tubulin inhibitor-6

Tubulin inhibitor 6 (iHAP1) is an inhibitor of tubulin and a potent inhibitor of multiple cancer cell lines.

Tubulin polymerization-IN-75 (Compound 6) is an inhibitor of tubulin polymerization, with an IC50 value of 30 μM. It effectively suppresses the proliferation of cancer cells Huh7 and 293T, demonstrating IC50 values of 14.3 μM and 13.8 μM, respectively.

Taltobulinintermediate-6 serves as an intermediate in the synthesis of Taltobulin. Taltobulin is a common cytotoxic component in the preparation of antibody-drug conjugates (ADC Cytotoxin) and acts as a potent inhibitor of microtubules/tubulin (Microtubule/Tubulin). It disrupts microtubule polymerization, induces mitotic arrest, and triggers apoptosis (apoptosis).

(4R,5S)-MonomethylauristatinE intermediate-6 is an intermediate reactant in the synthesis of MonomethylauristatinE. MonomethylauristatinE (MMAE) is a microtubule/tubulin inhibitor with anticancer activity and is widely utilized as the cytotoxic component in antibody-drug conjugates (ADC Cytotoxin).

HDAC6-IN-41 (Compound E24) is a selective inhibitor of histone deacetylase 6 (HDAC6), effectively reducing the activity of HDAC6 and HDAC8 with IC50 values of 14 and 422 nM, respectively. It enhances the acetylation of α-tubulin and the histone site SMC3.

IOR-160 is a dual inhibitor of casein kinase 2 (CK2) and HDAC. It exhibits high selectivity for CK2 with an IC50 of 1.7 nM and demonstrates broad inhibitory activity against HDAC (HDAC1, 2, 3, and 6) with IC50 values of 3.3 nM, 24.0 nM, 3.9 nM, and 13.0 nM, respectively, while showing low activity against HDAC8. IOR-160 modulates critical cell signaling pathways by inhibiting AKT phosphorylation and increasing α-tubulin acetylation. The compound reduces tumor growth and burden through its dual inhibition of CK2/HDAC and is relevant for research on triple-negative breast cancer.

MEK Inhibitor II (2-Chloro-3-(N-succinimidyl)-1,4-naphthoquinone) is a selective MEK1 inhibitor (IC50=0.38 μM) that inhibits tubulin polymerization in Trypanosoma cruzi (IC50=6 μM) and exhibits inhibitory activity against trypanosomes (IC50=2.77 μM).

AZD 1152 is an orally bioavailable prodrug of AZD 1152-HQPA, a selective inhibitor of Aurora kinase B (IC50= 0.36 nM).1AZD 1152 is converted to AZD 1152-HQPA in plasma. Inhibition of Aurora B results in disruption of spindle checkpoint functions and chromosome alignment, resulting in inhibition of cytokinesis followed by apoptosis.2,3AZD 1152 inhibits tumor xenograft growthin vivo.4,5 1.Mortlock, A.A., Foote, K.M., Heron, N.M., et al.Discovery, synthesis, and in vivo activity of a new class of pyrazoloquinazolines as selective inhibitors of aurora B kinaseJ. Med. Chem.50(9)2213-2224(2007) 2.Popescu, R., Heiss, E.H., Ferk, F., et al.Ikarugamycin induces DNA damage, intracellular calcium increase, p38 MAP kinase activation and apoptosis in HL-60 human promyelocytic leukemia cellsMutation Research709-71060-66(2011) 3.Moore, A.S., Blagg, J., Linardopoulos, S., et al.Aurora kinase inhibitors: Novel small molecules with promising activity in acute myeloid and Philadelphia-positive leukemiasLeukemia24(4)671-678(2010) 4.Wilkinson, R.W., Odedra, R., Heaton, S.P., et al.AZD1152, a selective inhibitor of Aurora B kinase, inhibits human tumor xenograft growth by inducing apoptosisClin. Cancer. Res13(12)3682-3688(2007) 5.Yang, J., Ikezoe, T., Nishioka, C., et al.AZD1152, a novel and selective aurora B kinase inhibitor, induces growth arrest, apoptosis, and sensitization for tubulin depolymerizing agent or topoisomerase II inhibitor in human acute leukemia cells in vitro and in vivoBlood110(6)2034-2040(2007)

PARP1-IN-6, a dual-function inhibitor, targets both tubulin and PARP-1, demonstrating inhibitory concentration (IC50) values of 0.94 μM for tubulin and 0.48 μM for PARP-1.

Tubulin polymerization-IN-6 (compound 5f) is a potent tubulin polymerization inhibitor with an IC50 of 1.09 μM. It inhibits cell migration and tube formation, exhibits anti-angiogenic properties, and effectively hinders tumor growth in HT29 xenograft Balb/c nude mice [1].

Tubulin polymerization-IN-63 (compound 6) is an inhibitor of tubulin polymerization. It exhibits an IC50 value of 0.29 μM against MES-SA cells, making it suitable for use in cancer research.