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].
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].
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].
KIF18A-IN-1 is a mitotic kinesin KIF18A inhibitor extracted from patent WO2021026098A1 example 100-13. KIF18A-IN-1 exhibits anti-tumor activity[1].
K858 Racemic is an ATP-uncompetitive inhibitor of Eg5 with an IC50 of 1.3 μM.
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].
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.
E7820 is an angiogenesis inhibitor by suppressing integrin a2, a cell adhesion molecule expressed on endothelial cells.
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].
αvβ5 integrin-IN-1 is a first potent and selective αvβ5 integrin inhibitor (pIC50 = 8.2) .
S516 (Compound 22) is an active metabolite of CKD-516 and a potent tubulin polymerization inhibitor with an IC50 of 4.29 μM. S516 has marked antitumor activity[1].
BTT-3033 is an orally active conformation-selective inhibitor of α2β1 (EC50: 130 nM) by binding to the α2I domain. BTT-3033 inhibits platelet binding to collagen Ⅰ and cell proliferation, and induces cell apoptosis. BTT-3033 can be used in the research of prostate cancer, inflammation and cardiovascular disease[1][2][4].
Dihydrocytochalasin B is a Cytokinesis inhibitor and changes the morphology of the cells, similar to that of cytochalasin B; does not inhibit glucose transport[1]. Dihydrocytochalasin B (H2CB) disrupts the actin structure and inhibits the ability of growth factors to stimulate DNA synthesis, reversibly blocks initiation of DNA synthesis, causes cell rounding and a loss of actin microfilament bundles[2]. Dihydrocytochalasin B is related to transcytoplasmic movement of calcium by inhibiting active calcium transport and causes a Ca+increase in the mucosal scrapings[3].
Alicaforsen is a 20-base antisense oligonucleotide inhibiting ICAM-1 production, which is an important adhesion molecule involved in leukocyte migration and trafficking to the site of inflammation.
FRAX1036 is a PAK inhibitor with Kis of 23.3 nM, 72.4 nM, and 2.4 μM for PAK1, PAK2 and PAK4, respectively.
Certepetide (CEND-1) is a bifunctional cyclic peptide (a.k.a. iRGD). Certepetide is a tumor-penetrating enhancer via RGD motif interaction with alphav-integrins and via activating NRP-1, and transforms the solid tumor microenvironment into a temporary drug conduit. Certepetide accumulates in tumors, and is used in the research of pancreatic cancer and other solid tumors[1][2][3].
CWHM-12 is a potent inhibitor of αV integrins with IC50s of 0.2, 0.8, 1.5, and 1.8 nM for αvβ8, αvβ3, αvβ6, and αvβ1.
Cys-Arg-Gly-Asp-Phe-Pro-Ala-Ser-Ser-Cys (Disulfide bridge:cys1-cys10), a decapeptide containing a cyclic RGD active sequence, is an Integrin αIIbβ3 antagonist that inhibits platelet and Adhesion of proMMP-13[1].
Sudocetaxel is a microtubule depolymerization inhibitor for pH-sensitive docetaxel delivery.
Microtubule inhibitor 5 (compound 17f) is a potent microtubule inhibitor. Microtubule inhibitor 5 shows cytotoxicity with an IC50 value of 154.5 nM for NCI-H460 cells. Microtubule inhibitor 5 shows good cell permeability[1].
Mps-BAY2a is a monopolar spindle 1 (MPS1) inhibitor with an IC50 of 1 nM against human MPS1. Mps-BAY2a induces mitotic aberrations and apoptosis in cancer cells[1].
Dynole 2−24 is an indole-based dynamin GTPase inhibitor (IC50=0.56 μM for dynamin I). Dynole 2−24 is nontoxic and shows increased potency against dynamin I and II in vitro and in cells (IC₅₀(CME)=1.9 μM). Dynole 2−24 also shows 4.4-fold selectivity for dynamin I. Dynole 2−24 is active in-cell inhibitor of clathrin-mediated endocytosis[1]. CME: Clathrin mediated endocytosis
Mdivi-1 is a selective dynamin-related protein 1 (Drp1) inhibitor.
MPI-0479605 is a potent and selective ATP-competitive inhibitor of Mps1, with an IC50 of 1.8 nM.
Vinblastine sulfate is a cytotoxic alkaloid used against various cancer types. Vinblastine sulfate inhibits the formation of microtubule and suppresses nAChR with an IC50 of 8.9 μM.