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Search Results for " microtubules "

33

抑制剂 & 化合物

6

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T21632	Myoseverin	Others; Microtubule Associated	Cytoskeletal Signaling; Others
	Myoseverina 是多核肌管可逆分裂成单核片段的诱导剂，影响多种生长因子、免疫调节、细胞外基质重塑和应激反应基因的表达，与伤口愈合和组织再生相关通路的激活一致。
T20759	XRP44X XRP-44-X,XRP 44X,XRP-44X,XRP 44 X	Ras	GPCR/G Protein; MAPK
	XRP44X (XRP 44X) 是Ras 诱导的转录激活的抑制剂，IC50为 10 nM，通过 FGF-2 抑制 Ras-Erk-1/2 通路激活。它抑制Elk3。它还对微管有影响。
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。
T13807	OSIP-486823 CP248	Microtubule Associated; PKA	Cytoskeletal Signaling; Tyrosine Kinase/Adaptors
	OSIP-486823（CP248）是一种新型有效的微管干扰剂，对蛋白激酶 G (PKG) 和微管均具有亲和力。
T13687	Eribulin mesylate B1939 mesylate,甲磺酸艾日布林,ER-086526 mesylate,E7389 mesylate	Apoptosis; Others; Microtubule Associated	Apoptosis; Cytoskeletal Signaling; Others
	Eribulin mesylate (E7389 mesylate) 是一种靶向微管的抗癌剂，通过结合微管蛋白和微管来抑制癌细胞的增殖，可研究转移性乳腺癌。
T15713	Larotaxel XRP9881	P-gp	Membrane transporter/Ion channel; Neuroscience
	Larotaxel (XRP9881) 是一种紫杉烷类似物，具有抗癌活性，通过促进微管蛋白装配和稳定微管发挥其细胞毒性作用，并通过细胞凋亡诱导细胞死亡。Larotaxel (XRP9881) 是一种可穿过血脑屏障的化合物，对 Docetaxel 的亲和力比 P-糖蛋白 1 高，可用于研究乳腺癌和膀胱癌。
T28886	Suprafenacine N'-[(E)-(4-methylphenyl)methylidene]-4,5,6,7-tetrahydro-1H-indazole-3-carbohydrazide	Microtubule Associated	Cytoskeletal Signaling
	Suprafenacine (N'-[(E)-(4-methylphenyl)methylidene]-4,5,6,7-tetrahydro-1H-indazole-3-carbohydrazide) 是一种细胞渗透性微管去稳定剂，可在 G2/M 期诱导细胞周期停滞和细胞凋亡。它与微管结合并抑制秋水仙碱连接处的聚集。它对癌细胞有选择性，包括耐药癌细胞。
T70407	cemadotin free base LU103793 free base	Microtubule Associated	Cytoskeletal Signaling
	Cemadotin free base(LU103793 free base) 是一种新型的抗限定性肽，是一种新型的抗有丝分裂肽，是Dolastatin 15的类似物。Dolastatin 15是一种天然存在的细胞毒肽，可阻断有丝分裂并抑制微管（管蛋白），Ki 为1μM。Cemadotin 用于研究抗癌。
T30794	Centmitor-1 Centmitor 1
	Centmitor-1 is a novel mitotic inducer that modulates the positive end of microtubules and reduces microtubule dynamics.
T71278	IBPR002
	IBPR002 is an aurora kinase inhibitor which reveals mechanisms of HURP in nucleation of centrosomal and kinetochore microtubules.
T13688	Eribulin B1939,艾日布林,ER-086526,E7389	Others	Others
	Eribulin inhibits the proliferation of cancer cells by binding microtubule proteins and microtubules. Eribulin is a microtubule targeting agent that is used in the treatment of metastatic breast cancer.
T36364	Flutax-2
	Green fluorescent taxol derivative. Used for microtubule imaging. Binds microtubules with high affinity (Ka ~ 107M-1). Excitation/emission maximum λ ~ 496/526 nm. Lillo et al (2002) Location and properties of the Tax. binding center in microtubules: a picosecond laser study with fluorescent taxoids. Biochemistry. 41 12436 PMID:12369834 \|Diaz et al (2000) Molecular recognition of Tax. by microtubules. Kinetics and thermodynamics of binding of fluorescent Tax. derivatives to an exposed site. J.Bio...
T31389	Desmethyl-HD-800 Desmethyl-HD800,Desmethyl HD800
	Desmethyl-HD-800 is a PET precursor of preparing radiolabel [11C]HD-800, a high affinity brain penetrant PET tracer for imaging microtubules.
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.
T72503	Antitubulin agent 1
	Antitubulin agents-1 是一种抗微管蛋白剂，可诱导微管 (microtubules) (Microtubule/Tubulin) 破坏并增加 α-微管蛋白乙酰化。Antitubulin agents-1 具有抗癌作用。
T37733	AMP-PNP tetralithium
	Non-hydrolyzable AMP analog. Kir6 (KATP) channel blocker. Inhibits fast axonal transport and stabilizes the interaction of membranous organelles with microtubules. Brady (1985) A novel brain ATPase with properties expected for the fast axonal transport motor. Nature 317 73 PMID:2412134 \|Yount et al (1971) Adenylyl imidodiphosphate, an adenosine triphosphate analog containing a P-N-P linkage. Biochemistry 10 2484 PMID:4326768 \|Hehl and Neumcke (1994) KATP channels of mouse skeletal muscle: mechan...
T62966	IQTub4P
	IQTub4P 是一种有效的微管 (microtubule) 抑制剂。IQTub4P 在 HeLa 细胞中表现出细胞毒性 (EC50: 170 nM)。IQTub4P 在体内耐受良好，可以抑制微管结构和功能。
T18278	Mal-PEG2-VCP-Eribulin	Others	Others
	Mal-PEG2-VCP-Eribulin is a chemotherapeutic compound comprising an antibody-drug conjugate (ADC) linker (Mal-PEG2-VCP) and the microtubule inhibitor Eribulin[1]. This compound uniquely targets microtubules, offering a novel approach to cancer treatment. Eribulin is specifically utilized in creating targeted Eribulin-based drugs for antibody conjugates[1].
T28179	NMK-TD-100 NMK-TD 100,NMK-TD100
	NMK-TD-100 is a microtubule modulating agent with anti-proliferative activity by disrupting microtubule functions through tubulin binding. NMK-TD-100 blocks mitosis and induces apoptosis in HeLa cells by binding to tubulin. Polymerization of tissue purifi
T68570	TPI-287
	TPI 287 is a synthetic, third generation taxane with potential antineoplastic activity. TPI 287 binds to tubulin and stabilizes microtubules, resulting in inhibition of microtubule assembly/disassembly dynamics, cell cycle arrest at the G2/M phase, and apoptosis.
T80921	Tubulin/JAK2-IN-1
	Tubulin/JAK2-IN-1是一种针对Janus激酶2 (JAK2)和微管的双重抑制剂，在抑制癌细胞增殖方面展现出有效活性。
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...
T37066	9-(2,2-Dicyanovinyl)julolidine
	9-(2,2-Dicyanovinyl)julolidine (DCVJ) is a fluorogenic dye that is considered a fluorescent molecular rotor because its properties depend on the rotational relaxation of the molecule, which can be influenced by the viscosity of the solvent used. It has an excitation maximum at approximately 450 nm, and its emission is approximately 480 or 505 nm for low or high viscosity solvents, respectively. DCVJ has been used to study tubulin dynamics because its fluorescence increases when bound to tubulin ...
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.
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,...
T36358	Diminutol
	Diminutol is a cell-permeable purine derivative that inhibits the NADP-dependent oxidoreductase, NQO1 (Ki = 1.72 μM), to destabilize microtubules and disrupt mitosis. At 50 μM, it directly affects tubulin polymerization in Xenopus egg extracts without interfering with the activity of Cdk1, DNA replication, or actin polymerization.
T83814	8-Bromoguanosine-5'-O-triphosphate sodium 8-bromo GTP
	8-Bromoguanosine-5'-O-triphosphate是一种guanosine 5'-triphosphate (GTP)的衍生物，后者是蛋白质合成和糖异生作用的能量底物。该化合物在31.8 µM的浓度下抑制大肠杆菌的GTPase FtsZ（Ki = 31.8 µM），但在500 µM的浓度下，能促进在无细胞测定中猪脑微管的组装。
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...
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...
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...
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 ...
T70006	DHA-paclitaxel
	DHA-paclitaxel, also know as Taxoprexin, is prodrug comprised of the naturally occurring omega-3 fatty acid docosahexaenoic acid (DHA) covalently conjugated to the anti-microtubule agent paclitaxel. Because tumor cells take up DHA, DHA-paclitaxel is delivered directly to tumor tissue, where the paclitaxel moiety binds to tubulin and inhibits the disassembly of microtubules, thereby resulting in the inhibition of cell division. Paclitaxel also induces apoptosis by binding to and blocking the func...
T36856	UA 62784
	Inhibitor of microtubule polymerization in vitro. Interacts with tubulin dimers and promotes the accumulation of mammalian cells in apoptosis. Potentiates antiproliferative effects of vinblastine in H2B-GFP HeLa cells. Originally thought to inhibit CENP-E ATPase activity. Tcherniuk et al (2011) UA62784 is a cytotoxic inhibitor of microtubules, not CENP-E. Chem.Biol. 18 631 PMID:21609844 \|Maiato and Logarinho et al (2011) Motor-dependent and -independent roles of CENP-E at kinetochores: the cauti...

化合物

Cat.No: T21632

Target: Others, Microtubule Associated

Cat.No: T20759

Synonym: XRP-44-X,XRP 44X,XRP-44X,XRP 44 X

Target: Ras

Cat.No: T6075

Synonym: 帕妥匹隆,Patupilone,EPO 906

Target: Apoptosis, Microtubule Associated, Antibiotic, Antifungal

Cat.No: T13807

Synonym: CP248

Target: Microtubule Associated, PKA

Eribulin mesylate

Cat.No: T13687

Synonym: B1939 mesylate,甲磺酸艾日布林,ER-086526 mesylate,E7389 mesylate

Target: Apoptosis, Others, Microtubule Associated

Cat.No: T15713

Synonym: XRP9881

Target: P-gp

Cat.No: T28886

Synonym: N'-[(E)-(4-methylphenyl)methylidene]-4,5,6,7-tetrahydro-1H-indazole-3-carbohydrazide

Target: Microtubule Associated

cemadotin free base

Cat.No: T70407

Synonym: LU103793 free base

Target: Microtubule Associated

Cat.No: T30794

Synonym: Centmitor 1

Cat.No: T71278

Cat.No: T13688

Synonym: B1939,艾日布林,ER-086526,E7389

Target: Others

Cat.No: T36364

Desmethyl-HD-800

Cat.No: T31389

Synonym: Desmethyl-HD800,Desmethyl HD800

20-O-Demethyl-AP3

Cat.No: T40838

Synonym: 20-O-Demethyl-AP3

Antitubulin agent 1

Cat.No: T72503

AMP-PNP tetralithium

Cat.No: T37733

Cat.No: T62966

Mal-PEG2-VCP-Eribulin

Cat.No: T18278

Target: Others

Cat.No: T28179

Synonym: NMK-TD 100,NMK-TD100

Cat.No: T68570

Tubulin/JAK2-IN-1

Cat.No: T80921

Cat.No: T69480

9-(2,2-Dicyanovinyl)julolidine

Cat.No: T37066

Cat.No: T68686

Cat.No: T71577

Cat.No: T36358

8-Bromoguanosine-5'-O-triphosphate sodium

Cat.No: T83814

Synonym: 8-bromo GTP

Cat.No: T68232

Cat.No: T69003

Cat.No: T68860

Cemadotin hydrochloride

Cat.No: T70235

Cat.No: T70006

Cat.No: T36856

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。
T1270	Vincristine sulfate Leurocristine,22-Oxovincaleukoblastine sulfate,Leurocristine sulfate,硫酸长春新碱	Apoptosis; Microtubule Associated	Apoptosis; Cytoskeletal Signaling
	Vincristine sulfate (Leurocristine sulfate) 是一种抗肿瘤长春花生物碱。在细胞周期的 S 期不可逆地与微管(Ki: 85 nM) 和纺锤体蛋白结合，并干扰有丝分裂纺锤体的形成。
T21351	Maytansine NSC-153858,NSC153858,Maitansina,NSC 153858,Maitansine,美坦新	Microtubule Associated; Antibiotic	Cytoskeletal Signaling; Microbiology/Virology
	Maytansine (NSC-153858) 是从变叶美登木中分离的一种高效微管靶向天然产物，可诱导有丝分裂阻滞并在亚纳摩尔浓度杀死肿瘤细胞。
T3S0209	Vincristine	ERK; p38 MAPK; NF-κB; Akt; JNK; mTOR	Cytoskeletal Signaling; MAPK; NF-κB; PI3K/Akt/mTOR signaling
	Vincristine 与微管蛋白结合并抑制微管的形成，从而抑制癌细胞的有丝分裂。 Vincristine 可用作微管去稳定剂，用于研究治疗血液系统癌症，如白血病和淋巴瘤以及儿童肉瘤的相关研究。
TN5109	Taxezopidine L	Calcium Channel	Membrane transporter/Ion channel; Metabolism
	Taxezopidines K and taxezopidine L can markedly inhibit Ca2+-induced depolymerization of microtubules.
T24002	Disermolide XAA 296,XAA296,XAA-296
	Disermolide is a polyketide natural product found to stabilize microtubules. Disermolide was found to be a potent inhibitor of tumor cell growth in several MDR cancer cell lines.

天然产物

Cat.No: T8678

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

Target: Apoptosis

Vincristine sulfate

Cat.No: T1270

Synonym: Leurocristine,22-Oxovincaleukoblastine sulfate,Leurocristine sulfate,硫酸长春新碱

Target: Apoptosis, Microtubule Associated

Cat.No: T21351

Synonym: NSC-153858,NSC153858,Maitansina,NSC 153858,Maitansine,美坦新

Target: Microtubule Associated, Antibiotic

Cat.No: T3S0209

Target: ERK, p38 MAPK, NF-κB, Akt, JNK, mTOR

Cat.No: TN5109

Target: Calcium Channel

Cat.No: T24002

Synonym: XAA 296,XAA296,XAA-296

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