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31

抑制剂 & 化合物

11

天然产物

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Cat. No. Product Name Target Signaling Pathways
T36674 DMU-212

Apoptosis; ERK Apoptosis; MAPK
DMU-212 是具有口服活性的白藜芦醇的甲基化衍生物,表现出抗分裂、抗增殖、抗氧化和促进细胞凋亡的活性。它通过诱导凋亡和激活ERK1/2蛋白阻止有丝分裂。
T1753 D-64131

Microtubule Associated Cytoskeletal Signaling
D64131 是一种微管蛋白聚合抑制剂,IC50 值为 0.53 μM。它具有抗丝分裂活性,可用于癌症研究。
T22661 CHM-1

Apoptosis; Others; Microtubule Associated Apoptosis; Cytoskeletal Signaling; Others
CHM-1 是细胞凋亡的诱导剂,通过激活 Cdc2 激酶活性在人肝细胞癌中显示出有效的抗肿瘤能力。 CHM-1 在体外和体内抑制微管蛋白聚合。
T10460 Batabulin

巴他布林,T138067

Apoptosis; Microtubule Associated Apoptosis; Cytoskeletal Signaling
Batabulin (T138067) 是一种抗肿瘤剂,可与 β-微管蛋白同种型的子集共价且选择性地结合,从而破坏微管聚合。它影响细胞形态并导致细胞周期停滞,最终诱导细胞凋亡。
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。
T4451 Estramustine phosphate sodium

Ro 21-8837/001,Estramustine phosphate disodium,雌莫司汀磷酸钠

Apoptosis; Microtubule Associated Apoptosis; Cytoskeletal Signaling
Estramustine phosphate sodium (Ro 21-8837/001) 是雌二醇类似物,是一种具有口服活性抗微管化疗剂,通过与微管相关蛋白和微管蛋白结合而使微管解聚。它可诱导前列腺癌细胞凋亡,可研究前列腺癌。
T0651 N-Phenylbenzylamine

Benzylaniline,Benzenemethanamine,N-苄基苯胺

Microtubule Associated Cytoskeletal Signaling
N-Phenylbenzylamine (Benzenemethanamine) 作为潜在的细胞毒性和抗有丝分裂剂,通过抑制微管蛋白聚合起作用。
T26046 Razoxane

Topoisomerase DNA Damage/DNA Repair
Razoxane 是拓扑异构酶 II 的有效抑制剂,具有抗血管生成的作用,在肾细胞癌中具有研究价值。
T6897 Monomethyl auristatin E

一甲基澳瑞他汀E,Vedotin,MMAE

Apoptosis; Microtubule Associated Apoptosis; Cytoskeletal Signaling
Monomethyl auristatin E (MMAE) 是海兔毒素 10 的合成衍生物,是一种抗有丝分裂剂,通过阻断微管蛋白的聚合来抑制细胞分裂,并且还具有抑制抗体-药物偶联物的活性。
T3256 MMAF

一甲基澳瑞他汀 F,MonoMethyl auristatin F

Others; Microtubule Associated Cytoskeletal Signaling; Others
MMAF (MonoMethyl auristatin F) 是一种抗有丝分裂剂,通过阻断微管蛋白的聚合来抑制细胞分裂,用作抗肿瘤药物和抗体偶联药物的细胞毒性成分。
T34787 TAS-119

TAS119,TAS2104,TAS 2104,TAS-2104,TAS 119

Aurora Kinase Cell Cycle/Checkpoint; Chromatin/Epigenetic
TAS-119 (TAS-2104) 是一种可口服且具有选择性和有效性的 Aurora A 抑制剂,IC50为1.0 nM。TAS-119 对 Aurora B 也具有抑制作用,IC50 为 95 nM。TAS-119 对 Aurora A 的亲和力比 Aurora B高。TAS-119 具有有效的抗肿瘤活性和潜在的抗有丝分裂活性。
T3124 Carbendazim

Bavistin,Carbendazole,多菌灵,Mercarzole

Antifungal Microbiology/Virology
Carbendazim (Mercarzole) 是一种具有抗肿瘤活性的苯并咪唑衍生物,可用于癌症研究。它是一种口服广谱苯并咪唑杀菌剂,可作为真菌疾病研究的杀虫剂。
T15576 Indibulin

2-(1-(4-氯苄基)-1H-吲哚-3-基)-2-氧代-N-(吡啶-4-基)乙酰胺,ZIO 301,D 24851

Apoptosis; Microtubule Associated Apoptosis; Cytoskeletal Signaling
Indibulin (D 24851) 是一种口服有效的微管蛋白合成抑制剂,具有抗有丝分裂和抗肿瘤活性,且神经毒性小。它降低了肌间神经张力,产生异常的纺锤体,激活有丝分裂检查点蛋白 Mad2 和 BubR1,并诱导有丝分裂停滞和细胞凋亡。
T69245 Amikhelline

Amikhelline is an antimitotic drug. It acts as a DNA intercalator and inhibits DNA polymerase.
T71924 AVE-8063

AVE-8063 is an antimitotic agent or microtubule inhibitor with potential anticancer activity.
T26391 5HPP-33

5HPP33

5HPP-33 is an microtubule-stabilizer with the properties of antiproliferative and antimitotic.
T16997 Tasidotin hydrochloride

ILX651

Microtubule Associated Cytoskeletal Signaling
Tasidotin hydrochloride is a peptide analog of the antimitotic depsipeptide dolastatin 15. Tasidotin hydrochloride is an inhibitor of microtubule assembly and microtubule dynamics.
T25290 DAT1

DAT-1,DAT 1

DAT1 is an antimitotic and antiangiogenic that acts by binding to the colchicine binding site of tubulin.
T15158 Dolastatin 15

DLS 15

Others Others
Dolastatin 15, a depsipeptide derived from Dolabella auricularia, is a potent antimitotic agent structurally related to the anti-tubulin agent Dolastatin 10. Dolastatin 15 can be used as an ADC cytotoxin and it induces cell cycle arrest and apoptosis in m
T68363 OUN10989

OUN10989, an analogue compound of LP-261, is a Potent Antimitotic Agent. OUN10989 exhibited potent inhibition of mitosis at the G2/M stage. OUN10989 was first reported in J. Med. Chem 54(1), 179-200; 2011 (compound 7). This product has no formal name at the moment. For the convenience of communication, a temporary code name was therefore proposed according to MedKoo Chemical Nomenclature (see web page: https://www.medkoo.com/page/naming).
T72552 Antitumor agent-88

Antitumor agent-88 表现出有效的抗有丝分裂活性并使细胞停滞在 G2/M 期。Antitumor agent-88 扰乱表达 CYP1A1 的乳腺癌细胞中的微管和细胞骨架。Antitumor agent-88 也是 CYP1A1的竞争性抑制剂 (Ki: 1.4 μM)。
T77874 Maytansinoid B

Maytansinoid B 是一种ADC Cytotoxin,用于形成与抗体结合的Antibody-Drug Conjugates (ADCs)。它是一种抗有丝分裂剂,能够结合微管蛋白并阻断其组装,诱导细胞周期在G2/M阶段停滞,进而触发细胞凋亡(apoptosis)。
T12141 N-Boc-Val-Dil-Dap-Doe

Others Others
N-Boc-Val-Dil-Dap-Doe is used to synthesize Dolastatin 10 , which is a potent antimitotic peptide, inhibits tubulin polymerization.
T70958 Dov-Val-Dil-OH TFA

Dov-Val-Dil-OH is a useful chemical intermediate for synthesis of auristatin-related compounds, such as Monomethyl auristatin E (MMAE), Auristatins are antimitotic agents which inhibits cell division by blocking the polymerisation of tubulin.
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...
T69283 Amikhellin HCl

Amikhellin HCl, an antimitotic drug, is a synthetic water-soluble derivative of khellin, an alkaloid extracted from seeds of Ammi Visnaga. Amikhellin has been used so far mostly as a vasodiator. Amikhellin binds to double-stranded DNA by an intercalation process. It inhibits the DNA-polymerase from murine sarcoma leukemia virus.
T74562 Nampt-IN-10 trihydrochloride

Nampt-IN-10 trihydrochloride (compound 4) 为磷酸核糖转移酶 (NAMPT) 抑制剂。在A2780与CORL23细胞中展现出活性,IC50值依次为5和19 nM。Nampt-IN-10 trihydrochloride 同时作为抗体偶联活性分子 (ADC) 的非限制性有效载荷。
T64273 Nampt-IN-10 TFA

Nampt-IN-10 TFA (compound 4) 是一种磷酸核糖转移酶 (NAMPT) 抑制剂。Nampt-IN-10 TFA 对 A2780 (IC50: 5 nM) 和 CORL23 (IC50: 19 nM) 具有细胞效能。Nampt-IN-10 TFA 能够用做 ADCs 的非抗有丝分裂有效载荷。
T22631 Dolastatin 10 trifluoroacetate

Others Others
Dolastatin 10 trifluoroacetate is a potent antimitotic polypeptide isolated from a marine animal and is developed as a potential antitumor agent. Dolastatin 10 is found to have an activity to inhibit tubulin polymerization (IC50: 1.2 μM). Besides that, it
T79708 SSE1806

SSE1806是鬼臼毒素(天然的抗有丝分裂剂)的一个衍生物,也是微管蛋白(Microtubule/Tubulin)的抑制剂,展现出显著的抗增殖和抗癌活性。该化合物抑制癌细胞生长的GI50在1.29-21.15 μM范围内。SSE1806能引发有丝分裂异常和G2/M期阻滞,升高p53蛋白的表达,并抑制结肠癌样器官的生长。此外,SSE1806能克服MDR-1高表达细胞系的多药耐药性。

化合物

DMU-212
Cat.No: T36674
Synonym:
Target: Apoptosis, ERK
D-64131
Cat.No: T1753
Synonym:
Target: Microtubule Associated
CHM-1
Cat.No: T22661
Synonym:
Target: Apoptosis, Others, Microtubule Associated
Batabulin
Cat.No: T10460
Synonym: 巴他布林,T138067
Target: Apoptosis, Microtubule Associated
Estramustine
Cat.No: T20681
Synonym: NSC-89201,NSC 89201,LEO 275,LEO275,雌莫司汀,NSC89201,LEO-275
Target: Microtubule Associated
Estramustine phosphate sodium
Cat.No: T4451
Synonym: Ro 21-8837/001,Estramustine phosphate disodium,雌莫司汀磷酸钠
Target: Apoptosis, Microtubule Associated
N-Phenylbenzylamine
Cat.No: T0651
Synonym: Benzylaniline,Benzenemethanamine,N-苄基苯胺
Target: Microtubule Associated
Razoxane
Cat.No: T26046
Synonym:
Target: Topoisomerase
Monomethyl auristatin E
Cat.No: T6897
Synonym: 一甲基澳瑞他汀E,Vedotin,MMAE
Target: Apoptosis, Microtubule Associated
MMAF
Cat.No: T3256
Synonym: 一甲基澳瑞他汀 F,MonoMethyl auristatin F
Target: Others, Microtubule Associated
TAS-119
Cat.No: T34787
Synonym: TAS119,TAS2104,TAS 2104,TAS-2104,TAS 119
Target: Aurora Kinase
Carbendazim
Cat.No: T3124
Synonym: Bavistin,Carbendazole,多菌灵,Mercarzole
Target: Antifungal
Indibulin
Cat.No: T15576
Synonym: 2-(1-(4-氯苄基)-1H-吲哚-3-基)-2-氧代-N-(吡啶-4-基)乙酰胺,ZIO 301,D 24851
Target: Apoptosis, Microtubule Associated
Amikhelline
Cat.No: T69245
Synonym:
Target:
AVE-8063
Cat.No: T71924
Synonym:
Target:
5HPP-33
Cat.No: T26391
Synonym: 5HPP33
Target:
Tasidotin hydrochloride
Cat.No: T16997
Synonym: ILX651
Target: Microtubule Associated
DAT1
Cat.No: T25290
Synonym: DAT-1,DAT 1
Target:
Dolastatin 15
Cat.No: T15158
Synonym: DLS 15
Target: Others
OUN10989
Cat.No: T68363
Synonym:
Target:
Antitumor agent-88
Cat.No: T72552
Synonym:
Target:
Maytansinoid B
Cat.No: T77874
Synonym:
Target:
N-Boc-Val-Dil-Dap-Doe
Cat.No: T12141
Synonym:
Target: Others
Dov-Val-Dil-OH TFA
Cat.No: T70958
Synonym:
Target:
Epofolate
Cat.No: T68232
Synonym:
Target:
E7974
Cat.No: T69003
Synonym:
Target:
Amikhellin HCl
Cat.No: T69283
Synonym:
Target:
Nampt-IN-10 trihydrochloride
Cat.No: T74562
Synonym:
Target:
Nampt-IN-10 TFA
Cat.No: T64273
Synonym:
Target:
Dolastatin 10 trifluoroacetate
Cat.No: T22631
Synonym:
Target: Others
SSE1806
Cat.No: T79708
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
T2773 Vindoline

文朵灵,文多灵

Microtubule Associated Cytoskeletal Signaling
Vindoline 是从长春花叶片中提取的一种生物碱,通过抑制微管组装而表现出抗有丝分裂活性。
T7565 3-Hydroxycapric acid

Endogenous Metabolite Metabolism
3-Hydroxycapric acid 是有丝分裂抑制剂。
TN2190 Scoulerine

Apoptosis; Beta-Secretase; BACE; Parasite Apoptosis; Microbiology/Virology; Neuroscience
Scoulerine 是抗有丝分裂化合物。它抑制细胞增殖,阻止细胞周期,并诱导癌细胞凋亡。它也是BACE1(淀粉样前体蛋白裂解酶 1) 的抑制剂。
TP1180 Dolastatin 10

尾海兔素10,NSC 376128,DLS 10

Microtubule Associated Cytoskeletal Signaling
Dolastatin 10 (DLS 10) 是一种多肽,可以抑制微管蛋白聚合,显示除抗有丝分裂的活性。
T2220 2-Methoxyestradiol

2-甲氧雌二醇,二甲氧基雌二醇,NSC-659853,2-MeOE2,2-ME2

Apoptosis; Reactive Oxygen Species; Microtubule Associated; Endogenous Metabolite; HIF; Autophagy Angiogenesis; Apoptosis; Autophagy; Chromatin/Epigenetic; Cytoskeletal Signaling; Immunology/Inflammation; Metabolism; NF-κB
2-Methoxyestradiol (2-ME2) 是一种口服生物可利用的雌二醇代谢物,具有抗肿瘤活性。它通过减少内皮细胞增殖和诱导内皮细胞凋亡来抑制血管生成,也可破坏微管的稳定。它可诱导半胱天冬酶活化,导致细胞周期停滞在 G2 期、DNA 断裂和细胞凋亡。
TN4747 (-)-beta-Peltatin

Others Others
(-)-beta-Peltatin has antimitotic, and antineoplastic activities.
T2S1797 Santalol

檀香醇;白檀油萜醇;檀香脑,檀香醇

Antioxidant; Antifungal Microbiology/Virology; oxidation-reduction
Santalol 是一种檀香醇的 α 和 β-异构体混合物。 其中α-santalol 分离自檀香油中,是一种有前途的抗癌药,能够预防口腔癌、前列腺癌、乳腺癌和皮肤癌。
T39610 Guattegaumerine

Guattegaumerine, a bisbenzylisoquinoline alkaloid, exhibits antimitotic, cytotoxic, and neuroprotective activities.
T10763 Ceratamine A

Others Others
Ceratamine A is an antimitotic heterocyclic alkaloid isolated from the marine sponge Pseudoceratina sp., acts as a microtubule-stabilizing agent with cytotoxicity against human cancer cell lines.
T73206 Wikstrol A

Wikstrol A 是一种有效的抗真菌剂、抗有丝分裂剂和抗HIV-1剂。Wikstrol A 诱导稻瘟病菌菌丝体的形态变形,MMDC 值为 70.1 µM。Wikstrol 对微管聚合具有活性,IC50值为 131 µM。Wikstrol A 显示抗HIV-1活性,IC50值为 67.8 µM。
TN4223 Homopterocarpin

Antifection Microbiology/Virology
Homopterocarpin and Pterocarpus extract offer gastroprotection against indomethacin- induced ulcer by antioxidative mechanism and the modulation of gastric homeostasis, homopterocarpin may be responsible for, or contribute to the antiulcerogenic property

天然产物

Vindoline
Cat.No: T2773
Synonym: 文朵灵,文多灵
Target: Microtubule Associated
3-Hydroxycapric acid
Cat.No: T7565
Synonym:
Target: Endogenous Metabolite
Scoulerine
Cat.No: TN2190
Synonym:
Target: Apoptosis, Beta-Secretase, BACE, Parasite
Dolastatin 10
Cat.No: TP1180
Synonym: 尾海兔素10,NSC 376128,DLS 10
Target: Microtubule Associated
2-Methoxyestradiol
Cat.No: T2220
Synonym: 2-甲氧雌二醇,二甲氧基雌二醇,NSC-659853,2-MeOE2,2-ME2
Target: Apoptosis, Reactive Oxygen Species, Microtubule Associated, Endogenous Metabolite, HIF, Autophagy
(-)-beta-Peltatin
Cat.No: TN4747
Synonym:
Target: Others
Santalol
Cat.No: T2S1797
Synonym: 檀香醇;白檀油萜醇;檀香脑,檀香醇
Target: Antioxidant, Antifungal
Guattegaumerine
Cat.No: T39610
Synonym:
Target:
Ceratamine A
Cat.No: T10763
Synonym:
Target: Others
Wikstrol A
Cat.No: T73206
Synonym:
Target:
Homopterocarpin
Cat.No: TN4223
Synonym:
Target: Antifection
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