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Search Results for " colchicine "

39

抑制剂 & 化合物

6

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T30999	Colchicine, deacetamido-5,6-didehydro- Deacetamido-6-dehydrocolchicine,Colchicine,deacetamido-6-dehydro- (7CI)
	Colchicine, deacetamido-5,6-didehydro- is a biochemical.
T31000	Colchicine, N-deacetyl-10-thio- N-Deacetylthiocolchicine,Desacetyl thiocolchicine,Deacetylthiocolchicine
	Colchicine, N-deacetyl-10-thio- is a biochemical.
T41248	Thiocolchicine	Microtubule Associated	Cytoskeletal Signaling
	Thiocolchicine 是一种有效的微管蛋白聚合抑制剂，IC50 为 2.5 µM，Ki 为 0.7 µM。 Thiocolchicine 诱导细胞凋亡。 Thiocolchicine 可用作 ADC 技术中的 ADC 细胞毒素。
T15012	Crolibulin EPC2407	Microtubule Associated	Cytoskeletal Signaling
	Crolibulin (EPC2407) 是一种微管蛋白聚合抑制剂，具有诱导凋亡和抑制细胞生长的作用。它有抗肿瘤活性，还具有心血管毒性和神经毒性。
T9812	Tubulin inhibitor 24	Microtubule Associated	Cytoskeletal Signaling
	Tubulin inhibitor 24 是一种 tubulin 抑制剂，可以抑制微管蛋白聚合，以浓度依赖性方式诱导细胞周期停滞在 G2/M 期，具有抗肿瘤活性且无明显毒性。
T31906	gamma-Lumicolchicine
	gamma-Lumicolchicine is three, alpha, beta, and gamma isomers of ultraviolet degradation products of colchicine that lack many of the physiological actions of the parent; used as experimental control for colchicine actions.
T72544	4-Formylcolchicine
	4-Formylcolchicine 为一有效抗癌化合物，展示对 A549、HT-29、HCT116 细胞具有细胞毒性活性，其 IC50 值分别为 1.007 µM、0.128 µM、0.054 µM。
T32946	Lumicolchicine
	Lumicolchicine is a bioactive chemical.
T31244	Deacetylisocolchicine
	Deacetylisocolchicine is a biochemical.
T31255	Deacetylthiocolchicine hydrochloride Deacetylthiocolchicine chlorhydrate,Deacetylthiocolchicine HCl
	Deacetylthiocolchicine hydrochloride is a biochemical.
T77647	Tubulin polymerization-IN-43	Apoptosis; Microtubule Associated	Apoptosis; Cytoskeletal Signaling
	Tubulin polymerization-IN-43 是一种微管蛋白聚合 (tubulin polymerization) 抑制剂。Tubulin polymerization-IN-43 具有多种作用，通过靶向 Colchicine 位点破坏细胞微管网络，促进白血病细胞的细胞周期停滞在 G2/M 期和细胞凋亡 (apoptosis)。Tubulin polymerization-IN-43 具有抗血管生成活性。
T60009	YS-370	P-gp	Membrane transporter/Ion channel; Neuroscience
	YS-370 是一种具有口服活性的 P-gp 抑制剂，对 CYP3A4 有中度抑制作用。 YS-370 有效逆转对紫杉醇和秋水仙碱的多药耐药性，与紫杉醇联合应用表现出更强的抗肿瘤活性。
T67935	Tubulin inhibitor 11	Apoptosis; Microtubule Associated	Apoptosis; Cytoskeletal Signaling
	Tubulin inhibitor 11 是一种口服活性的有效微管蛋白抑制剂。它通过靶向秋水仙碱结合位点，抑制tubulin聚合，进而促进有丝分裂阻断和apoptosis。
T9595	LP-261	Microtubule Associated	Cytoskeletal Signaling
	LP-261 是一种新型的微管蛋白靶向抗癌剂，可与微管蛋白上的秋水仙碱位点结合，诱导 G2/M 期阻滞，其EC50为 3.2 μM。它可抑制人非小细胞肺癌的生长，可用于癌症研究。
T2511	Plinabulin 普那布林,NPI-2358	Microtubule Associated	Cytoskeletal Signaling
	Plinabulin (NPI-2358) 是一种抗微管蛋白解聚肿瘤细胞的血管破坏剂，选择性地靶向并结合到微管蛋白的秋水仙碱结合位点，从而中断微管动力学的平衡。它对人肿瘤细胞系具有抑制作用，对 HT-29 细胞系的IC50值为 9.8 nM。
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。
T61084	Tubulin polymerization-IN-37
	Tubulin polymerization-IN-37 is a potent inhibitor (IC50: 2.3 μΜ) of tubulin polymerization by binding specifically to the colchicine site of tubulin and preventing colchicine binding. It has potential applications in cancer research, notably for lymphomas [1].
T28048	Mivobulin Isethionate NSC-613863,CI-980,NSC-635370,NSC-613862,NSC-350386
	Mivobulin is a tubulin inhibitor potentially for the treatment of glioma, malignant melanoma, prostate, ovarian cancer. CI-980 acts at the colchicine-binding site.
T68873	Cornigerine
	Cornigerine is a natural product analog of colchicine produced by Colchicum cornigerum that inhibited tubulin polymerization both with and without microtubule-associated proteins, inhibited the binding of radiolabeled colchicine to tubulin, and stimulated tubulin-dependent GTP hydrolysis.
T25290	DAT1 DAT-1,DAT 1
	DAT1 is an antimitotic and antiangiogenic that acts by binding to the colchicine binding site of tubulin.
T71974	ABI-274
	ABI-274 is a novel potent colchicine binding site inhibitor (CBSI) and tubulin inhibitor.
T60758	Tubulin polymerization-IN-36
	Tubulin polymerization-IN-36 可用于癌症研究，例如淋巴癌。Tubulin polymerization-IN-36 结合微管蛋白的秋水仙碱位点并且抑制秋水碱结合，是一种微管蛋白聚合的抑制剂，IC50值为 2.8 μM。
T21317	Avanbulin BAL27862,BAL-27862,BAL 27862
	Avanbulin is a potent inhibitor of tubulin polymerization with antitumor activity. It elicits a unique microtubule (MT) phenotype, distinct from colchicine, paclitaxel, and vinblastine has broad in vitro anti-proliferative activity against a diverse range
T61728	MY-875
	MY-875 is a potent microtubulin polymerization inhibitor that competes at colchicine binding sites, exhibiting an IC50 value of 0.92 μM. It effectively suppresses microtubulin polymerization, exerting its inhibitory effect. Additionally, MY-875 exerts its biological impact by activating the Hippo pathway, inducing apoptosis, and displaying commendable anticancer activity [1].
T69557	ABI-231 HCl
	ABI-231 is a potent, orally bioavailable tubulin inhibitor that interacts with the colchicine binding site and is currently undergoing clinical trials for prostate cancer. ABI-231, has an average IC50 = 5.2 nM against panels of melanoma and prostate cancer cell lines, is orally bioavailable, and strongly suppress melanoma tumors in vivo. ABI-231 holds great promise as a new generation of orally available tubulin inhibitor.
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.
T72167	Tubulin polymerization-IN-39
	Tubulin polymerization-IN-39，一种以IC50为4.9μM抑制微管蛋白聚合，通过占据秋水仙碱结合位点来实现其作用。此外，Tubulin polymerization-IN-39能有效抑制癌细胞增殖。
T80922	Tubulin polymerization-IN-56
	Tubulin polymerization-IN-56（compound 8l），一种吲唑衍生的微管蛋白聚合抑制剂，通过与秋水仙碱位点的相互作用，能够引发细胞周期停滞与细胞凋亡。该化合物还能降低细胞迁移并在体内更有效地抑制肿瘤生长。
T79341	Tubulin polymerization-IN-45
	Tubulin polymerization-IN-45 是针对微管蛋白的靶向抑制剂，通过与微管蛋白秋水仙碱结合位点相结合，能够诱导肝细胞癌细胞 (HCC) 发生细胞凋亡 (apoptosis)。
T61880	Tubulin polymerization-IN-26
	Tubulin polymerization-IN-26 (compound 12h) is a chemical compound that inhibits the polymerization of microtubulin. It achieves this by binding to the colchicine binding site of microtubulin, with an IC50 value of 4.64 μM. Additionally, Tubulin polymerization-IN-26 has the ability to induce apoptosis and inhibit cell metastasis or migration. Due to these properties, it holds potential as a valuable compound for researching lung cancer [1].
T71217	MPT0B214
	MPT0B214 is a novel and potent microtubule inhibitor with potential anticancer activity. MPT0B214 inhibited tubulin polymerization through strongly binding to the tubulin's colchicine-binding site and had cytotoxic activity in a variety of human tumor cell lines. After treatment with MPT0B214, KB cells were arrested in the G2-M phase before cell death occurred, which were associated with upregulation of cyclin B1, dephosphorylation of Cdc2, phosphorylation of Cdc25C and elevated expression of th...
T78798	MY-673
	MY-673是CBSI（秋水仙碱结合位点抑制剂），可抑制微管蛋白聚合。该化合物还可阻断ERK信号通路，进而调节TGF-β/SMAD通路中的SMAD4蛋白表达。MY-673已经证实能在体内外有效抑制细胞的增殖和迁移，同时诱导apoptosis（细胞凋亡）。
T60568	Tubulin inhibitor 29
	Tubulin inhibitor 29 (compound 3c) 是一种有效的微管抑制剂，可抑制微管聚合并与秋水仙碱位点结合 (IC 50 = 1.2 μM)。Tubulin inhibitor 29 具有抗增殖作用，对人乳腺癌细胞 MCF-7 细胞的 IC50值为 7.5 μM。
T79887	Tubulin polymerization-IN-49
	Tubulin polymerization-IN-49 (compound 12d) 是一种抑制微管蛋白聚合的有效化合物。它通过结合到微管蛋白的秋水仙碱位点来抑制其聚合。此外，Tubulin polymerization-IN-49 能够诱导细胞周期在 G2/M 期停滞并触发细胞凋亡，表现出对抗癌的活性，能够预防肿瘤的生成及抑制肿瘤增殖和血管生成。
T70906	EHT-6706
	EHT-6706 is a novel microtubule-disrupting agent that targets the colchicine-binding site to inhibit tubulin polymerization. At low nM concentrations, EHT 6706 exhibits highly potent antiproliferative activity on more than 60 human tumor cell lines, even those described as being drug resistant. EHT 6706 also shows strong efficacy as a vascular-disrupting agent, since it prevents endothelial cell tube formation and disrupts pre-established vessels, changes the permeability of endothelial cell mon...
T68401	IG-105
	IG-105 is a potent microtubule inhibitor with potential anticancer activity. IG-105 inhibits microtubule assembly by binding at colchicine pocket. IG-105 shows a potent anticancer activity in vitro and in vivo and has good safety in mice. IG-105 showed a potent activity against human leukemia and solid tumors in breast, liver, prostate, lung, skin, colon, and pancreas with IC(50) values between 0.012 and 0.298 mumol/L. It was also active in drug-resistant tumor cells and not a P-glycoprotein sub...
T71116	MPT0B098
	MPT0B098 is a potent microtubule inhibitor through binding to the colchicine-binding site of tubulin. MPT0B098 is active against the growth of various human cancer cells, including chemoresistant cells with IC50 values ranging from 70 to 150 nmol/L. MPT0B098 arrests cells in the G2Â–M phase and subsequently induces cell apoptosis. In addition, MPT0B098 effectively suppresses VEGF-induced cell migration and capillary-like tube formation of HUVECs. Distinguished from other microtubule inhibitors, ...
T68249	IRC-083927 HCl
	IRC-083927 HCl is novel and potent microtubule inhibitor with potential anticancer activity. IRC-083927 inhibits the tubulin polymerization by a binding to the colchicine site. IRC-083927 inhibits in vitro cell growth of human cancer cell lines in the low nanomolar range. More interesting, it remains highly active against cell lines resistant to microtubule-interacting agents (taxanes, Vinca alkaloids, or epothilones). Chronic oral treatment with IRC-083927 (5 mg/kg) inhibits the growth of two h...
T83892	33-BCRP Inhibitor 33-Breast Cancer Resistance Protein Inhibitor
	33-BCRP抑制剂是一种乳腺癌耐药蛋白(BCRP)的抑制剂。它使得对米托蒽醌耐药的H460/MX20肺癌细胞对米托蒽醌诱导的细胞死亡更加敏感，无论是单独使用还是与UV辐射联合使用。33-BCRP抑制剂还能够增强表达P-糖蛋白(P-gp，亦称为多药耐药蛋白MDR)的KB-C2表皮癌细胞对秋水仙碱诱导的细胞死亡的敏感性。当使用5 µM浓度时，它能增加米托蒽醌在H460/MX20细胞中的细胞内积累。

化合物

Colchicine, deacetamido-5,6-didehydro-

Cat.No: T30999

Synonym: Deacetamido-6-dehydrocolchicine,Colchicine,deacetamido-6-dehydro- (7CI)

Colchicine, N-deacetyl-10-thio-

Cat.No: T31000

Synonym: N-Deacetylthiocolchicine,Desacetyl thiocolchicine,Deacetylthiocolchicine

Cat.No: T41248

Target: Microtubule Associated

Cat.No: T15012

Synonym: EPC2407

Target: Microtubule Associated

Tubulin inhibitor 24

Cat.No: T9812

Target: Microtubule Associated

gamma-Lumicolchicine

Cat.No: T31906

4-Formylcolchicine

Cat.No: T72544

Cat.No: T32946

Deacetylisocolchicine

Cat.No: T31244

Deacetylthiocolchicine hydrochloride

Cat.No: T31255

Synonym: Deacetylthiocolchicine chlorhydrate,Deacetylthiocolchicine HCl

Tubulin polymerization-IN-43

Cat.No: T77647

Target: Apoptosis, Microtubule Associated

Cat.No: T60009

Target: P-gp

Tubulin inhibitor 11

Cat.No: T67935

Target: Apoptosis, Microtubule Associated

Cat.No: T9595

Target: Microtubule Associated

Cat.No: T2511

Synonym: 普那布林,NPI-2358

Target: Microtubule Associated

Cat.No: T28886

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

Target: Microtubule Associated

Tubulin polymerization-IN-37

Cat.No: T61084

Mivobulin Isethionate

Cat.No: T28048

Synonym: NSC-613863,CI-980,NSC-635370,NSC-613862,NSC-350386

Cat.No: T68873

Cat.No: T25290

Synonym: DAT-1,DAT 1

Cat.No: T71974

Tubulin polymerization-IN-36

Cat.No: T60758

Cat.No: T21317

Synonym: BAL27862,BAL-27862,BAL 27862

Cat.No: T61728

Cat.No: T69557

Combretastatin A-1 phosphate tetrasodium

Cat.No: T40367

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

Tubulin polymerization-IN-39

Cat.No: T72167

Tubulin polymerization-IN-56

Cat.No: T80922

Tubulin polymerization-IN-45

Cat.No: T79341

Tubulin polymerization-IN-26

Cat.No: T61880

Cat.No: T71217

Cat.No: T78798

Tubulin inhibitor 29

Cat.No: T60568

Tubulin polymerization-IN-49

Cat.No: T79887

Cat.No: T70906

Cat.No: T68401

Cat.No: T71116

Cat.No: T68249

33-BCRP Inhibitor

Cat.No: T83892

Synonym: 33-Breast Cancer Resistance Protein Inhibitor

Cat. No.	Product Name	Target	Signaling Pathways
T0320	Colchicine 秋水仙碱,秋水仙素,Colcin,Colchineos,Colchisol	Apoptosis; Microtubule Associated; Autophagy	Apoptosis; Autophagy; Cytoskeletal Signaling
	Colchicine (Colcin) 属于天然产物，是一种微管聚合的抑制剂 (IC50=3 nM)，通过与微管蛋白结合来阻断微管的聚合。Colchicine 可以被用于治疗通风和风湿病。
TN6706	3-demethylcolchicine 3-去甲秋水仙碱,3-去甲基秋水仙碱	Reactive Oxygen Species	Immunology/Inflammation; Metabolism; NF-κB
	3-Demethylcolchicine 是一种从金莲花中分离得到的天然产物，对纯化的牛脑微管蛋白的聚合有抑制作用。
TN7063	N-Acetaminophen NSC 403155,N-Acetyldemecolcine,N-Methylcolchicine,N-甲基-秋水仙碱,N-Acetylcolchamine	Others	Others
	N-Acetaminophen (N-Methylcolchicine) 是秋水仙碱的甲基化形式。
T65128	Tartaric acid disodium dihydrate Disodium L-(＋)-Tartrate Dihydrate	Phosphatase; Endogenous Metabolite	Metabolism
	Tartaric acid disodium dihydrate (Disodium L-(＋)-Tartrate Dihydrate) 常用来制作分子生物学和细胞培养中的缓冲液,。Tartaric acid disodium dihydrate 是酸性磷酸酶抑制剂, 可增加秋水仙碱结合 tubulin1的概率。
T36961	Malformin C
	Malformin C is a natural fungus-derived bicyclic pentapeptide that has antibacterial properties, particularly against species of Bacillus. Malformin C potently blocks the ability of bleomycin to induce G2 arrest in human T-cell leukemia-derived Jurkat cells (IC50 = 0.9 nM). It less potently abrogates colchicine-induced M phase arrest in Jurkat cells (IC50 = 24 nM). Malformin C inhibits cell growth dose-dependently in Colon 38 and HCT 115 cancer cells (IC50s = 0.27 and 0.18 μM, respectively) but ...
TN5153	Torilin	MMP; ERK; IκB/IKK; p38 MAPK; NF-κB; Tyrosinase; Reductase; DNA/RNA Synthesis; JNK	Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Endocrinology/Hormones; MAPK; Metabolism; NF-κB; Proteases/Proteasome
	Torilin 是一种睾酮5α还原酶抑制剂，它（IC50=31.7+/-4.23μM）对5α还原酶的抑制作用强于α-亚麻酸（IC50=160.3+/-24.62μM），但弱于非那雄胺（IC50=0.38+/-0.06μM）。Torilin 具有免疫调节、肝脏保护和抗炎特性，它通过限制 TAK1介导的 MAP 激酶和 NF-βB 活化来抑制炎症，它可以减轻关节炎的严重程度，改变 dLN 或关节中的白细胞活化，并恢复血清和脾细胞细胞因子失衡。托利林抑制α-黑素细胞刺激激素激活的 B16黑色素瘤细胞中的黑色素生成，IC（50）值为25μM。Torilin 对枯草芽孢杆菌 ATCC 6633孢子和营养细胞表现出优异的抗菌活性。Torilin 在体内和体外都具有强大的抗血管生成活性，它可能通过抑制肿瘤侵袭来抑制肿瘤发生，逆转癌细胞的多药耐药性，它可以增强阿霉素、长春碱、紫杉醇和秋水仙碱对多药耐药 KB-V1和 MCF7/ADR 细胞的细胞毒性。

天然产物

Cat.No: T0320

Synonym: 秋水仙碱,秋水仙素,Colcin,Colchineos,Colchisol

Target: Apoptosis, Microtubule Associated, Autophagy

3-demethylcolchicine

Cat.No: TN6706

Synonym: 3-去甲秋水仙碱,3-去甲基秋水仙碱

Target: Reactive Oxygen Species

N-Acetaminophen

Cat.No: TN7063

Synonym: NSC 403155,N-Acetyldemecolcine,N-Methylcolchicine,N-甲基-秋水仙碱,N-Acetylcolchamine

Target: Others

Tartaric acid disodium dihydrate

Cat.No: T65128

Synonym: Disodium L-(＋)-Tartrate Dihydrate

Target: Phosphatase, Endogenous Metabolite

Cat.No: T36961

Cat.No: TN5153

Target: MMP, ERK, IκB/IKK, p38 MAPK, NF-κB, Tyrosinase, Reductase, DNA/RNA Synthesis, JNK

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