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Search Results for " depolymerization "

14

抑制剂 & 化合物

4

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T20681	Estramustine NSC-89201,NSC 89201,LEO 275,LEO275,雌莫司汀,NSC89201,LEO-275	Microtubule Associated	Cytoskeletal Signaling
	Estramustine (LEO-275) 是一种与雌二醇相连的氮芥，通常为磷酸盐。它已被用于治疗前列腺肿瘤；还具有防辐射功能。它被前列腺细胞选择性吸收，并通过干扰微管动力学和降低血浆睾酮水平发挥抗肿瘤作用。
T6075	Epothilone B 帕妥匹隆,Patupilone,EPO 906	Apoptosis; Microtubule Associated; Antibiotic; Antifungal	Apoptosis; Cytoskeletal Signaling; Microbiology/Virology
	Epothilone B (EPO 906) 是微管稳定剂，Ki 为0.71 μM。它与αβ-微管蛋白异二聚体亚基结合，使αβ-微管蛋白解离减少。
T74418	Sudocetaxel
	Sudocetaxel 是一种可以用于pH 敏感的多西紫杉醇释放的微管解聚抑制剂。
T36726	6-keto Prostaglandin E1 6-keto Prostaglandin E1
	6-keto Prostaglandin E1 是 PGE1 的生物活性衍生物，在抗血小板聚集和解聚作用方面发挥作用。
T74648	TAM470
	TAM470 是一种新型的细胞溶素，可抑制微管蛋白聚集和微管解聚。TAM470 可作为有效载荷分子用于合成 OMTX705，OMTX705 是一种具有抗肿瘤活性的FAP 靶向抗体偶联活性分子 (ADCs)。
T40367	Combretastatin A-1 phosphate tetrasodium Combretastatin A-1 phosphate tetrasodium,OXi-4503 tetrasodium
	Combretastatin A-1 phosphate (OXi-4503) tetrasodium, a prodrug of Combretastatin A-1, is a tubulin-binding microtubule polymerization inhibitor that targets the colchicine-binding site. By inducing tubulin depolymerization, Combretastatin A-1 phosphate tetrasodium inhibits the Wnt/β-catenin pathway and leads to the deactivation of AKT. It possesses both anti-tumor and anti-vascular properties.
T69003	E7974
	E7974 is an analog of the sponge-derived anti-microtubule tripeptide hemiasterlin with antimitotic and potential antineoplastic activities. Hemiasterlin analog E7974 binds to the Vinca domain on tubulin, resulting in inhibition of tubulin polymerization and microtubule assembly; depolymerization of exsiting microtubules; inhibition of mitosis; and inhibition of cellular proliferation. This agent may have more affinity for the beta-3 tubulin isotype. Check for active clinical trials or closed cli...
T69480	Sagopilone
	Sagopilone is a fully synthetic low-molecular-weight epothilone with potential antineoplastic activity. Sagopilone binds to tubulin and induces microtubule polymerization while stabilizing microtubules against depolymerization, which may result in the inhibition of cell division, the induction of G2/M arrest, and apoptosis. The agent is not a substrate for the P-glycoprotein (P-gp) efflux pump and so may exhibit activity in multidrug-resistant (MDR) tumors. The epothilone class of metabolites wa...
T70808	Cabazitaxel-d6
	Cabazitaxel-d6 is a deuterium labeled cabazitaxel. Cabazitaxel is a semi-synthetic derivative of the natural taxoid 10-deacetylbaccatin III with potential antineoplastic activity. Cabazitaxel binds to and stabilizes tubulin, resulting in the inhibition of microtubule depolymerization and cell division, cell cycle arrest in the G2/M phase, and the inhibition of tumor cell proliferation. Unlike other taxane compounds, this agent is a poor substrate for the membrane-associated, multidrug resistance...
T70235	Cemadotin hydrochloride
	Cemadotin hydrochloride is the salt from of Cemadotin (free base), also known as, LU103793, a mitosis inhibitor potentially for the treatment of solid tumours. Cemadotin is also a synthetic derivative of Dolastatin 15, an antiproliferative compound which was isolated from the mollusk Dolabella auricularia. Like Dolastatin 15, LU103793 is highly cytotoxic in vitro (IC50 = 0.1 nM). LU103793 inhibits microtubule polymerization in a concentration-dependent manner (IC50 = 7 microM). Treatment with ...
T71577	KOS-1584
	KOS-1584 is a second-generation epothilone with potential antineoplastic activity. Epothilone KOS-1584 binds to tubulin and induces microtubule polymerization and stabilizes microtubules against depolymerization, which may result in the inhibition of cell division, the induction of G2/M arrest, and apoptosis. Compared to first-generation epothilones, this agent exhibits greater safety and efficacy with an enhanced pharmaceutical profile, including enhanced water solubility and tumor penetration,...
T68232	Epofolate
	Epofolate is folate receptor-targeting antimitotic agent with potential antineoplastic activity. Folate receptor-targeted epothilone BMS753493 contains an epothilone moiety linked to a single folate molecule. Mediated through the folate moiety, this agent delivers the antimitotic epothilone component into cells expressing folic acid receptors, frequently upregulated in many types of tumor cells. After ligand-receptor internalization, the epothilone moiety induces microtubule polymerization and s...
T69305	Milataxel
	Milataxel is an orally bioavailable taxane with potential antineoplastic activity. Upon oral administration, milataxel and its major active metabolite M-10 bind to and stabilize tubulin, resulting in the inhibition of microtubule depolymerization and cell division, cell cycle arrest in the G2/M phase, and the inhibition of tumor cell proliferation. Unlike other taxane compounds, milataxel appears to be a poor substrate for the multidrug resistance (MDR) membrane-associated P-glycoprotein (P-gp) ...
T68860	Iso-Fludelone
	Iso-Fludelone is the third-generation epothilone B analogue with potential anti-mitotic and antineoplastic activites. Iso-fludelone binds to tubulin and induces microtubule polymerization and stabilizes microtubules against depolymerization, which may result in the inhibition of cell division, the induction of G2/M arrest, and apoptosis. Compared to other generations of epothilones, iso-fludelone exhibits increased stability, water solubility, potency, duration of action, tumor penetration as we...

化合物

Cat.No: T20681

Synonym: NSC-89201,NSC 89201,LEO 275,LEO275,雌莫司汀,NSC89201,LEO-275

Target: Microtubule Associated

Cat.No: T6075

Synonym: 帕妥匹隆,Patupilone,EPO 906

Target: Apoptosis, Microtubule Associated, Antibiotic, Antifungal

Cat.No: T74418

6-keto Prostaglandin E1

Cat.No: T36726

Synonym: 6-keto Prostaglandin E1

Cat.No: T74648

Combretastatin A-1 phosphate tetrasodium

Cat.No: T40367

Synonym: Combretastatin A-1 phosphate tetrasodium,OXi-4503 tetrasodium

Cat.No: T69003

Cat.No: T69480

Cat.No: T70808

Cemadotin hydrochloride

Cat.No: T70235

Cat.No: T71577

Cat.No: T68232

Cat.No: T69305

Cat.No: T68860

Cat. No.	Product Name	Target	Signaling Pathways
T8678	Naphthazarin 萘茜,5,8-Dihydroxy-1,4-naphthoquinone,DHNQ	Apoptosis	Apoptosis
	Naphthazarin (5,8-Dihydroxy-1,4-naphthoquinone) 是来自毛紫草的一种天然产物，通过氧化应激、线粒体凋亡诱导因子的激活、微管的解聚、干扰溶酶体功能和 p53 依赖性 p21 激活，可触发细胞凋亡并具有抗肿瘤作用。
T1034	Docetaxel 多西他赛,NSC 628503,RP-56976,多烯紫杉醇	Apoptosis; Microtubule Associated; Endogenous Metabolite	Apoptosis; Cytoskeletal Signaling; Metabolism
	Docetaxel (RP-56976) 是紫杉醇的半合成类似物，是一种微管解聚抑制剂 (IC50=0.2 μM)。Docetaxel 可以减弱 bcl-2 和 bcl-xL 基因表达的影响，具有诱导凋亡、抗肿瘤活性。
TN5109	Taxezopidine L	Calcium Channel	Membrane transporter/Ion channel; Metabolism
	Taxezopidines K and taxezopidine L can markedly inhibit Ca2+-induced depolymerization of microtubules.
T15039	Cytochalasin E	Others	Others
	Cytochalasin E is a potent actin depolymerization agent and an epoxide containing Aspergillus-derived fungal metabolite. Cytochalasin E also inhibits angiogenesis and tumor growth. It binds and caps the barbed end of actin filaments to prevent actin elong

天然产物

Cat.No: T8678

Synonym: 萘茜,5,8-Dihydroxy-1,4-naphthoquinone,DHNQ

Target: Apoptosis

Cat.No: T1034

Synonym: 多西他赛,NSC 628503,RP-56976,多烯紫杉醇

Target: Apoptosis, Microtubule Associated, Endogenous Metabolite

Cat.No: TN5109

Target: Calcium Channel

Cat.No: T15039

Target: Others

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