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Search Results for " macrocyclic "

59

抑制剂 & 化合物

8

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T7605	Avermectin B1a 阿维菌素 B1a,Abamectin B1a,Avamectin B1a	Antibiotic; Parasite	Microbiology/Virology
	Avermectin B1a 是能够使线虫瘫痪的一种抗寄生虫剂。
T13303	Virginiamycin M1 Pristinamycin IIA,Ostreogrycin A	Antibacterial	Microbiology/Virology
	Virginiamycin M1 (Pristinamycin IIA)是一种大环内酯肽类抗生素，是链菌素a 类抗生素的成员。
T19637	Aluminum phthalocyanine chloride Phthalocyanine Chloroaluminum,铝酞菁,Chloroaluminum Phthalocyanine	Others	Others
	Aluminum phthalocyanine chloride (Phthalocyanine Chloroaluminum) 是一种强烈的蓝绿色芳香大环化合物，广泛用于染色。
T4072	Methyl-β-cyclodextrin Methyl-beta-cyclodextrin,甲基-β-环糊精,甲基倍他环糊精,beta-Cyclodextrin methyl ethers	Others	Others
	Methyl-β-cyclodextrin (Methyl-beta-cyclodextrin) 是一种大环化合物，可以作为疏水性化合物的增溶剂用于生物实验中。Methyl-β-cyclodextrin 也是一种脂筏抑制剂，具有降胆固醇活性，还具有潜在抗肿瘤活性。
T4059	Selamectin UK-124114,司拉克丁,塞拉菌素	Chloride channel; P-gp; Parasite	Membrane transporter/Ion channel; Microbiology/Virology; Neuroscience
	Selamectin (UK-124114) 是半合成的大环内酯，是一种驱虫剂，可增强线虫中谷氨酸和 GABA 门控氯离子通道的开放。它还是抗寄生虫剂，可激活神经元和咽肌中的谷氨酸门控氯离子通道，以预防恶丝虫，淋巴丝虫和线虫感染。它还是 P-糖蛋白底物和抑制剂，IC50为 120 nM。
T0124	UK-124114 UNII-A2669OWX9N,西拉菌素,Selamectin	Others	Others
	UK-124114 (Selamectin) 是伊维菌素的大环内酯衍生物，伊维菌素是一种驱虫剂，可增强线虫中谷氨酸和 GABA 门控氯离子通道的开放。在 H. contortus 幼虫发育试验中，赛拉菌素 (0.1 µg/ml) 显示出生长抑制作用。
T24193	Janthinocin C
	Janthinocin C is a novel macrocyclic peptide lactone antibiotic.
T26076	Rhizoxin WF1360,WF 1360,WF-1360
	Rhizoxin is an antitumor drug isolated from the fungus Rhizopus chinensis. It is a macrocyclic lactone compound that binds to tubulin and inhibits microtubule assembly.
T24191	Janthinocin A
	Janthinocin A is a macrocyclic peptide lactone antibiotic.
T71383	NB-533
	NB-533 is a macrocyclic peptidic BACE-1 inhibitor.
T68278	NB-216
	NB-216 is a macrocyclic peptidic BACE-1 inhibitor.
T31258	Deacylgymnemic acid DAGA
	Deacylgymnemic acid is a macrocyclic compound for proteomics research.
T33544	Myrotoxin B Myrotoxin-B
	Myrotoxin B is a macrocyclic trichothecene first isolated in 1985.
T24195	Jatrophone NSC-135037,NSC135037,Jatropha principle,NSC 135037
	Jatrophone is a novel inhibitor of the macrocyclic diterpenoid tumor.
T70457	MDL-73669
	MDL-73669 is a macrocyclic HIV-protease inhibitor that contains a difluorostatone peptide mimetic.
T70422	MDL-104168
	MDL-104168 is a macrocyclic HIV-protease inhibitor.
T70458	FXIa-6f
	FXIa-6f is a high affinity, orally bioavailable macrocyclic FXIa inhibitor with antithrombotic activity in preclinical species
T24192	Janthinocin B
	Janthinocin B is a novel macrocyclic peptide lactone antibiotic.
T31360	Deepoxy-deoxynivalenol DOM-I,DOM-1
	Deepoxy-deoxynivalenol is Metabolite of deoxynivalenol. Deepoxydeoxynivalenol is a macrocyclic polyol compound for proteomics research. Environmental contaminants; Food contaminants.
T19098	2-Aminoethyl-mono-amide-DOTA-tris(tBu ester)	Others	Others
	2-Aminoethyl-mono-amide-DOTA-tris(tBu ester) is a macrocyclic DOTA derivative designed for tumor pretargeting.
T12033	Micrococcin P1 微球菌素 P1	HCV Protease	Microbiology/Virology; Proteases/Proteasome
	Micrococcin P1 is a macrocyclic peptide antibiotic and is a potent hepatitis C virus (HCV) inhibitor(EC50 range of 0.1-0.5 μM)
T25882	7-O-Demethyl rapamycin CJ 12263,CJ12263,7-O-Demethyl Rapammune,Novolimus (80%),7-O-Demethyl Cypher,Novolimus,CJ-12263
	Novolimus is a macrocyclic lactone with anti-proliferative properties. It has similar efficacy to currently available agents but requires a lower dose.
T68335	MK-1220
	MK-1220 is a novel Macrocyclic Inhibitor of Hepatitis C Virus NS3/4A Protease with Improved Preclinical Plasma Exposure.
T40838	20-O-Demethyl-AP3 20-O-Demethyl-AP3
	20-O-Demethyl-AP3 is a secondary metabolite derived from Ansamitocin P-3, and Ansamitocin P-3 is a macrocyclic antitumor antibiotic exerting its therapeutic effects by inhibiting microtubules.
T79719	8304-vs	Parasite	Microbiology/Virology
	8304-vs为一种大环类(antimalarial)化合物，以共价、不可逆的方式靶向疟原虫蛋白酶体，能有效抑制恶性疟原虫生长。
T8675	Vaniprevir	Others	Others
	Vaniprevir is a macrocyclic hepatitis C virus NS3/4a protease inhibitor and is active against both the genotype 1 and genotype 2 NS3/4a protease enzymes. vaniprevir has good plasma exposure and excellent liver exposure in multiple species.
T82650	Cy5-PEG7-endo-BCN
	Cy5-PEG7-endo-BCN为Cyanine 5 (Cy5)染料的PEGylated衍生物，具有7个聚乙二醇(PEG)单元和亲液性二齿大环配体endo-BCN。该化合物能在点击化学反应中与叠氮化合物无催化剂地共价耦合，形成稳定的1,2,3-三氮唑环。
T82958	ASGPR modulator-1
	ASGPR modulator-1（Compound 5TJX）为一大环化合物，专用于蛋白质间相互作用研究。
T71853	Enzastaurin HCl
	Enzastaurin HCl, also known as DB-102 and LY317615, is a synthetic macrocyclic bisindolemaleimide with potential antineoplastic activity. Binding to the ATP-binding site, Enzastaurin HCl selectively inhibits protein kinase C beta, an enzyme involved in the induction of vascular endothelial growth factor (VEGF)-stimulated neo-angiogenesis. This agent may decrease tumor blood supply and so tumor burden.
T11972	Mcl-1 inhibitor 3	BCL	Apoptosis
	Mcl-1 inhibitor 3 shows good pharmacokinetic properties and excellent in vivo efficacy without toxicity.Mcl-1 inhibitor 3 is a highly potent and orally activate macrocyclic Mcl-1 inhibitor (Ki= 0.061 nM; IC50=19 nM in an OPM-2 cell viability assay).
T34053	Phthalocyanine
	Phthalocyanine is an intensely blue-green-coloured aromatic macrocyclic compound that is widely used in dyeing. Phthalocyanine can be used as an agent for Photodynamic Therapy and Imaging. Phthalocyanines form coordination complexes with most elements of
T82678	Coumarin-C2-exo-BCN
	Coumarin-C2-exoBCN是一种Coumarin染料衍生物。该化合物含有亲脂性双齿大环配体exo-BCN，可用于合成大环复合物。在点击化学中，exo-BCN能在无催化剂条件下与含有叠氮基团的分子发生反应，生成稳定的三唑。
T82659	Cy3-PEG2-endo-BCN
	Cy3-PEG2-endo-BCN是一种Cy3染料衍生物，包含2个PEG单元及亲液性二齿大环配体endo-BCN。该化合物可用于合成大环配合物，且在点击化学反应中，endo-BCN能在无需催化剂的条件下与含叠氮基团的分子反应，形成稳定的三氮唑。
T80538	Lib2-1
	Lib2-1为大环肽类IL-17C/IL-17RE相互作用抑制剂，用于自身免疫与炎症疾病研究。
T82652	Cy5-PEG2-exo-BCN
	Cy5-PEG2-exo-BCN 为含Cyanine 5 (Cy5) 基团及2个PEG单元的染料衍生物，配备亲液性的二齿大环配体BCN，适用于进一步合成大环配合物。在点击化学应用中，该BCN能与含叠氮基团的分子在无需催化剂条件下形成稳定的三氮唑环结构。
T82651	Cy5-PEG3-endo-BCN
	Cy5-PEG3-endo-BCN是Cyanine 5染料衍生物，含有三个聚乙二醇(PEG)单元和亲液性二齿大环配体endo-BCN。该化合物可以用于合成大环配合物，且在点击化学反应中，endo-BCN能在无催化剂条件下与含有叠氮基团的分子反应形成稳定的三氮唑环。
T74390	VD2173
	VD2173 是一种HGF 激活丝氨酸蛋白酶的侧链环化大环肽抑制剂。VD2173 有效抑制matriptase 和hepsin。VD2173 可用于肺癌的研究。
T76276	Zilucoplan
	Zilucoplan (RA101495)为含15个氨基酸的大环肽，兼作有效的补体成分5 (C5) 抑制剂，适用于免疫介导的坏死性肌病 (IMNM) 研究。
T76231	Cyclotheonellazole A
	Cyclotheonellazole A为一天然大环肽类化合物，对弹性蛋白酶具显著的抑制效果（IC50=0.034 nM），且对糜蛋白酶亦有抑制作用，IC50值达0.62 nM。
T78042	JB-95 acetate
	JB-95 acetate 是一种 β-发夹大环肽，对大肠杆菌具有有效抗菌活性。该化合物能选择性破坏大肠杆菌外膜，而不影响其内膜。
T36885	BMSpep-57 hydrochloride
	BMSpep-57 hydrochloride, a potent macrocyclic peptide, competitively inhibits PD-1/PD-L1 interaction, exhibiting an IC50 value of 7.68 nM. It binds to PD-L1 with dissociation constants (Kds) of 19 nM and 19.88 nM as determined by MST and SPR assays, respectively. This compound enhances T cell functionality by promoting IL-2 production in PBMCs[1].
T69354	Enzastaurin 2HCl
	Enzastaurin 2HCl, also known as DB-102 and LY317615, is a synthetic macrocyclic bisindolemaleimide with potential antineoplastic activity. Binding to the ATP-binding site, Enzastaurin 2HCl selectively inhibits protein kinase C beta, an enzyme involved in the induction of vascular endothelial growth factor (VEGF)-stimulated neo-angiogenesis. This agent may decrease tumor blood supply and so tumor burden.
T63713	Mytoxin B
	Mytoxin B 是一种大环内脂，作用与 LY294002 相似，也是一种 ADC 细胞毒素 (ADC cytotoxin)。Mytoxin B 能够利用 PI3K/Akt 通路，进而诱导细胞凋亡 (apoptosis)。
T80083	Zilucoplan TFA RA101495 TFA	Complement System	Immunology/Inflammation
	Zilucoplan TFA (RA101495)为含15个氨基酸的大环肽，有效抑制补体组分5 (C5)。该化合物适用于免疫介导的坏死性肌病 (IMNM) 研究。
T39106	BMSpep-57
	BMSpep-57, a potent macrocyclic peptide inhibitor, competitively disrupts the PD-1/PD-L1 interaction, demonstrating a significant inhibitory concentration (IC50) of 7.68 nM. It exhibits binding affinity towards PD-L1 with dissociation constants (Kd) of 19 nM and 19.88 nM in MicroScale Thermophoresis (MST) and Surface Plasmon Resonance (SPR) assays, respectively. This compound enhances T cell functionality by promoting Interleukin-2 (IL-2) production within Peripheral Blood Mononuclear Cells (PBM...
T62150	Cap-dependent endonuclease-IN-25
	Cap-dependent endonuclease-IN-25 是一种大环吡啶并三嗪衍生物，也是一种 cap-dependent 核酸内切酶 (CEN) 的有效抑制剂。Cap-dependent endonuclease-IN-25 具有潜力进行由 Orthomyxoviridae 家族病毒引起的病毒感染的研究。
T76224	NH2-c[X-R-L-S-X]-K-G-P-(D-2Nal)
	NH2-c[X-R-L-S-X]-K-G-P-(D-2Nal) (化合物40) 作为 Ape13 的大环类似物，是一种 APJ 强效激动剂，具有较低的亲和力 (Ki=5.7 nM)。该化合物在 Gα12 路线上显示出优先的信号传递特性，并且在体内具有延长的半衰期。
T35746	Milbemycin A3
	Milbemycin A3 is a member of a complex family of macrocyclic lactones that contain a characteristic spiroketal group produced from the fermentation of soil bacterium S. hygroscopicus subsp. aureolacrimosus. As a compound that potentiates glutamate and GABA-gated chloride-channel opening, milbemycin A3 is used as a nematocide and insecticide. The acaricidal and nematocidal activity of a mixture of milbemycin A3 and milbemycin A4 against adult spider mites, spider mite eggs, and C. elegans are rep...
T82658	Cy3-PEG2-exo-BCN
	Cy3-PEG2-exo-BCN是Cyanine 3 (Cy3)的染料衍生物，含有2个PEG单元。Cy3-PEG2-exo-BCN含有亲脂性双齿大环配体BCN，可用于进一步合成大环复合物。在无催化剂的情况下，点击化学中的exo-BCN能与含有叠氮基团的分子反应，形成稳定的三唑。
T61424	OD36 hydrochloride OD 36 hydrochloride,OD-36 hydrochloride	ALK; RIP kinase	Angiogenesis; Apoptosis; NF-κB; Tyrosine Kinase/Adaptors
	OD36 hydrochloride (OD-36 hydrochloride) 是一种强效的 RIPK2 抑制剂，IC50 为 5.3 nM。OD36 hydrochloride 是一种大环抑制剂，可与 ALK2 激酶 ATP 口袋有效结合，能有效拮抗突变 ALK2 信号传导和成骨分化。OD36 hydrochloride 靶向作用于 ALK2，KD 为 37 nM。

化合物

Cat.No: T7605

Synonym: 阿维菌素 B1a,Abamectin B1a,Avamectin B1a

Target: Antibiotic, Parasite

Virginiamycin M1

Cat.No: T13303

Synonym: Pristinamycin IIA,Ostreogrycin A

Target: Antibacterial

Aluminum phthalocyanine chloride

Cat.No: T19637

Synonym: Phthalocyanine Chloroaluminum,铝酞菁,Chloroaluminum Phthalocyanine

Target: Others

Methyl-β-cyclodextrin

Cat.No: T4072

Synonym: Methyl-beta-cyclodextrin,甲基-β-环糊精,甲基倍他环糊精,beta-Cyclodextrin methyl ethers

Target: Others

Cat.No: T4059

Synonym: UK-124114,司拉克丁,塞拉菌素

Target: Chloride channel, P-gp, Parasite

Cat.No: T0124

Synonym: UNII-A2669OWX9N,西拉菌素,Selamectin

Target: Others

Cat.No: T24193

Cat.No: T26076

Synonym: WF1360,WF 1360,WF-1360

Cat.No: T24191

Cat.No: T71383

Cat.No: T68278

Deacylgymnemic acid

Cat.No: T31258

Synonym: DAGA

Cat.No: T33544

Synonym: Myrotoxin-B

Cat.No: T24195

Synonym: NSC-135037,NSC135037,Jatropha principle,NSC 135037

Cat.No: T70457

Cat.No: T70422

Cat.No: T70458

Cat.No: T24192

Deepoxy-deoxynivalenol

Cat.No: T31360

Synonym: DOM-I,DOM-1

2-Aminoethyl-mono-amide-DOTA-tris(tBu ester)

Cat.No: T19098

Target: Others

Cat.No: T12033

Synonym: 微球菌素 P1

Target: HCV Protease

7-O-Demethyl rapamycin

Cat.No: T25882

Synonym: CJ 12263,CJ12263,7-O-Demethyl Rapammune,Novolimus (80%),7-O-Demethyl Cypher,Novolimus,CJ-12263

Cat.No: T68335

20-O-Demethyl-AP3

Cat.No: T40838

Synonym: 20-O-Demethyl-AP3

Cat.No: T79719

Target: Parasite

Cat.No: T8675

Target: Others

Cy5-PEG7-endo-BCN

Cat.No: T82650

ASGPR modulator-1

Cat.No: T82958

Enzastaurin HCl

Cat.No: T71853

Mcl-1 inhibitor 3

Cat.No: T11972

Target: BCL

Cat.No: T34053

Coumarin-C2-exo-BCN

Cat.No: T82678

Cy3-PEG2-endo-BCN

Cat.No: T82659

Cat.No: T80538

Cy5-PEG2-exo-BCN

Cat.No: T82652

Cy5-PEG3-endo-BCN

Cat.No: T82651

Cat.No: T74390

Cat.No: T76276

Cyclotheonellazole A

Cat.No: T76231

Cat.No: T78042

BMSpep-57 hydrochloride

Cat.No: T36885

Enzastaurin 2HCl

Cat.No: T69354

Cat.No: T63713

Cat.No: T80083

Synonym: RA101495 TFA

Target: Complement System

Cat.No: T39106

Cap-dependent endonuclease-IN-25

Cat.No: T62150

NH2-c[X-R-L-S-X]-K-G-P-(D-2Nal)

Cat.No: T76224

Cat.No: T35746

Cy3-PEG2-exo-BCN

Cat.No: T82658

OD36 hydrochloride

Cat.No: T61424

Synonym: OD 36 hydrochloride,OD-36 hydrochloride

Target: ALK, RIP kinase

Cat. No.	Product Name	Target	Signaling Pathways
TN6732	Oenothein B	Apoptosis; HCV Protease; Antibacterial; Antifungal	Apoptosis; Microbiology/Virology; Proteases/Proteasome
	Oenothein B 是一种聚（ADP-核糖）糖水解酶的特异性抑制剂。 Oenothein B 具有抗氧化、抗炎、抗真菌、抗 HCV 和抗肿瘤特性。
T9327	ω-Pentadecalactone Cyclopentadecanolide,ω-十五内酯,Oxacyclohexadecan-2-one,Exaltolide,Pentadecanolide	Others	Others
	ω-Pentadecalactone (Exaltolide) 是香料成分，是一种香味结构组大环内酯和丙交酯衍生物的成员。
T9076	Spinosad	Others	Others
	Spinosad 是在土壤细菌 S. spinosa 中发现的一种杀虫剂，是大环内酯多杀菌素 A 和多杀菌素 D 的混合物，可作为昆虫烟碱乙酰胆碱酯酶受体 (nAChRs) 的激动剂。它具有优良的环境和哺乳动物毒理学特征，以及杀灭幼虫的活性。
T16340	Nosiheptide RP 9671,Multhiomycin,那西肽	Antibacterial; Antibiotic	Microbiology/Virology
	Nosiheptide (Multhiomycin) 是一种由 Streptomyces actuosus 生产的硫肽类抗生素，已被广泛用作动物生长的饲料添加剂。它抑制细菌蛋白质合成，并在特征性大环核心上带有独特的吲哚侧环系统和区域特异性羟基。
T75493	Ellipyrone B
	Ellipyrone B，一种大环肽，对二肽基肽酶 4 (dipeptidyl peptidase-4: IC50=0.48 mM) 表现出抑制作用。
T75529	Malacidin B
	Malacidin B 是一种大环脂肽抗生素，以钙依赖的方式发挥抗菌活性。
T38243	Hygrolidin
	Hygrolidin is a macrocyclic lactone originally isolated from S. hygroscopicus. It inhibits proliferation of a variety of cancer cell lines, including DLD-1 colon cancer, LNCaP prostate cancer, and K562 leukemia cells (IC50s = 2.9, 5.2, and 33 ng/ml, respectively). Hygrolidin induces the expression and levels of p21 in DLD-1 cells, but not WI-38 fibroblasts, and leads to cell accumulation in the G1 and S phases without inducing apoptosis. It has antiparasitic activity against T. cruzi, L. donovan...
T75492	Ellipyrone A
	Ellipyrone A为一种大环肽，对二肽基肽酶 4 (dipeptidyl peptidase-4: IC50=0.35 mM) 显示出抑制活性，并对α-葡萄糖苷酶 (IC50=0.74 mM) 及α-淀粉酶 (IC50=0.59 mM) 也具有明显的抑制效果，表现出其抗碳水化合物分解的性能。

天然产物

Cat.No: TN6732

Target: Apoptosis, HCV Protease, Antibacterial, Antifungal

ω-Pentadecalactone

Cat.No: T9327

Synonym: Cyclopentadecanolide,ω-十五内酯,Oxacyclohexadecan-2-one,Exaltolide,Pentadecanolide

Target: Others

Cat.No: T9076

Target: Others

Cat.No: T16340

Synonym: RP 9671,Multhiomycin,那西肽

Target: Antibacterial, Antibiotic

Cat.No: T75493

Cat.No: T75529

Cat.No: T38243

Cat.No: T75492

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