Tubulin inhibitor 28 (compound 2g) is a potent tubulin inhibitor with an IC50 value of 1.2 µM. Tubulin inhibitor 28 shows anti-proliferative activity for MCF-7 cells[1].
Mertansine (DM1) is a microtubulin inhibitor which binds at the tips of microtubules and suppresses the dynamicity of microtubules.. Mertansine is an antibody-conjugatable maytansinoid that was developed to overcome systemic toxicity associated with maytansine and to enhance tumor-specific delivery.
Dynamin inhibitory peptide competitively blocks binding of dynamin to amphiphysin, thus preventing endocytosis. Dynamin inhibitory peptide blocks the dopamine D3 effect on GABAA receptors[1].
Tubulin polymerization-IN-57 (compound 5a) is a tubulin inhibitor and is an α-naphthoxy-substituted carbendazim (HY-13582) derivative. Tubulin polymerization-IN-57 induces mitotic arrest and inhibits cancer cell proliferation[1].
Latrunculin A (LAT-A) is a toxin isolated from the red sea sponge Latrunculia magnifica, binds to actin monomers, inhibits polymerization of actin, with Kds of 0.1, 0.4, 4.7 μM and 0.19 μM for ATP-actin, ADP-Pi-actin, ADP-actin and G-actin, respectively[1][2].
Kif15-IN-2 is an inhibitor of the mitotic kinesin Kif15, and is used for the research of cellular proliferative diseases.
Aminobenzenesulfonic auristatin E is a drug-linker conjugate for ADC with potent antitumor activity by using Auristatin E (a cytotoxic tubulin modifier), linked via the ADC linker Aminobenzenesulfonic[1].
Tubulin inhibitor 1 is a tubulin inhibitor, occupying the colchicine binding site, inhibits tubulin polymerization. Tubulin inhibitor 1 shows potent anti-tumor activity, casues cellular mitotic arrest in the G2/M phase, and induces cellular apoptosis[1].
Integrin-IN-2 (compound 39) is an orally bioavailable pan αv integrin inhibitor. Integrin-IN-2 can increases the αvβ6, αvβ3, αvβ5 and αvβ8 binding affinities with pIC50 values of 7.8, 8.4, 8.4 and 7.4, respectively[1].
187-1, N-WASP inhibitor, a 14-aa cyclic peptide, is an allosteric neural Wiskott-Aldrich syndrome protein (N-WASP) inhibitor. 187-1, N-WASP inhibitor potently inhibits actin assembly induced by phosphatidylinositol 4,5-bisphosphate (PIP2) with an IC50 of 2 μM. 187-1, N-WASP inhibitor prevents the activation of Arp2/3 complex by N-WASP by stabilizing the autoinhibited state of the protein[1][2].
5-Aminosalicylic acid-13C6 is the 13C labeled 5-Aminosalicylic Acid[1]. 5-Aminosalicylic acid (Mesalamine) acts as a specific PPARγ agonist and also inhibits p21-activated kinase 1 (PAK1) and NF-κB[2][3][4].
KIF18A-IN-1 is a mitotic kinesin KIF18A inhibitor extracted from patent WO2021026098A1 example 100-13. KIF18A-IN-1 exhibits anti-tumor activity[1].
Sirt1/2-IN-1 (Compound 7) is a SIRT1 and SIRT2 inhibitor with IC50 values of 1.81, 2.10 and 20.5 µg/mL against SIRT1, SIRT2 and SIRT3, respectively. Sirt1/2-IN-1 displays activity in hyperacetylation of α-tubulin protein with an IC50 of 32.05 µg/mL. Sirt1/2-IN-1 shows prominent anticancer activity[1].
Ixabepilone is an orally bioavailable microtubule inhibitor, which binds to tubulin and promotes tubulin polymerization and microtubule stabilization, thereby arrests cells in the G2-M phase of the cell cycle and induces tumor cell apoptosis.
K858 Racemic is an ATP-uncompetitive inhibitor of Eg5 with an IC50 of 1.3 μM.
Cyclo(RGDyK) is a potent and selective αVβ3 integrin inhibitor with an IC50 of 20 nM.
Entasobulin is a β-tubulin polymerization inhibitor with potential anticancer activity.
Cantuzumab mertansine (SB-408075; huC242-DM1), an ADC, is an immunoconjugate of the potent maytansine derivative (DM1; HY-19792) and the humanized monoclonal antibody (huC242) directed to CanAg. Cantuzumab mertansine has cytotoxic toward colon cancer cells and has broad antitumor efficacy against a range of CanAg-positive human tumor xenografts[1][2].
KX2-391 is an inhibitor of Src that targets the peptide substrate site of Src, with GI50 of 9-60 nM in cancer cell lines.
para-Nitroblebbistatin is a non-cytotoxic, photostable, fluorescent and specific Myosin II inhibitor, usd in the study of the specific role of myosin II in physiological, developmental, and cell biological studies[1].
Tubulin/HDAC-IN-1 is a dual tubulin and HDAC-IN-1 inhibitor through CH/π interaction with tubulin and hydrogen bond interaction with HDAC8. Tubulin/HDAC-IN-1 inhibits tubulin polymerization and selectively inhibits HDAC8 (IC50: 150 nM). Tubulin/HDAC-IN-1 has cytotoxicity against various human cancer cells, also arrests cell cycle in the G2/M phase and induces cell apoptosis. Tubulin/HDAC-IN-1 can be used in the research of hematologic and solid tumors such as neuroblastoma, leukemia[1].
PM050489 is an effective polyketone inhibitor of Microtubule/Tubulin that can be isolated from Madagascan sponge Lithoplocamia lithistoides. PM050489 inhibits mitosis with an IC50 value of 26.4 nM. PM050489 has antitumor activity and can be used in cancer research[1][2].
Cytochalasin B is a cell-permeable mycotoxin binding to the barbed end of actin filaments, disrupting the formation of actin polymers, with Kd value of 1.4-2.2 nM for F-actin.
Mps1-IN-1 is a potent, selective and ATP-competitive Mps1 kinase inhibitor, with an IC50 and a Kd of 367 nM and 27 nM.
Dimethylenastron is a potent Eg5 inhibitor, with an IC50 of 200 nM.
E7820 is an angiogenesis inhibitor by suppressing integrin a2, a cell adhesion molecule expressed on endothelial cells.
FRAX597 is a potent group I p21-activated Kinases (PAKs) inhibitor with IC50 of 8, 13 and 19 nM for PAK1, 2 and 3.
Antitumor agent-68 is a potent tubulin inhibitor. Antitumor agent-68 shows potent anticancer activity with IC50s of 3.6 and 3.8 µM for HeLa and MCF-7 cells, respectively. Antitumor agent-68 exhibits good scavenging activity of ROS and DPPH radical in a dose-dependent manner[1].
Kif15-IN-1 is an inhibitor of the mitotic kinesin Kif15, and is used for the research of cellular proliferative diseases.
LXW7 is an octamer disulfide cyclic peptide, also a αvβ3 integrin ligand, acts as a potent and specific endothelial progenitor cells (EPCs) and endothelial cells (ECs) targeting ligand. LXW7 increases phosphorylation of VEGFR-2 and activation of ERK1/2[1].