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11

抑制剂 & 化合物

2

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T83638	IR820-PTX	Others	Others
	IR820-PTX 是一种由 IR-820 和紫杉醇组成的纳米颗粒，具有高渗透性且可靶向肿瘤。IR820-PTX 可用于近红外荧光成像和肿瘤诊断。
T19699	Triciribine phosphate TCN-P,VD 002,VQD-002	Apoptosis; Akt	Apoptosis; Cytoskeletal Signaling; PI3K/Akt/mTOR signaling
	Triciribine phosphate (VD 002) 是一种高选择性的 AKT 抑制剂，可诱导细胞周期停滞和半胱天冬酶依赖性细胞凋亡，抑制新生血管的生成，可用于研究白血病。
T16413	OTX008 Calixarene 0118,PTX008	Galectin	Immunology/Inflammation
	OTX008 (PTX008) 是半乳糖凝集素 1 选择性抑制剂。
T34056	PhTX-343 TFA (S)-PhTX 343,PhTX-343,(S)-PTX 343,(S)-Philanthotoxin 343,PhTX= 343
	PhTX-343, also known as Philanthotoxin 343, is synthetic analogue of Philanthotoxin 433. PhTX-343 blocks NMDA-gated ion channels; synthetic analog of the wasp polyamine amide toxin δ-philanthotoxin.
T80042	GpTx-1	Sodium Channel	Membrane transporter/Ion channel
	GpTx-1作为NaV1.7选择性抑制剂，具有高效性，其半抑制浓度(IC50)为10 nM。
T69976	WS-691
	WS-691 is a highly Potent and Orally Active ABCB1 Modulator. WS-691 significantly increased sensitization of ABCB1-overexpressed SW620/Ad300 cells to paclitaxel (PTX) (IC50 = 22.02 nM). WS-691 significantly increased the intracellular concentration of PTX and [3H]-PTX while decreasing the efflux of [3H]- PTX in SW620/Ad300 cells by inhibiting the efflux function of ABCB1. WS-691 could stabilize ABCB1 by directly binding to ABCB1 WS-691 increased the sensitivity of SW620/Ad300 cells to PTX in vi...
T64016	WS-898
	WS-898 是 ABCB1 的高效抑制剂，能够逆转耐药SW620/Ad300、KB-C2 和 HEK293/ABCB1 细胞对紫杉醇（PTX）的耐药性，他们的 IC50 值分别为 5.0、3.67 和 3.68 nM。
T36896	6α-hydroxy Paclitaxel 6alpha-hydroxypaclitaxel	Drug Metabolite	Metabolism
	6α-hydroxy Paclitaxel (6α-OH-PTX) 是抗癌化合物紫杉醇的主要代谢产物，具有部分细胞毒性。
T63267	P-gp/BCRP-IN-1
	P-gp/BCRP-IN-1 (compound 19) 是一种潜在的、相对安全的、口服有效的外排转运蛋白(P-gp 和 BCRP) 抑制剂。P-gp/BCRP-IN-1 通过抑制 P-gp 和BCRP 的外排功能产生耐药性逆转，P-gp/BCRP-IN-1可克服紫杉醇的耐药性，提高紫杉醇的口服生物利用度。
T72473	NOD1/2 antagonist-1
	NOD1/2 antagonist-1 是一种有效的NOD1/2双拮抗剂，其IC50值分别为 1.13 (NOD1) 和 0.77 μM (NOD2)。NOD1/2 antagonist-1 有可接受的 T1/2(67.6 min)。NOD1/2 antagonist-1 可提高紫杉醇 (PTX) 的抗肿瘤作用。
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...

化合物

Cat.No: T83638

Target: Others

Triciribine phosphate

Cat.No: T19699

Synonym: TCN-P,VD 002,VQD-002

Target: Apoptosis, Akt

Cat.No: T16413

Synonym: Calixarene 0118,PTX008

Target: Galectin

Cat.No: T34056

Synonym: (S)-PhTX 343,PhTX-343,(S)-PTX 343,(S)-Philanthotoxin 343,PhTX= 343

Cat.No: T80042

Target: Sodium Channel

Cat.No: T69976

Cat.No: T64016

6α-hydroxy Paclitaxel

Cat.No: T36896

Synonym: 6alpha-hydroxypaclitaxel

Target: Drug Metabolite

Cat.No: T63267

NOD1/2 antagonist-1

Cat.No: T72473

Cat.No: T69162

Cat. No.	Product Name	Target	Signaling Pathways
T0070	Pentoxifylline Oxpentifylline,PTX,己酮可可碱,BL-191	HIV Protease; PDE; Adenosine Receptor; Autophagy	Autophagy; GPCR/G Protein; Metabolism; Microbiology/Virology; Neuroscience; Proteases/Proteasome
	Pentoxifylline (PTX) 是一种具有口服活性的磷酸二酯酶非选择性抑制剂，具有免疫调节、抗炎、抗纤溶、抗增殖和血液流变学改善作用。它可研究周围血管疾病、脑血管疾病和其他一些涉及局部微循环缺陷的疾病。
T37219	N-Palmitoyl Glycine
	The acyl amides are a family of endogenous lipids that act as potent modulators of pain and inflammation. The best characterized members of this family are the arachidonoyl amides, which includes N-arachidonoyl ethanolamide (AEA; anandamide). N-palmitoyl glycine (PalGly) contains an 18-carbon saturated fatty acid that is amide-linked to glycine and is structurally similar to the phospholipid-derived N-acyl ethanolamines. Endogenously produced in rat skin and spinal cord, PalGly is present in 100...

天然产物

Cat.No: T0070

Synonym: Oxpentifylline,PTX,己酮可可碱,BL-191

Target: HIV Protease, PDE, Adenosine Receptor, Autophagy

N-Palmitoyl Glycine

Cat.No: T37219

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