Novel irreversible transglutaminase 2 (TG2) inhibitor
Cemadotin (LU103793) is an analogue of Dolastatin 15 (HY-P1126) which is naturally occurring cytotoxic peptides. Cemadotin blocks cells at mitosis, and exhibits Ki value of 1 μM for inhibiting tubulin. Cemadotin can be used to research anticancer[1].
Thiocolchicine-d3 is deuterium labeled Thiocolchicine. Thiocolchicine, a derivative modified in the C Ring of Colchicine (HY-16569) with enhanced biological properties. Thiocolchicine is a potent inhibitor of tubulin polymerization (IC50=2.5 µM) and competitively binds to tubulin with a Ki of 0.7 µM. Thiocolchicine induces cell apoptosis[1][2]. Thiocolchicine can be used as an ADC cytotoxin in ADC technology.
Crolibulin is a small molecule tubulin polymerization inhibitor.
Myoseverina, a microtubule-binding molecule, induces the reversible fission of multinucleated myotubes into mononucleated fragments. Myoseverina affects the expression of a variety of growth factor, immunomodulatory, extracellular matrix-remodeling, and stress response genes, consistent with the activation of pathways involved in wound healing and tissue regeneration[1].
Podophyllotoxone is isolated from the roots of Dysosma versipellis and has anti-cancer activities.Podophyllotoxone is able to inhibit the tubulin polymerization[1].
TAM470 is a novel cytolysin, inhibiting tubulin polymerization and microtubule depolymerization. TAM470 can be used in the synthesis of OMTX705 as payload molecule, OMTX705 is a novel FAP-targeting antibody-drug conjugates (ADCs) with antitumor activity[1].
Tubulin polymerization-IN-11 is a potent tubulin polymerization inhibitor with an IC50 value of 3.4 µM. Tubulin polymerization-IN-11 shows antiproliferative activity. Tubulin polymerization-IN-11 induces Apoptosis and cell cycle arrest at G2/M phase. Tubulin polymerization-IN-11 decreases the expression of cyclin B1, p-cdc2, and Bcl-2 protein levels and increases the expression of cleaved PARP[1].
Tubulin polymerization-IN-13 (Compound 4f) is a tubulin polymerization inhibitor (IC50=0.37 μM). Tubulin polymerization-IN-13 shows anti-proliferative activity against cancer cells, induces apoptosis and potential antivascular activity[1].
Microtubule inhibitor 1 is an antitumor agent with microtubule polymerization inhibitory activity, with an IC50 value of 9-16 nM in cancer cells[1].
10-Oxo Docetaxel (Docetaxel Impurity) is a novel taxoid having remarkable anti-tumor properties and a Docetaxel intermediate.
Cabazitaxel-d9 is deuterium labeled Cabazitaxel. Cabazitaxel is a semi-synthetic derivative of the natural taxoid 10-deacetylbaccatin III with potential antineoplastic activity.
AChE/GSK-3β-IN-1 (compound GT15) is a potent, dual AChE/GSK-3β inhibitor with IC50 values of 1.2, 149.8 and 22.4 nM for hAChE , hBChE and hGSK-3β, respectively. AChE/GSK-3β-IN-1 penetrates the blood-brain barrier (BBB). AChE/GSK-3β-IN-1 has high kinase selectivity profiles for the CMGC kinase family. AChE/GSK-3β-IN-1 occupies the ATP binding site of DYRK1A. AChE/GSK-3β-IN-1 inhibits ROS expression and reduces oxidative stress. AChE/GSK-3β-IN-1 can be used for Alzheimer’s disease research[1].
Tubulin polymerization-IN-43 (compound 15h) is a tubulin polymerization inhibitor. Tubulin polymerization-IN-43 disrupts cellular microtubule networks by targeting the Colchicine (HY-16569) site, and promots cell cycle arrest of leukemia cells at G2/M phase and cell apoptosis, as well as inhibiting angiogenesis[1].
ENMD-119 is a 2-methoxyestradiol analogue with antiproliferative and antiangiogenic activity, and is suitable for inhibiting HIF-1α and STAT3 in human HCC cells.
D8-MMAE is a deuterated labeled MMAE, a potent mitotic inhibitor.
Tubulin polymerization-IN-22 is a tubulin polymerization inhibitor with an IC50 of 8.1 μM. Tubulin polymerization-IN-22 arrests cell cycle at G2/M phase and induces apoptosis[1].
Mc-MMAF is a protective group-conjugated MMAF. MMAF is a more potent drug than Monomethyl auristatin E (MMAE), but is charged and relatively membrane-impermeable, is a potent tubulin inhibitor, is a toxin payload in antibody drug conjugate.Target:MMAF is a new auristatin derivative with a charged C-terminal phenylalanine that attenuates its cytotoxic activity compared to its uncharged counterpart, Monomethyl auristatin E (MMAE). Because of MMAF is highly toxic, it cannot be used as a drug itself. MMAF induces potent antitumor effects when conjugated via protease cleavable linkers to a monoclonal antibody targeting internalizing, tumor-specific cell surface antigens. The linker to the monoclonal antibody is stable in extracellular fluid, but is cleaved by cathepsin once the conjugate has entered a tumor cell, thus activating the anti-mitotic mechanism.
Tubulin polymerization-IN-25 (compound 17f) is a dual inhibitor of tubulin polymerization and farnesyl transferase (FTase) with IC50s of 1.11 μM and 0.39 μM, respectively. Tubulin polymerization-IN-25 displays cytotoxicity and excellent antitumor activity [1].
Tubulin inhibitor 33, a tubulin polymerization inhibitor, inhibits tubulin polymerization in a dose-dependent manner with an IC50 of 9.05 μM. Tubulin inhibitor 33 has antitumor effects and induces cell apoptosis that can be used for antitumor research[1].
Mivobulin (NSC 613862) is a tubulin inhibitor, binds to tubulin in the region that overlaps the colchicine site, and inhibits tubulin polymerization. Mivobulin (NSC 613862) promotes the formation of abnormal polymers and a GTPase activity in the tubulin dimer. Anti-cancer activity[1].
Taxinine B is a taxoid that can be isolated from Japanese Yew Taxus Cuspid. Taxinine B inhibits CaCl2-induced depolymerization of microtubule. Taxinine B is useful for overcoming multidrug resistance in tumor cells[1].
Vincristine-d3-ester (Leurocristine-d3-ester) sulfate is the deuterium labeled Vincristine sulfate. Vincristine sulfate is an antitumor vinca alkaloid which inhibits microtubule formation in mitotic spindle, resulting in an arrest of dividing cells at the metaphase stage. It binds to microtubule with a Ki of 85 nM[1].
Tubulysin IM-2 is an ADC Cytotoxin and tubulin binder used as anti-microtubule toxins.
Violanone, an isoflavanone compound, can inhibit tubulin polymerization. Violanone also exhibits larvicidal activity against A. aegypti[1][2].
Anticancer agent 98 (compound 12k) is a microtubule/tubulin-polymerization inhibitor (Kd=16.9 μM). Anticancer agent 98 exerts antiproliferative potency against tumor cells, exhibits anti-angiogenesis effect in vitro. Anticancer agent 98 exhibits good human and mouse liver microsomes stability with both t1/2>300 min[1].
Tubulin polymerization-IN-42 (compound 10j), an indole-substituted furanone, is an inhibitor of tubulin polymerization with anti-cancer activity[1].
Cantuzumab ravtansine (IMGN242; huC242-DM4), an ADC, is a humanized monoclonal antibody, huC242, covalently linked via a disulfide bond to DM4 (DM4 (HY-12454)). Cantuzumab ravtansine has broad antitumor efficacy against a range of CanAg-positive human tumor xenografts[1][2].