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25

抑制剂 & 化合物

4

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T8182L	Guan-fu base A hydrochloride(1394-48-5 free base)	P450	Metabolism
	Guan-fu base A hydrochloride(1394-48-5 free base) 是一种从乌头中分离得到的抗心律失常生物碱。它是一种 CYP2D6 人类、猴子和狗同工型的抑制剂。
T7614	Eniluracil GW776C85,5-Ethynyluracil	Others	Others
	Eniluracil (GW776C85) 是不可逆的二氢嘧啶脱氢酶(DPD)抑制剂，是一种尿嘧啶类似物，能够使 5-FU 的口服生物利用度提高到 100%，促进均匀吸收和可预测的毒性。
T0984	5-Fluorouracil 5-FU,Fluorouracil,5-氟脲嘧啶,NSC 19893,5-Fluoracil,氟尿嘧啶	Apoptosis; Nucleoside Antimetabolite/Analog; HIV Protease; DNA/RNA Synthesis; Endogenous Metabolite	Apoptosis; Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Metabolism; Microbiology/Virology; Proteases/Proteasome
	5-Fluorouracil (5-FU) 是一种尿嘧啶类似物，一种 DNA 合成抑制剂。5-Fluorouracil 具有抗肿瘤活性，通过抑制胸苷酸合成酶影响嘧啶的合成。5-Fluorouracil 可以引起细胞凋亡和自噬。
T33762	Fosifloxuridine nafalbenamide NUC-3373,NUC3373,NUC 3373	DNA/RNA Synthesis	Cell Cycle/Checkpoint; DNA Damage/DNA Repair
	Fosifloxuridine nafalbenamide (NUC 3373) 是一种胸腺嘧啶合酶抑制剂，属于嘧啶核苷酸类似物，具有抗癌活性。它能诱发宿主免疫反应，有潜力增强免疫治疗。
T10013	1-Acetyl-3-o-toluyl-5-fluorouracil A-OT-Fu	Others	Others
	1-Acetyl-3-o-toluyl-5-fluorouracil is a potent antineoplastic agent.
TNU1475	5’-O-DMTr-2’-FU-methyl phosphonamidite
	5’-O-DMTr-2’-FU-methyl phosphonamidite 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 TNU1475。
T4374	Edoxudine 依度尿苷,Aedurid,EUDR,Epoxudine,乙去氧尿啶	Antiviral; Antibacterial	Immunology/Inflammation; Microbiology/Virology
	Edoxudine (Epoxudine) 是胸苷的类似物，是一种抗病毒药物，对单纯疱疹病毒有效。
T1600	Doxifluridine Ro 21-9738,AMC 0101,5'-DFUR,5-Fluoro-5'-deoxyuridine,去氧氟尿苷	Nucleoside Antimetabolite/Analog; DNA/RNA Synthesis	Cell Cycle/Checkpoint; DNA Damage/DNA Repair
	Doxifluridine (AMC 0101) 是一种胸苷磷酸化酶活化剂，对 PC9-DPE2细胞的 IC50为0.62 μM。它是具有抗肿瘤活性的抗肿瘤剂 5-fluorouracil (5-FU) 的氟嘧啶衍生物和口服前药。
T1408	Capecitabine Xeloda,卡培他滨,Capecitibine,Capiibine,RO 09-1978	Apoptosis; Nucleoside Antimetabolite/Analog; DNA/RNA Synthesis	Apoptosis; Cell Cycle/Checkpoint; DNA Damage/DNA Repair
	Capecitabine (Capecitibine) 是一种可口服的前药，可由胸苷磷酸化酶催化转变为其活性代谢物 Fluorouracil。
T21327	Uridine triacetate RG 2133 triacetate,PN-401,Tri-O-acetyluridine,PN401,RG 2133,RG-2133,PN 401,RG2133,RG2133 triacetate	Others	Others
	Uridine triacetate (RG 2133 triacetate) 是一种具有口服活性的 Uridine 前药。Uridine triacetate 能在肠道内迅速被吸收，在循环中迅速脱乙酰，生成游离尿苷。Uridine triacetate 可用于研究 5-氟尿嘧啶 (5-FU) 和卡培他滨的毒性，或早发性心脏或中枢神经系统 (CNS) 毒性。
T5987	Potassium oxonate Oxonic Acid (potassium salt),氧嗪酸钾,Potassium otastat,Potassium azaorotate	Others	Others
	Potassium oxonate (Potassium azaorotate) 是用作尿酸酶抑制剂，都5-FU 磷酸化为5-fluorouridine-5'-monophosphate 具有抑制作用。
T72991	Bis-Pro-5FU
	Bis-Pro-5FU 是一种 5-FU 前体，可增强5-氟尿嘧啶 (5-FU) 的口服生物利用度并提高其疗效。5-FU 是一种抗肿瘤抗代谢物，广泛用于结直肠癌和胰腺癌的研究。
T36870	5,6-dihydro-5-Fluorouracil 5-fluorodihydrouracil,5-Fluoro-dihydro-pyrimidine-2,4-dione	Others	Others
	5,6-dihydro-5-Fluorouracil (5-FUH2)是 5-FU 的无活性代谢产物，可用于用于研究机体代谢。
T33686	Nitrocaphane AT 1258,AT-1258,AT1258
	Nitrocaphane, in combination with 5-FU (fluorouracil), chemotherapy is considered as a protocol of choice in the treatment of malignant trophoblastic tumor.
T40932	Benzylacyclouridine 5-Benzylacyclouridine,BAU
	Benzylacyclouridine (BAU) is a powerful and selective inhibitor of uridine phosphorylase, the initial enzyme involved in uridine catabolism. Additionally, it can regulate the cytotoxic adverse effects of 5-fluorouracil (5-FU) and its derivatives.
T63868	α5β1 integrin agonist-1
	α5β1 integrin agonist-1 是一种 α5β1 integrin 激动剂，可选择性地将 5-FU 输送到肿瘤细胞中，诱导肿瘤细胞死亡。
TP2108	TAPI 2
	ADAM-17 (TACE) and MMP inhibitor (Ki = 120 nM at ADAM-17). Sensitizes cancer stem cells to the lethal effects of 5-FU in vitro. Blocks shedding of TNF-α from cell membranes.
T30095	APG-1387 SM 1387,SM-1387,SM1387,APG 1387l
	APG-1387 (SM-1387) is an IAP inhibitor that promotes the rapid degradation of cIAP1/2 and XIAP and exerts an anti-tumor effect on nasopharyngeal carcinoma stem cells. Studies have shown that APG-1387 combined with NPC's CDDP and 5-FU enhance chemoresensit
T39792	AMPC
	AMPC, a powerful and efficient inhibitor of TFF3, demonstrates inhibitory effects on cell proliferation, survival, oncogenicity, and CSC-like behavior in TFF3-positive CMS4 CRC cells. It acts as a promising standalone anti-cancer agent and also enhances the effects of 5-FU when used in combination, making it a valuable tool for cancer research.
T73558	W1131
	W1131 是一种有效的STAT3抑制剂，可引发铁死亡。W1131 在胃癌皮下异种移植模型、类器官模型和 PDX 模型中抑制癌症进展。W1131 有效减轻癌细胞对 5-FU 化学耐药性。W1131 调节细胞周期、DNA 损伤反应和氧化磷酸化，包括IL6-JAK-STAT3通路和铁死亡 (ferroptosis) 通路。
T63074	Ivaltinostat formic
	Ivaltinostat (CG-200745) formic 是一种口服具有活力的泛 HDAC 抑制剂，具有异羟肟酸部分，能够在催化袋底部结合锌。Ivaltinostat formic 对组蛋白 H3 和微管蛋白的脱乙酰作用具有抑制效果。Ivaltinostat formic 能够促使 p53 的积累，诱导 p53 依赖性反式激活，并提高 MDM2 和 p21 (Waf1/Cip1) 蛋白的表达。Ivaltinostat formic 增加 Gemcitabine 耐药细胞对 Gemcitabine 和 5-Fluorouracil (5-FU) 的敏感性。Ivaltinostat formic 诱导凋亡，并具有抗肿瘤效果。
T80847	W1131 TFA	STAT	JAK/STAT signaling; Stem Cells
	W1131 TFA 是一种抑制STAT3并诱导铁死亡(ferroptosis)的有效化合物。在胃癌的皮下异种移植模型、类器官模型以及PDX模型中，它都能显著阻止疾病的发展。此外，W1131能有效缓解癌细胞对5-FU的化学耐药性。该化合物还通过调节IL6-JAK-STAT3和铁死亡(ferroptosis)通路来影响细胞周期、DNA损伤响应和氧化磷酸化过程。
T71549	RKS-262
	RKS262 is a specific cyclin/CDK inhibitor. RKS262 was identified by structural optimization of Nifurtimox which is currently undergoing phase II clinical trials to treat high-risk neuroblastoma. In a NCI(60) cell-line assay RKS262 exhibited significant cytotoxicity in ovarian cancer cells and a variety of other cell lines exceeding effects of commercial drugs such as cisplatin, 5-FU, cyclophosphamide or sapacitabine. Various leukemia cell-lines were most sensitive (GI(50): ~ 10 nM) while several...
T36679	Rp-cAMPS sodium salt
	Rp-cAMPS sodium salt, a cAMP analog, is a potent, competitive cAMP-induced activation of cAMP-dependent PKA I and II (Kis of 12.5 μM and 4.5 μM, respectively) antagonist. Rp-cAMPS sodium salt is resistant to hydrolysis by phosphodiesterases[1][2][3][4][5][6]. A membrane-permeable competitive cAMP antagonist (Rp-cAMPS) that blocks PKA activation by binding to the regulatory subunits without dissociating the kinase holoenzyme also inhibits synaptic plasticity but has no effect on normal synaptic t...
T35432	α-Conotoxin ImI (trifluoroacetate salt)
	α-Conotoxin ImI is a conotoxin that has been found inC. imperialisand has receptor antagonist and anticancer activities.1It is a peptide antagonist of homomeric α7 nicotinic acetylcholine receptors (nAChRs; IC50= 220 nM). α-Conotoxin ImI is selective for α7 nAChRs over α2β2, α3β2, α4β2, α2β4, α3β4, α4β4, and α1β1γδ subunit-containing nAChRs at 5 μM but does inhibit homomeric α9 nAChRs (IC50= 1,800 nM). Administration of paclitaxel in micelles containing α-conotoxin ImI decreases tumor growth in ...

化合物

Guan-fu base A hydrochloride(1394-48-5 free base)

Cat.No: T8182L

Target: P450

Cat.No: T7614

Synonym: GW776C85,5-Ethynyluracil

Target: Others

Cat.No: T0984

Synonym: 5-FU,Fluorouracil,5-氟脲嘧啶,NSC 19893,5-Fluoracil,氟尿嘧啶

Target: Apoptosis, Nucleoside Antimetabolite/Analog, HIV Protease, DNA/RNA Synthesis, Endogenous Metabolite

Fosifloxuridine nafalbenamide

Cat.No: T33762

Synonym: NUC-3373,NUC3373,NUC 3373

Target: DNA/RNA Synthesis

1-Acetyl-3-o-toluyl-5-fluorouracil

Cat.No: T10013

Synonym: A-OT-Fu

Target: Others

5’-O-DMTr-2’-FU-methyl phosphonamidite

Cat.No: TNU1475

Cat.No: T4374

Synonym: 依度尿苷,Aedurid,EUDR,Epoxudine,乙去氧尿啶

Target: Antiviral, Antibacterial

Cat.No: T1600

Synonym: Ro 21-9738,AMC 0101,5'-DFUR,5-Fluoro-5'-deoxyuridine,去氧氟尿苷

Target: Nucleoside Antimetabolite/Analog, DNA/RNA Synthesis

Cat.No: T1408

Synonym: Xeloda,卡培他滨,Capecitibine,Capiibine,RO 09-1978

Target: Apoptosis, Nucleoside Antimetabolite/Analog, DNA/RNA Synthesis

Uridine triacetate

Cat.No: T21327

Synonym: RG 2133 triacetate,PN-401,Tri-O-acetyluridine,PN401,RG 2133,RG-2133,PN 401,RG2133,RG2133 triacetate

Target: Others

Potassium oxonate

Cat.No: T5987

Synonym: Oxonic Acid (potassium salt),氧嗪酸钾,Potassium otastat,Potassium azaorotate

Target: Others

Cat.No: T72991

5,6-dihydro-5-Fluorouracil

Cat.No: T36870

Synonym: 5-fluorodihydrouracil,5-Fluoro-dihydro-pyrimidine-2,4-dione

Target: Others

Cat.No: T33686

Synonym: AT 1258,AT-1258,AT1258

Benzylacyclouridine

Cat.No: T40932

Synonym: 5-Benzylacyclouridine,BAU

α5β1 integrin agonist-1

Cat.No: T63868

Cat.No: TP2108

Cat.No: T30095

Synonym: SM 1387,SM-1387,SM1387,APG 1387l

Cat.No: T39792

Cat.No: T73558

Ivaltinostat formic

Cat.No: T63074

Cat.No: T80847

Target: STAT

Cat.No: T71549

Rp-cAMPS sodium salt

Cat.No: T36679

α-Conotoxin ImI (trifluoroacetate salt)

Cat.No: T35432

Cat. No.	Product Name	Target	Signaling Pathways
T2911	Stevioside 甜菊苷,蛇菊苷	TLR	Immunology/Inflammation
	Stevioside 是一种天然甜味剂，从甜叶菊叶中提取的获得，具有抗癌作用。
T4720	6-Hydroxypyridin-2(1H)-one hydrochloride 2,6-二羟基吡啶盐酸盐,2,6-Dihydroxypyridine hydrochloride	Others; Endogenous Metabolite	Metabolism; Others
	6-Hydroxypyridin-2(1H)-one hydrochloride (2,6-Dihydroxypyridine hydrochloride) 是内源性代谢产物的一种。
T4S1551	Cinnamaldehyde Cinnamic Aldehyde,肉桂醛	HIF	Angiogenesis; Chromatin/Epigenetic
	Cinnamaldehyde (Cinnamic Aldehyde) 具有解热作用。它是镇静剂。它抑制MDA-MB-435S 细胞的侵袭能力与下调miR-27a 的表达有关。它诱导活性氧的产生，发挥血管扩张和抗癌作用。它似乎是一种有希望的候选药物，可作为与 5-氟尿嘧啶 (5-FU) 和奥沙利铂 (OXA) 这两种用于 CRC 治疗的化疗药物联合治疗的辅助剂。其作用的可能机制可能涉及药物代谢基因的调节。它在抑制黑色素瘤的发生和发展方面具有一定的作用，其作用机制可能表现为抑制VEGF 和HIF-α的表达，从而使血管模拟和黑色素瘤细胞新生血管的形成，促进肿瘤的生长。
TN3152	6-Acetonyldihydrochelerythrine	ERK; BCL; Akt; HIV Protease; PPAR; p53	Apoptosis; Cytoskeletal Signaling; DNA Damage/DNA Repair; MAPK; Metabolism; Microbiology/Virology; PI3K/Akt/mTOR signaling; Proteases/Proteasome
	6-Acetonyldihydrochelerythrine exhibits significant antioxidant activities, it exhibits significant anti-HIV activity in H9 lymphocytes with EC50 and TI (Therapeutic Index) values of 1.77 microg/mL and 14.6, respectively. 6-Acetonyldihydrochelerythrine is

天然产物

Cat.No: T2911

Synonym: 甜菊苷,蛇菊苷

Target: TLR

6-Hydroxypyridin-2(1H)-one hydrochloride

Cat.No: T4720

Synonym: 2,6-二羟基吡啶盐酸盐,2,6-Dihydroxypyridine hydrochloride

Target: Others, Endogenous Metabolite

Cat.No: T4S1551

Synonym: Cinnamic Aldehyde,肉桂醛

Target: HIF

6-Acetonyldihydrochelerythrine

Cat.No: TN3152

Target: ERK, BCL, Akt, HIV Protease, PPAR, p53

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