Catalog No.
Product Name
Application
Product Information
Citations
-
cardiac myosin modulator
Mavacamten is a modulator of cardiac myosin, with IC50s of 490, 711 nM for bovine cardiac and human cardiac, respectively. -
Microtubule polymerization inhibitor
Cucurbitacin B, a natural triterpenoid is well-known for its strong anticancer activity, and recent studies showed that the compound inhibits JAK/STAT3 pathway. Also it is an potent Microtubule polymerization inhibitor -
Dynamin inhibitor
Dynamin Inhibitory Peptide is a peptide inhibitor of the GTPase dynamin. -
Panx-1 mimetic inhibitor
Scrambled 10Panx, Panx-1 mimetic inhibitory peptide, is a blocker of pannexin-1 gap junctions. - 7-Epi 10-Desacetyl Paclitaxel is a derivative of Paclitaxel, which is a microtubule polymer stabilizer with IC50 of 0.1 pM in human endothelial cells.
- 7-xylosyltaxol is a taxol derivative, Paclitaxel binds to tubulin and inhibits the disassembly of microtubules.
-
KSP inhibitor
ARRY-520 R enantiomer is the R form of ARRY-520, which is a synthetic, small molecule kinesin spindle protein (KSP) inhibitor with IC50 of 6 nM. -
Gap-junction modifier
GAP-134 Hydrochloride, a small modified dipeptide, has been identified as a potent and selective second generation gap junction modifier with oral bioavailability. -
PAK4/NAMPT Inhibitor
KPT 9274 ( ATG-019) is an orally bioavailable small molecule that is a non-competitive dual inhibitor of PAK4 and NAMPT. It shows an IC50 of ~120 nM for NAMPT in a cell-free enzymatic assay. -
EDA-integrin Interactions Inhibitor
Irigenin is an inhibitor of EDA-integrin interactions, specifically targeting α9β1 and α4β1 integrins by blocking their binding sites on the C-C loop of Extra Domain A (EDA). This compound exhibits significant anti-cancer properties, particularly in gastric cancer cells, where it enhances TRAIL-induced apoptosis by increasing the expression of pro-apoptotic molecules. Irigenin may be valuable in cancer research, particularly in studies focused on metastasis and apoptosis modulation. -
PAK4 Inhibitor
LCH-7749944 is a potent inhibitor of PAK4, demonstrating an IC50 of 14.93 μM. It effectively inhibits the proliferation of human gastric cancer cells by downregulating the PAK4/c-Src/EGFR/cyclin D1 signaling pathway and induces apoptosis in these cells. This reagent is valuable for research focused on cancer biology and therapeutic strategies targeting PAK4-related pathways. -
PAK4 Inhibitor
PAK4-IN-2 is a potent inhibitor of the p21-activated kinase 4 (PAK4), exhibiting an IC50 value of 2.7 nM. This compound effectively induces cell cycle arrest at the G0/G1 phase and promotes apoptosis in MV4-11 cancer cells. PAK4-IN-2 is suitable for investigations into cancer biology and therapeutic development targeting PAK4 signaling pathways. -
pan-SIK/PAK2/3 Inhibitor
MRIA9 is an ATP-competitive inhibitor targeting pan Salt-Inducible kinases (SIK) as well as PAK2 and PAK3. It exhibits potent biological activity with IC50 values of 516 nM for SIK1, 180 nM for SIK2, and 127 nM for SIK3. MRIA9 is suitable for applications in signaling pathway research and the study of various cellular processes influenced by SIK and PAK kinases. -
Microtubule/Tubulin Inhibitor
Tubulysin B is a potent microtubule destabilizing agent that selectively inhibits tubulin polymerization. Naturally derived from the myxobacteria Archangium geophyra and Angiococcus disciformis, it exhibits high cytotoxicity with IC50 values in the picomolar range across various cancer cell lines, including those exhibiting multidrug resistance. This compound is valuable for studies focused on cancer biology, specifically in elucidating mechanisms of cell cycle arrest and apoptosis. -
Src/Tubulin Inhibitor
KX2-361 is an inhibitor of Src-kinase and tubulin polymerization. This compound exhibits significant anti-tumor activity and induces apoptosis in glioblastoma (GBM) cells. With good oral bioavailability and the ability to cross the blood-brain barrier in murine models, KX2-361 is a valuable tool for investigating Src-related signaling pathways and therapeutic strategies in cancer research. -
Tubulin/JAK2-IN-1 inhibitor, Antitumor
Tubulin/JAK2-IN-1 is a dual inhibitor targeting Janus kinase 2 (JAK2) and microtubules, exhibiting potent antitumor activity. This compound demonstrates significant antiproliferative effects against various cancer cell lines, making it a valuable tool in cancer research. Its dual mechanism of action supports investigations into therapies that disrupt cell division and signaling pathways in malignancies. -
Microtubule-Binding Molecule
Myoseverin is a microtubule-binding molecule that acts as an angiogenesis inhibitor. This compound induces the reversible fission of multinucleated myotubes into mononucleated fragments, thereby affecting muscle cell dynamics. Additionally, Myoseverin demonstrates anti-angiogenic properties by inhibiting both endothelial cell function and the differentiation of endothelial progenitor cells. Its unique mechanism makes it a valuable tool for research in muscle biology and vascular development. -
Integrin αvβ6 Inhibitor
MORF-627 is a selective integrin αvβ6 inhibitor that effectively impairs TGF-β1 activation and pSMAD2 signaling. This compound significantly decreases collagen deposition and markers of epithelial-mesenchymal transition in fibrotic cells, demonstrating notable antifibrotic activity in idiopathic pulmonary fibrosis models without causing genotoxicity. While MORF-627 induces bladder epithelial proliferation and early invasive urothelial carcinoma in cynomolgus monkeys and human cells, these toxic effects can be mitigated by exogenous TGF-β. This reagent is valuable for investigating the pathological mechanisms underlying pulmonary fibrosis and assessing associated drug safety. -
Tubulin Inhibitor
Antiproliferative agent-30 is a tubulin inhibitor that disrupts tubulin assembly and effectively inhibits FLT3 and Abl1 activity. This compound demonstrates impressive antiproliferative effects against various cancer cell lines, exhibiting IC50 values of 0.054 nM, 0.008 nM, and 0.144 nM for HCT-116, K562, and MV-4-11 cells, respectively. Additionally, Antiproliferative agent-30 shows potential in targeting acute myeloid leukemia (AML) cells with FLT3-ITD-TKD mutations, highlighting its significance in cancer research and potential therapeutic applications. -
Microtubule Inhibitor
MPT0B002 is a potent microtubule inhibitor that targets tubulin polymerization, leading to significant anticancer effects. This compound induces apoptosis and effectively arrests the cell cycle at the G2/M phase. MPT0B002 is useful in various cancer research applications, providing insights into microtubule dynamics and the mechanisms of tumor cell proliferation. -
Tubulin/VEGFR Inhibitor
Tubulin/VEGFR-2-IN-2 is an orally active inhibitor targeting tubulin and VEGFR-2, exhibiting IC50 values of 3.27 μM and 0.09 μM, respectively. This compound demonstrates significant antitumor activity by enhancing reactive oxygen species generation, disrupting mitochondrial membrane potential, inducing apoptosis, and arresting the cell cycle. Additionally, Tubulin/VEGFR-2-IN-2 possesses anti-angiogenic effects, impairing endothelial cell migration, invasion, and tube formation in vitro. It effectively suppresses angiogenesis, tumor growth, and metastasis in vivo, making it a valuable tool for research involving non-small cell lung cancer, breast cancer, gastric cancer, and lymphoma. -
Tubulin polymerization Inhibitor
Tubulin polymerization-IN-11 is a potent inhibitor of tubulin polymerization with an IC50 value of 3.4 μM. It demonstrates significant antiproliferative activity by inducing apoptosis and causing cell cycle arrest at the G2/M phase. Mechanistically, Tubulin polymerization-IN-11 reduces the expression levels of cyclin B1, phosphorylated cdc2, and Bcl-2 while increasing the expression of cleaved PARP, making it valuable for research in cancer biology and cell cycle regulation. -
Tubulin Polymerization Inhibitor
Tubulin Inhibitor 17 is a potent tubulin polymerization inhibitor, demonstrating an IC50 value of 12.38 µM. This compound exhibits significant anticancer activity by inducing apoptosis in tumor cells. It is suitable for research applications focused on cancer biology and the study of microtubule dynamics. -
Microtubule Inhibitor
4SC-207 is a potent microtubule inhibitor that induces cell cycle arrest and apoptosis by obstructing microtubule growth. This compound effectively inhibits tumor cell proliferation both in vitro and in vivo, demonstrating significant activity against taxane-resistant xenograft mouse models. 4SC-207 is suitable for cancer research applications, particularly in the study of colon adenocarcinoma and other malignancies. -
Tubulin/HDAC Inhibitor
Tubulin/HDAC-IN-1 is a dual inhibitor targeting tubulin and histone deacetylase 8 (HDAC8) through CH/π interaction and hydrogen bonding, respectively. This compound effectively inhibits tubulin polymerization and selectively inhibits HDAC8 with an IC50 value of 150 nM. Tubulin/HDAC-IN-1 demonstrates cytotoxic effects against a range of human cancer cell lines, induces cell cycle arrest in the G2/M phase, and promotes apoptosis. It is a valuable reagent for research involving hematologic malignancies and solid tumors, including neuroblastoma and leukemia. -
Tubulin Polymerization Inhibitor
Tubulin polymerization-IN-28 is a selective inhibitor of microtubule protein polymerization, primarily targeting tubulin. This compound demonstrates significant anticancer activity by activating NQO1, leading to the release of combretastatin A-4, which promotes apoptosis in tumor cells. Tubulin polymerization-IN-28 is valuable for research applications focused on cancer therapy and the mechanisms of cell death. -
Tubulin Polymerization Inhibitor
Tubulin polymerization-IN-60 is a tubulin polymerization inhibitor that targets the colchicine binding site on tubulin, effectively disrupting microtubule assembly. This compound induces cell cycle arrest at the G2/M phase, leading to increased apoptosis in cancer cells. It serves as a valuable tool in cancer research, enabling the study of microtubule dynamics and the development of novel therapeutic strategies against malignant tumors. -
Tubulin Inhibitor
Tubulin polymerization-IN-9 is a potent inhibitor of tubulin polymerization, exhibiting an IC50 value of 1.82 μM. This compound effectively induces cell cycle arrest at the G2/M phase and triggers apoptosis in K562 cells, accompanied by depolarization of mitochondria. Tubulin polymerization-IN-9 demonstrates significant anti-vascular and antitumor activities, making it a valuable tool in cancer research and therapeutic studies. -
Tubulin Inhibitor
Tubulin Inhibitor 23 is a potent inhibitor of tubulin with an IC50 value of 4.8 µM. This compound induces apoptosis in cancer cells and exhibits antiangiogenic activity in a dose-dependent manner. Tubulin Inhibitor 23 is relevant for research applications related to leukemia and other malignancies involving aberrant angiogenesis and cell proliferation. -
Tubulin Polymerization Inhibitor
Tubulin polymerization-IN-13 is an inhibitor of tubulin polymerization, exhibiting an IC50 of 0.37 μM. This compound demonstrates significant anti-proliferative activity against various cancer cell lines, inducing apoptosis and potentially exhibiting antivascular properties. It serves as a valuable tool for research focused on cancer therapeutics and the mechanisms of cell division. -
Tubulin Inhibitor
Tubulin Inhibitor 14 targets NQO2 (quinone oxidoreductase 2) and exhibits a potent inhibitory effect with an IC50 of 1.0 μM. It disrupts tubulin polymerization and impedes the formation of capillary-like structures in endothelial cells. This microtubule-destabilizing agent possesses potential tumor-selectivity and exhibits antiangiogenic and vascular-disruptive properties, making it valuable for research in cancer biology and angiogenesis. -
Tubulin polymerization Inhibitor
Tubulin polymerization-IN-4 is a potent inhibitor of tubulin polymerization, exhibiting an IC50 value of 4.6 μM. This compound effectively disrupts tubulin dynamics, leading to cell cycle arrest at the G2/M phase, induction of apoptosis, and inhibition of both clonogenesis and migration in HeLa cells. Tubulin polymerization-IN-4 serves as a valuable tool in research related to cervical cancer, facilitating the exploration of therapeutic strategies targeting tubulin dynamics. -
Tubulin Inhibitor
Disorazol A is a potent tubulin inhibitor that disrupts microtubule formation by hindering tubulin polymerization. This action effectively blocks mitosis, leading to cell cycle arrest at the G2/M phase and subsequent induction of apoptosis. Additionally, Disorazol A has demonstrated inhibitory effects on L929 mouse fibroblasts, with an IC50 value of 3 pM, and promotes the accumulation of p53 protein within the nucleus. This compound holds potential for research in cancer biology and therapeutic applications. -
Tubulin/NRP1 Inhibitor
Tubulin/NRP1-IN-1 is a dual inhibitor targeting tubulin and neuropilin-1 (NRP1), exhibiting IC50 values of 0.71 μM and 0.85 μM, respectively. This compound effectively decreases the viability of prostate tumor cell lines and promotes apoptotic processes. Its unique mechanism makes it a valuable tool for studying cancer biology and exploring potential therapeutic strategies. -
Tubulin Polymerization Inhibitor
Tubulin polymerization-IN-14 is a selective inhibitor of tubulin polymerization, exhibiting an IC50 of 3.15 μM. This compound demonstrates significant anti-vascular and anticancer activities by inducing apoptosis in cancer cells. It is particularly valuable in research focused on cancer biology and therapeutic drug development targeting microtubule dynamics. -
Microtubule/Tubulin Inhibitor
SSE1806 is a microtubule/tubulin inhibitor derived from podophyllotoxin, exhibiting notable anticancer and antiproliferative effects. It demonstrates a GI50 range of 1.29-21.15 μM against cancer cell growth, inducing mitotic abnormalities and G2/M phase cell cycle arrest. Additionally, SSE1806 enhances p53 expression and effectively inhibits the growth of colon cancer organoids, while also overcoming multidrug resistance in MDR-1 overexpressing cell lines, making it a valuable tool for cancer research. -
PAK1 Inhibitor
ZMF-10 is a potent PAK1 inhibitor, exhibiting an IC50 of 174 nM for PAK1 and varying potencies for related isoforms PAK2 and PAK3 at 1.038 µM and 1.372 µM, respectively. This compound effectively inhibits PAK1 activity, influencing PAK1-regulated processes such as apoptosis, ER stress response, and cellular migration in MDA-MB-231 breast cancer cells. ZMF-10 is suitable for investigations into mechanisms of anticancer therapy and related cellular pathways. -
Tubulin Polymerization Inhibitor
KY216 is a potent tubulin polymerization inhibitor that targets the colchicine-binding site of tubulin, with an IC50 value of 2.61 μM. This compound demonstrates significant biological activity in hindering tubulin polymerization, making it a valuable tool for research applications in non-small cell lung cancer (NSCLC) and breast cancer studies. KY216's mechanism of action positions it as a promising candidate for further investigation into therapeutic strategies against these malignancies. -
Tubulin Polymerization Inhibitor
5HPP-33 is a potent inhibitor of tubulin polymerization with an IC50 of 8.1 μM. It demonstrates significant anti-proliferative activity against leukemia and multiple myeloma cells, exhibiting IC50 values ranging from 1 to 10 μM. 5HPP-33 effectively induces cell cycle arrest at the G2/M phase and promotes apoptosis, making it a valuable tool for cancer research and therapeutic studies targeting microtubule dynamics. -
Microtubule Inhibitor
Kribb3 is a microtubule inhibitor that effectively disrupts microtubule dynamics. It demonstrates significant biological activity by inhibiting cancer cell proliferation with a GI50 range of 0.2-2.5 μM, promoting G2/M phase cell cycle arrest, and inducing apoptosis in HCT-116 cells. Additionally, Kribb3 has shown promising antitumor activity in murine models, making it a valuable tool for cancer research.
