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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
4 Results for "
colchicine-binding pocket
" in MedChemExpress (MCE) Product Catalog:
Products (4)
4 Results for "colchicine-binding pocket" in MCE Product Catalog:
Cat. No.: HY-176537
CAS No.: 3055038-20-2
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RGN6024 is a brain-penetrant, orally active and reversible small molecule tubulin destabilizer. RGN6024 inhibits microtubule polymerization both in biochemical and cellular assays, binds to the colchicine binding pocket of β-tubulin (SPR: Kd = 6.7 μM; tryptophan assay: Kd = 7.4 μM), and triggers G2/M arrest in glioblastoma (GB) cells. RGN6024 retains activity in βIII-tubulin overexpressing cells. RGN6024 inhibits tumor growth in a GB xenograft mouse model. RGN6024 can be used for the study of glioblastoma (GB) .
Cat. No.: HY-182245
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Anticancer agent 314 is a multi-target anticancer agent with tubulin polymerization inhibitory activity (IC50 = 6.35 μM) and human carbonic anhydrase IX (Ki = 27.1 nM) and XII (Ki 20.9 = nM) inhibitory activity. Anticancer agent 314 binds to the colchicine-binding pocket of tubulin and inhibits tumor-associated carbonic anhydrase isoforms via zinc coordination within enzyme active sites. Anticancer agent 314 induces G2/M phase cell cycle arrest, apoptosis via p53-dependent signaling, and broad-spectrum antiproliferative activity across multiple cancer cells. Anticancer agent 314 can be used for the research of cancer, such as leukemia, melanoma, ovarian cancer .
Cat. No.: HY-179372
CAS No.: 2982893-14-9
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Tubulin polymerization-IN-84 inhibits tubulin polymerization by targeting the colchicine-binding pocket, with anIC50 = 10.9 μM. Tubulin polymerization-IN-84 shows antiproliferative activity against Jurkat, B16-F10, HCT116, and MDA-MB-231 cells (IC50 = 60 nM, 380 nM, 138 nM, and 1.054 μM). Tubulin polymerization-IN-84 induces G2/M-phase arrest and apoptosis in B16-F10 cells. Tubulin polymerization-IN-84 suppresses tumor growth in a B16-F10 melanoma model and potentiates anti-tumor immunity in combination with a PD-L1 mAb for the research of T-cell acute lymphoblastic leukemia, melanoma, colon cancer, and breast cancer.
Cat. No.: HY-111175
CAS No.: 905978-63-4
Research Areas:
IG-105 is a potent tubulin inhibitor, with an IC50 of 0.6 μM for competitive inhibition of [ 3H] colchicine binding to tubulin, and an IC50 of 3 μM for inhibition of tubulin polymerization. IG-105 inhibits microtubule polymerization by binding to the colchicine pocket of tubulin, induces cell cycle arrest at the G2-M phase, and subsequently activates the caspase cascade through Bcl-2 inactivation and p53 upregulation to induce apoptosis. As a non-Pgp substrate, IG-105 effectively overcomes multidrug resistance. IG-105 can be used in the research of leukemia, breast cancer, liver cancer, prostate cancer, lung cancer, melanoma, pancreatic cancer and colon cancer .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
