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14

抑制剂 & 化合物

4

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T22223	3PO	Glucokinase; Autophagy	Autophagy; Metabolism
	3PO 是一种 PFKFB3 的小分子抑制剂，IC50值为22.9 μM。它抑制几种人类恶性造血和腺癌细胞系的增殖，IC50在1.4到24 μM 之间。它抑制葡萄糖摄取，并降低 Fru-2,6-BP、乳酸、ATP、NAD+ 和 NADH 的细胞内浓度。
T8979	AEM1	Nrf2	Immunology/Inflammation
	AEM1 是 Nrf2抑制剂，能够降低 A549 细胞中 Nrf2 依赖基因的表达，并在体外和体内抑制 A549 细胞的生长。
T38679	DODAP
	DODAP, an ionizable cationic lipid, serves as a vital component in liposome formation. Its applications encompass the capability to encapsulate siRNA, immunostimulatory chemotherapeutic agents for in vitro and in vivo delivery, among others.
T69005	CEP-6800
	CEP-6800 is a potent PARP inhibitor with potential anticancer activity. CEP-6800 could be used as a chemopotentiating agent with a variety of clinically effective chemotherapeutic agents.
T68781	3Ac-SL0101
	3Ac-SL0101 is a potent RSK-specific inhibitor. It facilitates the development of RSK inhibitors as anti-cancer chemotherapeutic agents.
T69993	BIM-46068
	BIM-46068 is a potent and specific inhibitor of human farnesyltransferase. In regard to a panel of cell lines, using the Compare analysis to determine the Pearson coefficient correlation, the anti-proliferative spectrum of BIM-46068 has been shown to be distinct from the profile of typical chemotherapeutic agents.
T77855	Mal-PEG8-Val-Ala-PAB-Exatecan
	Mal-PEG8-Val-Ala-PAB-Exatecan（化合物9b）是一种用于连接抗体与Nectin-4多肽结合的化疗活性分子的ADC linker，适用于癌症研究。
T69162	Ki23057
	Ki23057 is a a FGFR2 inhibitor, which enhances the chemosensitivity of drug-resistant gastric cancer cell lines when used in combination with chemotherapeutic drugs. Ki23057 might be therapeutically promising for treating drug-resistant gastric cancer cells, especially when used in combination with SN38, PTX, or VP16. The apoptosis process might be the main mechanism underlying the synergistic effect of these combinations. The ERCC1 and p53 genes may play an integral role in the synergism betwee...
T61485	S07-2010
	S07-2010 is a potent pan-AKR1C inhibitor, effectively inhibiting AKR1C3, AKR1C4, AKR1C1, and AKR1C2 with IC50 values of 0.19, 0.36, 0.47, and 0.73 μM, respectively. This compound induces apoptosis in A549/DDP cells and enhances the cytotoxicity of chemotherapeutic agents in drug-resistant cells, making it a viable option for combating drug resistance. Furthermore, S07-2010 significantly inhibits the proliferation of drug-resistant cells [1].
T35439	(E)-5-(2-Bromovinyl)uracil
	(E)-5-(2-Bromovinyl)uracil (BVU) is a pyrimidine base and an inactive metabolite of the antiviral agents sorivudine and (E)-5-(2-bromovinyl)-2'-deoxyuridine (BVDU) that may be regenerated to BVDU in vivo. BVU irreversibly inactivates dihydropyrimidine dehydrogenase (DPD) in an NADPH-dependent manner. It enhances the efficacy of the chemotherapeutic agent and DPD substrate 5-fluorouracil in a P388 murine leukemia model when administered at a dose of 200 μmol/kg, increasing survival time.
T78841	Nrf2-IN-3
	Nrf2-IN-3 (Compound R16) 为Nrf2抑制剂，与KEAP1突变体 (G333C mKEAP1) 结合，能够恢复受损的KEAP1/NRF2相互作用。该化合物通过修复mKEAP1/NRF2复合物，增加KEAP1突变癌细胞对Cisplatin和Gefitinib的敏感性。
T72522	Aurora kinase-IN-1
	Aurora kinase-IN-1 是aurora kinase 的有效抑制剂。Aurora kinase-IN-1 上调 G1 细胞周期抑制蛋白 (包括 p21 和 p27) 以及 G1 进行性细胞周期蛋白 D1 的表达，并下调 G1-to-S 进行性细胞周期蛋白，导致细胞周期停滞在 G1/S 边界。Aurora 激酶-IN-1 还诱导细胞凋亡 (apoptosis）。Aurora 激酶-IN-1 是化疗药物的先导化合物。
T38503	(2-pyridyldithio)-PEG1-hydrazine (2-pyridyldithio)-PEG1-hydrazine
	(2-Pyridyldithio)-PEG1-hydrazine is a one-unit cleavable polyethylene glycol (PEG) linker specifically designed for the synthesis of antibody-drug conjugates (ADCs). This linker offers the advantage of controlled release of the drug payload from the ADC construct. It is utilized in the conjugation process between the antibody and the cytotoxic drug, enabling the targeted delivery of the drug to cancer cells. The (2-pyridyldithio) group of this linker provides stability during circulation in the ...
T36195	CAY10744
	CAY10744 is a topoisomerase II-α poison.1 It inhibits topoisomerase II-α by 78.9% when used at a concentration of 20 μM. CAY10744 is selective for topoisomerase II-α over topoisomerase I providing 100 and 0% inhibition, respectively, at 100 μM. It inhibits proliferation of HCT15 colon, T47D breast, DU145 prostate, and HeLa cervical cancer cells (IC50s = 0.014, 0.00267, 0.072, and 2.46 μM, respectively). CAY10744 induces apoptosis in T47D cells when used at concentrations of 10 and 30 μM. CAY1074...

化合物

Cat.No: T22223

Target: Glucokinase, Autophagy

Cat.No: T8979

Target: Nrf2

Cat.No: T38679

Cat.No: T69005

Cat.No: T68781

Cat.No: T69993

Mal-PEG8-Val-Ala-PAB-Exatecan

Cat.No: T77855

Cat.No: T69162

Cat.No: T61485

(E)-5-(2-Bromovinyl)uracil

Cat.No: T35439

Cat.No: T78841

Aurora kinase-IN-1

Cat.No: T72522

(2-pyridyldithio)-PEG1-hydrazine

Cat.No: T38503

Synonym: (2-pyridyldithio)-PEG1-hydrazine

Cat.No: T36195

Cat. No.	Product Name	Target	Signaling Pathways
T6S1683	Demethoxycurcumin Curcumin II,去甲氧基姜黄素,Desmethoxycurcumin,脱甲氧姜黄,Monodemethoxycurcumin	Apoptosis; Antioxidant; Antibacterial; Autophagy	Apoptosis; Autophagy; Microbiology/Virology; oxidation-reduction
	Demethoxycurcumin (Desmethoxycurcumin) 是姜黄素的主要活性成分，有抗炎和抗癌作用。
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。
TN2118	Lup-20(29)-en-28-oic acid Pulsatilla saponin D,白头翁皂苷D	ERK; mTOR; Autophagy	Autophagy; MAPK; PI3K/Akt/mTOR signaling
	Lup-20(29)-en-28-oic acid exhibits anticancer activities in various cancer types, it Inhibits autophagic flux and synergistically enhances the anticancer activity of chemotherapeutic agents against HeLa cells.Pulsatilla saponin D has strong haemolytic act
TN3348	(+)-Acuminatin Acuminatin	PAFR	GPCR/G Protein
	(+)-Acuminatin exerts hepatoprotective activities, perhaps by serving as a potent antioxidant. (+)-trans-Acuminatin, and (+)-cis-acuminatin show weak activity against platelet aggregation with IC50 values of 108.5 and 90.02 uM, respectively. (+)-Acuminatin, and machilin G show dose-dependent potent inhibitory activities against PLCgamma1 in vitro with IC50 values ranging from 8.8 to 26.0 microM, the inhibition of PLCgamma1 may be an important mechanism for an antiproliferative effect on the huma...

天然产物

Demethoxycurcumin

Cat.No: T6S1683

Synonym: Curcumin II,去甲氧基姜黄素,Desmethoxycurcumin,脱甲氧姜黄,Monodemethoxycurcumin

Target: Apoptosis, Antioxidant, Antibacterial, Autophagy

Cat.No: T4S1551

Synonym: Cinnamic Aldehyde,肉桂醛

Target: HIF

Lup-20(29)-en-28-oic acid

Cat.No: TN2118

Synonym: Pulsatilla saponin D,白头翁皂苷D

Target: ERK, mTOR, Autophagy

Cat.No: TN3348

Synonym: Acuminatin

Target: PAFR

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