazolimab 也被认为在小细胞肺癌、食管鳞状细胞癌 (ESCC)、晚期尿路上皮癌及骨肉瘤治疗中具有潜在应用价值。
T72912	(R)-Afatinib (R)-BIBW 2992
	(R)-Afatinib ((R)-BIBW 2992) 是 Afatinib 异构体。Afatinib 是一种口服有效且不可逆的 ErbB 家族 (EGFR 和HER2) 双特异性抑制剂，对 EGFRwt, EGFRL858R, EGFRL858R/T790M 和 HER2 的 IC50值分别为 0.5 nM、0.4 nM、10 nM 和 14 nM。Afatinib 可用于食管鳞状细胞癌 (ESCC)、非小细胞肺癌 (NSCLC) 和胃癌的研究。
T35616	Migrastatin
	Migrastatin is a bacterial metabolite that has been found inStreptomyceswith antimuscarinic and anticancer activities.1,2It binds to M1-5muscarinic acetylcholine receptors (Kis = >200, 200, 31, 43, and >200 μM, respectively) and inhibits calcium mobilization induced by carbamoylcholine in SK-N-SH cells (IC50= 28 μM), as well as in primary rat bladder smooth muscle cells.1Migrastatin inhibits the migration of EC17 esophageal cancer cells in a wound healing assay (IC50= 10 μg/ml) and 4T1 mouse mam...
T36714	Sucrose octasulfate (potassium salt)
	Sucrose octasulfate (SOS), a component of the gastrointestinal protectant sucralfate, is an alkaline aluminum-sucrose complex that inhibits peptic hydrolysis and raises gastric pH, protecting esophageal epithelium against acid injury. It can bind to exosite II of thrombin (KD = ~1.4 μM) and inhibit its catalytic activity (IC50 = 4.5 μM) and, as such, has been used as a surrogate for heparin. Furthermore, SOS has been shown to inhibit tumor growth in mouse melanoma and lung carcinoma models by pr...
T72215	Lesogaberan hydrochloride AZD-3355 hydrochloride
	Lesogaberan (AZD-3355) hydrochloride 是一种有效的选择性 GABAB 受体激动剂，对人重组 GABAB 受体的 EC50为 8.6 nM。通过脑膜中 [3H]GABA 结合位移测量，Lesogaberan hydrochloride 对大鼠 GABAB 和 GABAA 受体的亲和力 (Kis)：分别为 5.1 nM 和 1.4 μM。Lesogaberan hydrochloride 通过外周作用模式抑制短暂的食管下括约肌松弛。
T64075	Afatinib oxalate
	Afatinib (BIBW 2992) oxalate 是一种不可逆的、口服具有活力的 ErbB 家族 (EGFR 和 HER2) 双特异性抑制剂，能够作用于 EGFRwt (IC50: 0.5 nM)、EGFRL858R (IC50: 0.4 nM)、EGFRL858R/T790M (IC50: 10 nM) 和 HER2 (IC50: 14 nM)。Afatinib oxalate 能够用于研究食管鳞状细胞癌 (ESCC)、非小细胞肺癌 (NSCLC) 和胃癌。

化合物

Cat.No: T8796

Target: CDK

Cat.No: T15771

Synonym: D-19466,络铂

Target: DNA Alkylation

Cat.No: T2455

Synonym: PFK15,PFK 015

Target: Glucokinase, Autophagy

Cat.No: T7322

Synonym: 席栗替尼,西利替尼

Target: EGFR

Carbenoxolone disodium

Cat.No: T0992

Synonym: Biogastrone,Duogastrone,甘珀酸钠,Bioral

Target: Gap Junction Protein

Cat.No: T0866

Synonym: Rythmol,普罗帕酮,Propafenonum

Target: Potassium Channel, MRP, Sodium Channel

Cat.No: T11918

Synonym: Lysine vasopressin,[Lys8]-Vasopressin,赖氨加压素

Target: Others

Cat.No: T8341

Synonym: QX-314

Target: Others

Cat.No: T24610

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

Target: Topoisomerase

Cat.No: T39640

Synonym: SHP2-IN-6

Target: Phosphatase

Cat.No: T38387

Target: GTPase

Cat.No: T76717

Synonym: HLX 10

Target: COX

Sintilimab (anti-PD-1)

Cat.No: T35394

Synonym: IBI308,Sintilimab (anti-PD-1)

Target: PD-1/PD-L1

Cat.No: T0044

Synonym: 奥昔卡因,Oxetacaine

Target: HBV, Sodium Channel

Cat.No: T1291

Synonym: 西沙必利,西沙比利,Prepulsid,R 51619,Pridesia,Kaudalit,(±)-Cisaprid,Kinestase

Target: Potassium Channel, 5-HT Receptor, HER

Cat.No: T61699

Synonym: AC 484,Osunprotafib,AC484,ABBV-CLS-484

Target: Phosphatase

Cat.No: T6136

Synonym: PD-183805,CI-1033,卡纽替尼

Target: EGFR

Cat.No: T9636

Synonym: SHR-6390

Target: CDK

Cat.No: T71399

Synonym: CYC140

Cat.No: T7057

Target: Histone Demethylase, Others

Monoethanolamine Oleate

Cat.No: T33471

Synonym: FO-611,Ethamolin,brand name: Ethamolin,FO 611,FO611

Itopride free base

Cat.No: T1552L

Synonym: HSR803,HSR-803,Itopride hydrochloride,HSR 803

Cat.No: T80599

Synonym: QAX576

Cat.No: T11691

Target: Others

N’-Nitrosonornicotine

Cat.No: T36709

Cat.No: T35822

Cat.No: T74997

Dalpiciclib hydrochloride

Cat.No: T63199

Lesogaberan napadisylate

Cat.No: T40572

Synonym: AZD-3355 napadisylate

Cat.No: T76997

Cat.No: T72912

Synonym: (R)-BIBW 2992

Cat.No: T35616

Sucrose octasulfate (potassium salt)

Cat.No: T36714

Lesogaberan hydrochloride

Cat.No: T72215

Synonym: AZD-3355 hydrochloride

Afatinib oxalate

Cat.No: T64075

Cat. No.	Product Name	Target	Signaling Pathways
T6S1844	Tenacissoside H Tenacissimoside C,通关藤苷H	Others	Others
	Tenacissoside H (Tenacissimoside C) 是一种分离自通关藤中的天然产物，具有抗肿瘤作用。
T4S1796	Heterophyllin B	PI3K	PI3K/Akt/mTOR signaling
	Heterophyllin B 是一种活性环肽，从 Pseudostellaria heterophylla 中分离得到，可用于研究食管癌。
TN1721	Gypenoside L	ERK; p38 MAPK; Calcium Channel; NF-κB; ROS	Immunology/Inflammation; MAPK; Membrane transporter/Ion channel; Metabolism; NF-κB
	Gypenoside L 是存在于绞股蓝中的一种皂苷，可增加 SA-β-半乳糖苷酶活性，促进衰老相关分泌细胞因子的产生。它还可以激活p38和ERK MAPK 通路和NF-κB 通路以诱导衰老，具有抗肿瘤和抗炎活性。
T2836	Isorhamnetin 3-methylquercetin,3'-Methylquercetin,Isorhamnetol,异鼠李素,3'-Methoxyquercetin	MEK; PI3K; Endogenous Metabolite	MAPK; Metabolism; PI3K/Akt/mTOR signaling
	Isorhamnetin (3-methylquercetin) 是从中草药沙棘中提取的一种类黄酮，可通过抑制MEK1和PI3K 来抑制皮肤癌。
T75569	Xerophilusin B
	Xerophilusin B 是一种从 Isodon xerophilus 中分离得到的抗癌剂，对食管鳞状细胞癌 (ESCC) 细胞系表现出抗增殖作用，可诱导 G2/M 细胞周期停滞，介导细胞凋亡 apoptosis。
TN4166	Griffipavixanthone	ERK; Raf; ROS; MEK; Caspase	Apoptosis; Immunology/Inflammation; MAPK; Proteases/Proteasome
	Griffipavixanthone inhibits the growth of human Non-small-cell lung cancer H520 cells in dose- and time-dependent manners, it induces cell apoptosis through mitochondrial apoptotic pathway accompanying with ROS production. It can inhibit tumor metastasis
T36448	(E)-Ajoene
	(E)-Ajoene is a disulfide that has been found inA. sativumand has diverse biological activities.1,2,3,4It is active against Gram-positive and Gram-negative bacteria (MICs = 10-250 and 150->500 μg/ml, respectively) and fungi (MICs = 15-50 μg/ml).1(E)-Ajoene inhibits proliferation of a variety of cancer cells, including MDA-MB-231 breast, HeLa cervical, and WHCO1 esophageal cancer cells (IC50s = 18.6, 61, and 39.2 μM, respectively).2It also inhibits human glutathione reductase andT. cruzitrypanoth...

天然产物

Tenacissoside H

Cat.No: T6S1844

Synonym: Tenacissimoside C,通关藤苷H

Target: Others

Heterophyllin B

Cat.No: T4S1796

Target: PI3K

Cat.No: TN1721

Target: ERK, p38 MAPK, Calcium Channel, NF-κB, ROS

Cat.No: T2836

Synonym: 3-methylquercetin,3'-Methylquercetin,Isorhamnetol,异鼠李素,3'-Methoxyquercetin

Target: MEK, PI3K, Endogenous Metabolite

Cat.No: T75569

Griffipavixanthone

Cat.No: TN4166

Target: ERK, Raf, ROS, MEK, Caspase

Cat.No: T36448

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