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25

抑制剂 & 化合物

2

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T19235	CHAPS	Others	Others
	CHAPS 是一种两性离子洗涤剂，是一种 Cholic acid 的衍生物，可溶解膜蛋白。它用于稳定各种蛋白质-DNA 复合物，并可以保留溶液中蛋白质的生化活性。
T32781	Lipofundin S Phospholipid - stabilized soybean oil,Intralipid,Intralipid 20,Medialipid,Lipofundin S 10
	Lipofundin S is an emulsion containing soybean oil, glycerol, and soy phosphatides.
T17203	UNC0224	Histone Methyltransferase	Chromatin/Epigenetic
	UNC0224 是 G9a 的特异性抑制剂，Ki 为 2.6 nM，IC50 为 15 nM。 UNC0224 还有效抑制 GLP，IC50 值为 20-58 nM。
T39508	KY-02327	Others	Others
	KY-02327 是 KY-02061的一种类似物，具有代谢稳定性。KY-02327是Dishevelled (Dvl)-CXXC5相互作用抑制剂。KY-02327激活Wnt/β-catenin 途径，从而促进成骨细胞分化。
T32589	Laudanidine Tritopin,Tritopine,L-Laudanine
	Laudanidine is a nitrile-stabilized ammonium ylide.
T34457	RX 783030 RX783030,RX-783030
	RX 783030 is an enkephalin analog that is stabilized.
T69998	DG046
	DG046 is a novel potent phosphinic pseudopeptide ERAP1 inhibitor, binding in the ERAP1 active site, being stabilized by an unusual extensive network of π-stacking interactions
T24639	PIH pyrimidine-indole hybrid
	PIH is a ciliogenesis inhibitor by microtubule destabilization that acts by antagonizing Hh signaling by repressing cilia biogenesis and disassembly of alpha-tubulin in its stabilized form.
TP2117	SAHM1
	Notch pathway inhibitor - stabilized hydrocarbon-stapled alpha helical peptide. Targets the protein-protein interface and prevents Notch complex assembly.
T18722	MAC glucuronide α-hydroxy lactone-linked SN-38	Others	Others
	MAC glucuronide α-hydroxy lactone-linked SN-38 (Topoisomerase I inhibitor) is a stabilized lactone MAC glucuronide α-hydroxy lactone-linked SN-38 drug linker. MAC glucuronide α-hydroxy lactone-linked SN-38 is cytotoxic across L540cy cells and Ramos cells
T68686	DAP-81
	DAP-81 is a diaminopyrimidine derivative that targets PLKs, destabilizing kinetochore microtubules. Other spindle tubules are stabilized, resulting in monopolar mitotic spindles. In vitro, DAP-81 inhibits Plk1 at an IC50 of 0.9 nM. DAP-81 is currently in ongoing preclinical evaluations.
T11059	DM4-SMe	Others	Others
	DM4-SMe is a cytotoxic part of antibody-drug conjugates (ADCs) and a metabolite of antibody-maytansin conjugates (AMCs) and tubulin inhibitors, which can also be stabilized by disulfide bonds or thioether The bond binds to the antibody. The IC50 of DM4-SM
T27210	DRX-065 DRX 065,DRX065,deuterated R-enantiomer of pioglitazone
	DRX-065 is a stabilized and deuterated R-enantiomer of pioglitazone. DRX-065 has pharmacological properties desirable for the treatment of NASH (mitochondrial function modulation, non-steroidal anti-inflammatory effects, and glucose lowering effects) with
T80454	BmK-M1	Sodium Channel	Membrane transporter/Ion channel
	BmK-M1，一种含64个氨基酸通过四个二硫桥交联形成的蝎子毒素，作用于抑制Na+通道，属于心脏毒素和神经毒素类。
T76694	Odronextamab
	Odronextamab是一种IgG4型的人源化、稳定性CD20×CD3双特异性抗体，能够同时与T细胞上的CD3和B细胞上的CD20结合。
T80078	Calciseptin	Calcium Channel	Membrane transporter/Ion channel; Metabolism
	Calciseptine 是从黑曼巴Dendroaspis p. polylepis分离得到的天然神经毒素。含有60个氨基酸和四个二硫键，特异性阻断L型钙通道（calcium channel）[1]。
T80040	Polyphemusin I
	Polyphemusin I 是一种具有卓越抗菌活性的天然抗菌肽，能有效对抗革兰氏阴性菌和革兰氏阳性菌。该化合物由 18 个氨基酸组成，并通过两个二硫桥形成稳定的两亲性反向平行 β-发夹结构。
T69936	NK314
	NK314 is a novel synthetic benzo[c]phenanthridine alkaloid that shows strong antitumor activity. It inhibited topoisomerase II activity and stabilized topoisomerase II-DNA cleavable complexes. The DNA breaks occurred within 1h after treatment with NK314 even without digestion of topoisomerase II by proteinase K, whereas etoposide required digestion of the enzyme protein in cleavable complex to detect DNA breaks. Pretreatment with topoisomerase II catalytic inhibitors, ICRF-193 and suramin, reduc...
T71500	Palifosfamide tromethamine IPM tromethamine,Isophosphoramide mustard tromethamine,ZIO-201 tromethamine,Isophosphoramide mustard tromethamine ; IPM tromethamine ; ZIO-201 tromethamine
	Palifosfamide (tromethamine) 是一种具有潜在抗肿瘤活性的合成烷基化剂。作为异环磷酰胺 (ifosfamide) 稳定的活性代谢物，Palifosfamide (tromethamine) 通过GC 碱基对不可逆地烷基化和交联DNA，导致了DNA 复制的抑制，并导致细胞死亡。与异环磷酰胺相比，Palifosfamide (tromethamine)的毒性较小。
T76506	Coibamide A
	Coibamide A 是一种 N-甲基稳定的细胞毒性缩酚肽，具有强大的抗增殖活性。Coibamide A 通过mTOR 独立机制诱导自噬体积累。Coibamide A 诱导细胞凋亡。Coibamide A 抑制VEGFA/VEGFR2表达并抑制胶质母细胞瘤异种移植物中的肿瘤生长。
TP1533	HIF-1 alpha (556-574) HIF-1 alpha 556-574
	HIF-1 alpha (556-574) is a hypoxia-inducible factor-1 19-mer fragment. HIF-1 functions as master regulator of response to oxygen homeostasis. Hypoxia-induced gene expression is initiated when HIF-1subunit is stabilized in response to a lack of oxygen. Thi
TP2301	type II collagen fragment	Others	Others
	Type II collagen is composed of a triple helix of three identical α chains. These molecules associate to form a fibril that is stabilized by intermolecular crosslinks1. Damage to the fibrillar meshwork, made up of primarily type II collagen (z 90–95%), ma
T63884	IZTZ-1
	IZTZ-1 是一种 c-MYC G4配体，是咪唑-苯并噻唑缀合物。IZTZ-1 能够稳定 c-MYC G4，并下调 c-MYC 的表达。IZTZ-1 能够阻滞细胞周期，并诱导细胞凋亡 (apoptosis)，能够抑制 B16 细胞的增殖。IZTZ-1 表现出抗肿瘤作用，能够用于研究黑色素瘤。
TP1546	HIF-1 alpha (556-574) TFA (1201633-99-9 free base) HIF-1 alpha (556-574) TFA
	This is a hypoxia-inducible factor-1 (HIF-1 a) 19-mer fragment. HIF-1 functions as master regulator of response to oxygen homeostasis. Hypoxia-induced gene expression is initiated when HIF-1 subunit is stabilized in response to a lack of oxygen. This part
T82841	BODIPY FL hydrazide
	BODIPY FL Hydrazide 是一种与多糖和糖蛋白上的醛/酮反应形成席夫碱的绿色荧光染料，通过还原剂，如硼氢化钠或氰硼氢化钠，可以产生稳定的链接物。（λex=495 nm，λem=516 nm）。

化合物

Cat.No: T19235

Target: Others

Cat.No: T32781

Synonym: Phospholipid - stabilized soybean oil,Intralipid,Intralipid 20,Medialipid,Lipofundin S 10

Cat.No: T17203

Target: Histone Methyltransferase

Cat.No: T39508

Target: Others

Cat.No: T32589

Synonym: Tritopin,Tritopine,L-Laudanine

Cat.No: T34457

Synonym: RX783030,RX-783030

Cat.No: T69998

Cat.No: T24639

Synonym: pyrimidine-indole hybrid

Cat.No: TP2117

MAC glucuronide α-hydroxy lactone-linked SN-38

Cat.No: T18722

Target: Others

Cat.No: T68686

Cat.No: T11059

Target: Others

Cat.No: T27210

Synonym: DRX 065,DRX065,deuterated R-enantiomer of pioglitazone

Cat.No: T80454

Target: Sodium Channel

Cat.No: T76694

Cat.No: T80078

Target: Calcium Channel

Cat.No: T80040

Cat.No: T69936

Palifosfamide tromethamine

Cat.No: T71500

Synonym: IPM tromethamine,Isophosphoramide mustard tromethamine,ZIO-201 tromethamine,Isophosphoramide mustard tromethamine ; IPM tromethamine ; ZIO-201 tromethamine

Cat.No: T76506

HIF-1 alpha (556-574)

Cat.No: TP1533

Synonym: HIF-1 alpha 556-574

type II collagen fragment

Cat.No: TP2301

Target: Others

Cat.No: T63884

HIF-1 alpha (556-574) TFA (1201633-99-9 free base)

Cat.No: TP1546

Synonym: HIF-1 alpha (556-574) TFA

BODIPY FL hydrazide

Cat.No: T82841

Cat. No.	Product Name	Target	Signaling Pathways
T7966	3-O-Ethyl-L-ascorbic acid	Tyrosinase	Proteases/Proteasome
	3-O-Ethyl-L-ascorbic acid 是一种具有增白能力的化妆品酪氨酸酶 (tyrosinase) 抑制剂，是一种稳定的维生素 C 衍生物。它还具有抗氧化能力。
T75319	Taurodeoxycholic acid Taurodeoxychloic acid	Apoptosis; Calcium Channel; Caspase	Apoptosis; Membrane transporter/Ion channel; Metabolism; Proteases/Proteasome
	Taurodeoxycholic acid (Taurodeoxychloic acid) 是脱氧胆酸的胆汁酸牛磺酸共轭物，是一种人体代谢物，可稳定线粒体膜，减少自由基形成。Taurodeoxycholic acid 通过阻断钙介导的凋亡通路以及 Caspase-12 激活来抑制凋亡 (apoptosis)。Taurodeoxycholic acid具有神经保护活性，可用于研究 3-硝基丙酸诱导或稳定遗传的亨廷顿舞蹈病 (HD) 。

天然产物

3-O-Ethyl-L-ascorbic acid

Cat.No: T7966

Target: Tyrosinase

Taurodeoxycholic acid

Cat.No: T75319

Synonym: Taurodeoxychloic acid

Target: Apoptosis, Calcium Channel, Caspase

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