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Search Results for " colchicine-binding "

21

抑制剂 & 化合物

2

天然产物

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Cat. No. Product Name Target Signaling Pathways
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。
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。
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。
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].
T25290 DAT1

DAT-1,DAT 1

DAT1 is an antimitotic and antiangiogenic that acts by binding to the colchicine binding site of tubulin.
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.
T71974 ABI-274

ABI-274 is a novel potent colchicine binding site inhibitor (CBSI) and tubulin inhibitor.
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.
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。
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.
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.
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].
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。
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)。
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)。
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...
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 G2–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, ...
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...
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...

化合物

Crolibulin
Cat.No: T15012
Synonym: EPC2407
Target: Microtubule Associated
Tubulin inhibitor 11
Cat.No: T67935
Synonym:
Target: Apoptosis, Microtubule Associated
Plinabulin
Cat.No: T2511
Synonym: 普那布林,NPI-2358
Target: Microtubule Associated
Tubulin polymerization-IN-37
Cat.No: T61084
Synonym:
Target:
DAT1
Cat.No: T25290
Synonym: DAT-1,DAT 1
Target:
Mivobulin Isethionate
Cat.No: T28048
Synonym: NSC-613863,CI-980,NSC-635370,NSC-613862,NSC-350386
Target:
ABI-274
Cat.No: T71974
Synonym:
Target:
Cornigerine
Cat.No: T68873
Synonym:
Target:
Tubulin polymerization-IN-36
Cat.No: T60758
Synonym:
Target:
Combretastatin A-1 phosphate tetrasodium
Cat.No: T40367
Synonym: Combretastatin A-1 phosphate tetrasodium,OXi-4503 tetrasodium
Target:
MY-875
Cat.No: T61728
Synonym:
Target:
ABI-231 HCl
Cat.No: T69557
Synonym:
Target:
Tubulin polymerization-IN-26
Cat.No: T61880
Synonym:
Target:
Tubulin polymerization-IN-39
Cat.No: T72167
Synonym:
Target:
Tubulin polymerization-IN-45
Cat.No: T79341
Synonym:
Target:
MPT0B214
Cat.No: T71217
Synonym:
Target:
MY-673
Cat.No: T78798
Synonym:
Target:
EHT-6706
Cat.No: T70906
Synonym:
Target:
MPT0B098
Cat.No: T71116
Synonym:
Target:
IG-105
Cat.No: T68401
Synonym:
Target:
IRC-083927 HCl
Cat.No: T68249
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
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。
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。

天然产物

Tartaric acid disodium dihydrate
Cat.No: T65128
Synonym: Disodium L-(+)-Tartrate Dihydrate
Target: Phosphatase, Endogenous Metabolite
Colchicine
Cat.No: T0320
Synonym: 秋水仙碱,秋水仙素,Colcin,Colchineos,Colchisol
Target: Apoptosis, Microtubule Associated, Autophagy
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